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Flupirtine maleate

Catalog No. A10251
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NMDA 拮抗剂

Flupirtine maleate是Flupirine的盐形式，是一种非阿片类中枢性镇痛药，是一种选择性的神经元钾离子通道开放剂，也具有NMDA受体拮抗剂特性。了解更多

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GDC-0449 (Vismodegib)

Catalog No. A10258
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Hedgehog 拮抗剂

GDC-0449 (Vismodegib)是一种新型有效的，特异性hedgehog抑制剂，IC50为3 nM。了解更多

Product Citations (3)

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- Daniel Doheny, .et al. Combined inhibition of JAK2-STAT3 and SMO-GLI1/tGLI1 pathways suppresses breast cancer stem cells, tumor growth, and metastasis, Oncogene, 2020, Oct;39(42):6589-6605 PMID: 32929154
- Yi Yang, .et al. Tumidulin, a Lichen Secondary Metabolite, Decreases the Stemness Potential of Colorectal Cancer Cells, Molecules, 2018, Nov; 23(11): 2968 PMID: 30441806
- Olesen UH, .et al. Topical delivery of vismodegib using ablative fractional laser and micro-emulsion formulation in vitro, Lasers Surg Med, 2018, Aug 28 PMID: 30152536
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MDV3100

Catalog No. A10562
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Androgen receptor 拮抗剂

MDV3100(Enzalutamide)是一种androgen-receptor (AR)拮抗剂。在AR研究中强烈推荐的抑制剂。了解更多

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- Shiv Verma, .et al. Increased cytokine gene expression and cognition risk associated with androgen deprivation therapy, Prostate, 2022, Oct;82(14):1389-1399 PMID: 35821621
- Mi Chen, .et al. TRIM33 drives prostate tumor growth by stabilizing androgen receptor from Skp2-mediated degradation, EMBO Rep, 2022, Aug 3;23(8):e53468 PMID: 35785414
- Prem P Kushwaha, .et al. Role of solute carrier transporters SLC25A17 and SLC27A6 in acquired resistance to enzalutamide in castration-resistant prostate cancer, Mol Carcinog, 2021, Dec 22 PMID: 34939235
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FTY720 (Fingolimod)

Catalog No. A10408
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S1P Receptor 拮抗剂

FTY720 (Fingolimod)是ISP-1(肉豆蔻酸)的衍生物，ISP-1是中国草药Iscaria sinclarii的真菌代谢物，也是鞘氨醇的结构类似物。了解更多

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- Tina Sepasi, .et al. Targeted gene delivery to the brain using CDX-modified chitosan nanoparticles, BioImpacts, 2022, 28 May
- Zengzi Zhou, .et al. Effects of immunomodulatory drug Fingolimod (FTY720) on Chlamydia dissemination and pathogenesis, Infect Immun, 2020, Oct 19;88(11):e00281-20 PMID: 32868341
- Mayu Idehara, .et al. Inulooligosaccharides in Atractylodis lanceae rhizoma and Atractylodis rhizoma of hochuekkito formula are essential for regulation of the pulmonary immune system of immuno-compromised mice, Traditional & Kampo Medicine, 2020, 22 July
- Luwa Yuan, .et al. 14-3-3 signal adaptor and scaffold proteins mediate GPCR trafficking, Sci Rep, 2019, 9:11156 PMID: 31371790
- Sakai Y, .et al. Peyer's patch-immunomodulating glucans from sugar cane enhance protective immunity through stimulation of the hemopoietic system, Int J Biol Macromol, 2018, Nov 22;124:505-514 PMID: 30471397
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Bicalutamide (Casodex)

Catalog No. A10142
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Androgen Receptor 拮抗剂

