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Solifenacin succinate

Catalog No. A11215
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muscarinic M3 receptor antagoinst

Solifenacin succinate是毒蕈碱M3受体拮抗剂，用于治疗尿失禁。了解更多

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SB-408124

Catalog No. A11567
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OX Receptor 拮抗剂

SB-408124是一种选择性的非肽orexin OX1受体拮抗剂(人OX1和OX2受体的Kb值分别为21.7和1405 nM)。体内口服后阻断orexin-A诱导的修饰。了解更多

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RU 58841

Catalog No. A11541
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AR 拮抗剂

RU 58841，也称为PSK-3841或HMR-3841，是一种非甾体类抗雄激素药物。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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SYN-115 (Tozadenant)

Catalog No. A11560
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A2a receptor 拮抗剂

SYN115是口服，有效和选择性的腺苷2a（A2a）受体抑制剂，作用于人类和恒河猴的 adenosine A2A 受体，Ki 值分别为 11.5 nM 和 6 nM。了解更多

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Firategrast (SB 683699)

Catalog No. A12787
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α4β1/α4β7 integrin 拮抗剂

Firategrast (SB 683699)是一种口服可生物利用的alpha4 beta1/alpha4 beta7整联蛋白拮抗剂，旨在减少淋巴细胞向中枢神经系统（CNS）的运输。了解更多

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- Higuchi S, .et al. Inhibition of the integrin signal constitutes a mouse iPS cell niche, Dev Growth Differ, 2016, Sep;58(7):586-99 PMID: 27633818
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SB225002

Catalog No. A14209
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CXCR2 拮抗剂

SB225002是一种有效的选择性CXCR2拮抗剂，IC50为22 nM，可抑制白介素IL-8与CXCR2的结合，选择性是其他测试的7-TMR的150倍以上。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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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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AMD3100 (Plerixafor)

Catalog No. A13074
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CXCR4 拮抗剂

AMD3100 (Plerixafor)是用于增殖造血干细胞的免疫刺激剂，并且是用于动员造血干细胞进行移植的趋化因子受体-4拮抗剂。了解更多

Product Citations (11)

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- Hitoshi Maeda, .et al. Cell-penetrating albumin enhances the sublingual delivery of antigens through macropinocytosis, Int J Biol Macromol, 2022, Sep 17;221:1439-1