Bicalutamide (Casodex)是一种口服非甾体抗雄激素，用于治疗前列腺癌和多毛症。了解更多

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- Mi Chen, .et al. TRIM33 drives prostate tumor growth by stabilizing androgen receptor from Skp2-mediated degradation, EMBO Rep, 2022, Aug 3;23(8):e53468 PMID: 35785414
- Takashi Azuma, .et al. Removal of pharmaceuticals in water by introduction of ozonated microbubbles, SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Anowara Khatun, .et al. Transcriptional Repression and Protein Degradation of the Ca2+-Activated K+ Channel KCa1.1 by Androgen Receptor Inhibition in Human Breast Cancer Cells, Front Physiol, 2018, 9: 312 PMID: 29713287
- Azuma T, .et al. Distribution of six anticancer drugs and a variety of other pharmaceuticals, and their sorption onto sediments, in an urban Japanese river, Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. Detection of pharmaceuticals and phytochemicals together with their metabolites in hospital effluents in Japan, and their contribution to sewage treatment plant influents, Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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Amisulpride

Catalog No. A10067
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Dopamine Receptor 拮抗剂

Amisulpride是一种非典型抗精神病药，用于治疗精神分裂症的精神病和双相情感障碍的躁狂发作。了解更多

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Maraviroc (UK-427857)

Catalog No. A10556
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CCR 拮抗剂

Maraviroc (UK-427857)是CCR5受体拮抗剂类别的抗逆转录病毒药物，用于治疗HIV感染。了解更多

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- Roman V Uzhachenko, .et al. Metabolic modulation by CDK4/6 inhibitor promotes chemokine-mediated recruitment of T cells into mammary tumors, Cell Rep, 2021, Apr 6;35(1):108944 PMID: 33826903
- Karampoor S, .et al. Maraviroc attenuates the pathogenesis of experimental autoimmune encephalitis, Int Immunopharmacol, 2020, Mar;80:106138 PMID: 32007705
- Taisuke Ito, .et al. CCR5 is a novel target for the treatment of experimental alopecia areata, JCIA, 2020, 22 January
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Agomelatine

Catalog No. A10048
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5-HT Receptor 拮抗剂

Agomelatine是一种褪黑素激动剂（MT1和MT2受体）和5-HT2C拮抗剂。了解更多

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Candesartan (Atacand)

Catalog No. A10175
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RAAS 拮抗剂

Candesartan (Atacand)是一种血管紧张素受体阻滞剂（也称为血管紧张素II受体拮抗剂或AIIRA）。了解更多

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- Hideki Kobara, .et al. Antihypertensive drug telmisartan inhibits cell proliferation of gastrointestinal stromal tumor cells in vitro, Molecular Medicine Reports, 2020, 22(2)
- Dao-Lai Zhang, .et al. Gq activity- and β-arrestin-1 scaffolding-mediated ADGRG2/CFTR coupling are required for male fertility, eLife, 2018, 7: e33432 PMID: 29393851
- Toshihide Kashihara, .et al. Angiotensin II activates CaV1.2 Ca2+ channels through β‐arrestin2 and casein kinase 2 in mouse immature cardiomyocytes, J Physiol, 2017, Jul 1; 595(13): 4207-4225 PMID: 28295363
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Ki16425

Catalog No. A10501
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LPA Receptor 拮抗剂

ki16425是对LPA1和LPA3具有选择性的LPA受体拮抗剂，对人LPA1、LPA2和LPA3受体分别显示Ki值为0.34、6.5和0.93 μM。了解更多

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- Maria F Fernandes, .et al. Glucagon-like Peptide-1 Secretion Is Inhibited by Lysophosphatidic Acid, Int J Mol Sci, 2022, Apr 9;23(8):4163 PMID: 35456981
- Rieko Suenaga, .et al. Lateral access mechanism of LPA receptor probed by molecular dynamics simulation, PLoS One, 2022, Feb 3;17(2):e0263296 PMID: 35113924
- Inoue A, .et al. Illuminating G-Protein-Coupling Selectivity of GPCRs, Cell, 2019, Jun 13;177(7):1933-1947 PMID: 31160049
- Taniguchi R, .et al. Structural insights into ligand recognition by the lysophosphatidic acid receptor LPA6, Nature, 2017, Aug 17;548(7667):356-360 PMID: 28792932
- T. HASHIMOTO, .et al. Generalized pruritus in primary sclerosing cholangitis: implications of histamine release by lysophosphatidic acid., Br J Dermatol., 2015, Nov;173(5):1334-6 PMID: 26122943
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JTC-801

Catalog No. A11076
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Opioid Receptor 拮抗剂

JTC-801是nociceptin receptor（也称为ORL-1受体）的选择性拮抗剂。了解更多

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- Lihao Gu, .et al. 10-Hydroxy-2-Decenoic Acid in Royal Jelly Extract Induced Both Filaggrin and Amino Acid in a Cultured Human Three-Dimensional Epidermis Model, Cosmetics, 2017, 4(4), 48
- Toshio Yawata, .et al. Brain opioid and nociceptin receptors are involved in regulation of bombesin-induced activation of central sympatho-adrenomedullary outflow in the rat, Mol Cell Biochem, 2016, Jan;411(1-2):201-11 PMID: 26427671
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LDE225 (NVP-LDE225, Sonidegib)

Catalog No. A10520
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Smo 拮抗剂

LDE225 (NVP-LDE225)是一种强效、选择性和口服生物可利用的平滑(SMO)拮抗剂，通过平滑受体(SMO)的拮抗作用抑制hedgehog (Hh)信号通路。了解更多

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- Daniel Doheny, .et al. Combined inhibition of JAK2-STAT3 and SMO-GLI1/tGLI1 pathways suppresses breast cancer stem cells, tumor growth, and metastasis, Oncogene, 2020, Oct;39(42):6589-6605 PMID: 32929154
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NPS-2143 (SB-262470)

Catalog No. A11140
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CaSR 拮抗剂

NPS-2143 (SB-262470)是一种选择性的Ca2+感应受体拮抗剂，显示可阻止HEK293细胞中表达的人Ca2+受体引起的细胞质Ca2+浓度增加，IC50为43 nM。了解更多

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SB-705498

Catalog No. A11143
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TRPV1 拮抗剂

SB-705498是有效，选择性和口服生物利用的TRPV1拮抗剂，抑制TRPV1的Capsaicin，酸和热激活，IC50分别为3 nM， 0.1 nM和6 nM，该作用具有一定的电压依赖性，作用于TRPV1比作用于TRPM8选择性高100倍以上。了解更多

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Fesoterodine fumarate (Toviaz)

Catalog No. A10386
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AChR 拮抗剂

Fesoterodine fumarate是一种用于尿急的药物，可减少尿液通过的频率并促使尿失禁。了解更多

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PF 3716556

Catalog No. A11408
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ATPase 拮抗剂

PF 3716556是H+,K+-ATPase酶抑制剂(在人类重组离子渗漏试验中PIC50 = 6)。了解更多

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Cyproterone acetate

Catalog No. A11409
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Androgen Receptor 拮抗剂

Cyproterone acetate是17-羟孕酮的合成衍生物，可作为雄激素受体拮抗剂以及具有弱孕激素和糖皮质激素活性的弱孕激素受体激动剂。了解更多

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Aprepitant (MK-0869)

Catalog No. A10083
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neurokinin-1 receptor 拮抗剂

Aprepitant (MK-0869)被归类为NK1拮抗剂。已经显示，阿瑞匹坦通过阻止P物质降落在大脑神经元受体上，从而抑制细胞毒性化疗药物引起的急性呕吐和延迟呕吐。还显示出它能增加5-HT3受体拮抗剂恩丹西酮和皮质类固醇地塞米松的活性，它们也可用于预防化学疗法引起的恶心和呕吐。了解更多

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- Kodji X, .et al. Sensory nerves mediate spontaneous behaviors in addition to inflammation in a murine model of psoriasis, FASEB J, 2018, Sep 11:fj201800395RR PMID: 30204499
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5-hydroxymethyl tolterodine (PNU 200577)

Catalog No. A11166
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muscarinic receptor 拮抗剂

5-hydroxymethyl tolterodine (PNU 200577)是托特罗定的代谢产物，tolterodine是一种用于治疗尿失禁的毒蕈碱受体拮抗剂。了解更多

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BRL-15572 dihydrochloride

Catalog No. A11178
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5-HT1D receptor 拮抗剂

BRL-15572是一种选择性的h5-HT1D拮抗剂，相对于h5-HT1B表现出60倍的选择性，对一系列其他受体类型的亲和力很小或没有亲和力。了解更多

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Naftopidil 2HCl

Catalog No. A10619
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5-HT1A and α1-adrenergic receptor 拮抗剂

Naftopidil 2HCl是选择性5-HT1A和α1-肾上腺素能受体拮抗剂，IC50分别为0.1μM和0.2μM。了解更多

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Puerarin (Kakonein)

Catalog No. A10759
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5-HT2C receptor 拮抗剂

Puerarin (Kakonein)是几种已知的异黄酮之一。Puerarin是5-HT2C受体和苯二氮卓类拮抗剂。Puerarin正在研究作为一种自微乳化药物递送系统。了解更多

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- Takashi Azuma, .et al. Removal of pharmaceuticals in water by introduction of ozonated microbubbles, SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. Distribution of six anticancer drugs and a variety of other pharmaceuticals, and their sorption onto sediments, in an urban Japanese river, Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. Detection of pharmaceuticals and phytochemicals together with their metabolites in hospital effluents in Japan, and their contribution to sewage treatment plant influents, Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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Zibotentan (ZD4054)

Catalog No. A11006
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ETA-receptor 拮抗剂

Zibotentan (ZD4054)是一种有效且特异性的ETA受体（内皮素A受体）拮抗剂（IC50 = 21 nM），对ETB没有抑制活性。了解更多

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- Tony Ngo, .et al. Orphan receptor ligand discovery by pickpocketing pharmacological neighbors, Nat Chem Biol, 2017, Feb; 13(2): 235-242 PMID: 27992882
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Tropisetron (ICS 205930)

Catalog No. A11226
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5-HT3 拮抗剂

Tropisetron (ICS 205930)是5-羟色胺5-HT3受体拮抗剂，主要用作止吐药，用于治疗化疗后的恶心和呕吐。了解更多

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Rocuronium bromide

Catalog No. A10803
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AchR 拮抗剂

Rocuronium Bromide是一种竞争性AchR拮抗剂，用于现代麻醉中。了解更多

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Ginkgolide B

Catalog No. A10429
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PAFR 拮抗剂

Ginkgolide B (BN 52021)是一种PAFR拮抗剂，IC50为3.6 μM。了解更多

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MK 3207 HCl

Catalog No. A10598
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CGRP Receptor 拮抗剂

MK 3207 hydrochloride是一种有效的CGRP受体拮抗剂，IC50为0.12 nM。了解更多

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- Marlene Dallmayer, .et al. Targeting the CALCB/RAMP1-axis inhibits growth of Ewing sarcoma, bioRxiv, 2018, 2018
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Tolterodine tartrate (Detrol LA)

Catalog No. A10937
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muscarinic receptor 拮抗剂

Tolterodine tartrate (Detrol LA)是毒蕈碱受体拮抗剂。了解更多

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Ambrisentan (BSF 208075)

Catalog No. A11291
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EndothelinA receptor 拮抗剂

Ambrisentan (BSF 208075)充当内皮素受体拮抗剂，对A型内皮素受体（ETA）具有选择性。了解更多

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- Naoki Dohi, .et al. Quantitative real-time measurement of endothelin-1-induced contraction in single non-activated hepatic stellate cells, PLoS One, 2021, 16(8): e0255656 PMID: 34343209
- Tony Ngo, .et al. Orphan receptor ligand discovery by pickpocketing pharmacological neighbors, Nat Chem Biol, 2017, Feb; 13(2): 235-242 PMID: 27992882
- Toshiaki Okamoto, .et al. Antifibrotic effects of ambrisentan, an endothelin-A receptor antagonist, in a non-alcoholic steatohepatitis mouse model, World J Hepatol, 2016, Aug 8; 8(22): 933-941 PMID: 27574547
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Atropine

Catalog No. A10098
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mAChR 拮抗剂

Atropine是M1，M2，M3，M4和M5型毒蕈碱乙酰胆碱受体的竞争性拮抗剂。了解更多

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Tamoxifen Citrate

Catalog No. A10885
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Estrogen receptor 拮抗剂

Tamoxifen Citrate是哺乳动物甾醇异构酶的选择性和有效抑制剂。了解更多

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- Renu Sudhakar, .et al. Bazedoxifene, a Postmenopausal Drug, Acts as an Antimalarial and Inhibits Hemozoin Formation, Microbiol Spectr, 2022, Jun 29;10(3) PMID: 35616371
- Takashi Azuma, .et al. Removal of pharmaceuticals in water by introduction of ozonated microbubbles, SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. Distribution of six anticancer drugs and a variety of other pharmaceuticals, and their sorption onto sediments, in an urban Japanese river, Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. Detection of pharmaceuticals and phytochemicals together with their metabolites in hospital effluents in Japan, and their contribution to sewage treatment plant influents, Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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MRS 2578

Catalog No. A11486
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P2Y6 Receptor 拮抗剂

MRS 2578是P2Y6核苷酸受体的选择性拮抗剂。了解更多

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SB269970 HCl

Catalog No. A11925
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5-HT7 receptor 拮抗剂

SB269970 HCl是有效的选择性5-HT7受体拮抗剂。了解更多

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LCL-161

Catalog No. A11928
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拮抗剂of IAPs抑制剂

LCL161是口服生物可利用的第二个线粒体衍生的半胱天冬酶（SMAC）类似物激活剂，也是IAP（细胞凋亡抑制蛋白）家族蛋白的抑制剂，具有潜在的抗肿瘤活性，抑制 HEK293 细胞中 XIAP 和 MDA-MB-231细胞中 cIAP1 的 IC50分别为 35 和 0.4 nM。了解更多

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- Han-Hee Park, .et al. RIPK3 activation induces TRIM28 derepression in cancer cells and enhances the anti-tumor microenvironment, Mol Cancer, 2021, Aug 21;20(1):107 PMID: 34419074
- Se-Yeon Park, .et al. Reduction in MLKL-mediated endosomal trafficking enhances the TRAIL-DR4/5 signal to increase cancer cell death, Cell Death & Disease, 2020, 11:744 PMID: 32917855
- J Chen, .et al. Interferon-γ induces the cell surface exposure of phosphatidylserine by activating MLKL in the absence of caspase-8 activity, JBC, 2019, June PMID: 31217278
- Choi SW, .et al. PELI1 Selectively Targets Kinase-Active RIP3 for Ubiquitylation-Dependent Proteasomal Degradation, Mol Cell, 2018, Jun 7;70(5):920-935.e7 PMID: 29883609
- Han-Hee Park, .et al. HS-1371, a novel kinase inhibitor of RIP3-mediated necroptosis, Exp Mol Med, 2018, Sep; 50(9): 125 PMID: 30237400
- Gi-Bang Koo, .et al. Methylation-dependent loss of RIP3 expression in cancer represses programmed necrosis in response to chemotherapeutics, Cell Res, 2015, Jun; 25(6): 707-725 PMID: 25952668
- Kim SK, .et al. Upregulated RIP3 Expression Potentiates MLKL Phosphorylation-Mediated Programmed Necrosis in Toxic Epidermal Necrolysis, J Invest Dermatol, 2015, Aug;135(8):2021-2030 PMID: 25748555
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Memantine hydrochloride

Catalog No. A11708
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NMDA receptor 拮抗剂

Memantine hydrochloride是nmda受体的拮抗剂，与离子通道位点结合。它还是CYP2B6和CYP2D6抑制剂，作用于重组CYP2B6和CYP2D6，Ki分别为0.51 nM和94.9 μM。它被用于治疗帕金森综合征。了解更多

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Orphenadrine citrate

Catalog No. A11712
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NMDA receptor 拮抗剂

Orphenadrine柠檬酸盐是NMDA受体拮抗剂，Ki为6.0μM，还是HERG钾离子通道阻断剂。了解更多

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Lafutidine

Catalog No. A11714
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H2 receptor 拮抗剂

Lafutidine是具有多峰作用机制的第二代H2受体拮抗剂。了解更多

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Proparacaine HCl

Catalog No. A11715
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Voltage-gated sodium channels 拮抗剂

Proparacaine HCl是一种电压门控钠通道拮抗剂，ED50为3.4 mM。了解更多

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Buflomedil HCl

Catalog No. A11737
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VEGFR 拮抗剂

Buflomedil HCl是一种用于治疗外周血管疾病的血管活性剂。了解更多

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Aminophylline

Catalog No. A10066
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Adenosine receptor 拮抗剂

Aminophylline是一种非选择性的腺苷受体拮抗剂和磷酸二酯酶抑制剂，能够逆转局部缺血引起的bradyasystole。了解更多

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Asenapine maleate

Catalog No. A10091
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H1 拮抗剂

Asenapine maleate平对多种受体具有高亲和力（pKi），包括5-羟色胺5-HT1A（8.6），5-HT1B（8.4），5-HT2A（10.2），5-HT2B（9.8），5-HT2C（10.5），5 -HT5A（8.8），5-HT6（9.5）和5-HT7（9.9）受体，肾上腺素α1（8.9），α2A（8.9），α2B（9.5）和α2C（8.9）受体，多巴胺D1（ 8.9），D2（8.9），D3（9.4）和D4（9.0）受体以及组胺H1（9.0）和H2（8.2）受体。了解更多

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- Keisuke Obara, .et al. Inhibitory Effects of Antipsychotics on the Contractile Response to Acetylcholine in Rat Urinary Bladder Smooth Muscles, Biol Pharm Bull, 2021, 44, 1140-1150
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Cimetidine

Catalog No. A10218
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H2-receptor 拮抗剂

Cimetidine是一种抑制胃酸产生的组胺H2受体拮抗剂。了解更多

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Dyphylline

Catalog No. A10339
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Adenosine receptor 拮抗剂

Dyphylline是黄嘌呤衍生物，具有支气管扩张药和血管扩张药的作用。它充当腺苷受体拮抗剂和磷酸二酯酶抑制剂。了解更多

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Ki16198

Catalog No. A11966
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LPA Receptor 拮抗剂

Ki16198是有效的LPA受体拮抗剂，可抑制LPA1和LPA3诱导的肌醇磷酸生成，Ki分别为0.34μM和0.93μM。了解更多

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Bepotastine Besilate

Catalog No. A11340
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Histamine Receptor 拮抗剂

Bepotastine Besilate是组胺H1受体激动剂。了解更多

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- Reiko Watanabe, .et al. Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration, J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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MK-0517 (Fosaprepitant)

Catalog No. A11756
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neurokinin-1 receptor 拮抗剂

MK-0517 (Fosaprepitant,L-758,298)是Aprepitant的水溶性磷酰基前药，它是NK1拮抗剂。了解更多

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GW 9662

Catalog No. A11984
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PPARγ 拮抗剂

GW 9662是一种选择性PPARγ拮抗剂（PPARγ，PPARα和PPARδ的IC50值分别为3.3、32和2000 nM）。了解更多

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Gallamine triethiodide

Catalog No. A10417
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mAChR M2 拮抗剂

Gallamine Triethiodide是一种具有显著心脏选择性的mAChR M2拮抗剂。了解更多

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Ipratropium bromide

Catalog No. A10476
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Ipratropium bromide是毒蕈碱拮抗剂、支气管扩张剂、阿托品的N-异丙基盐。了解更多

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Mianserin hydrochloride

Catalog No. A10588
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5-HT2/5-HT1 拮抗剂

Mianserin hydrochloride是5-HT2/5-HT1拮抗剂。对5-HT6非选择性5-HT2受体拮抗剂具有中等亲和力。对5-HT6具有中等亲和力。了解更多

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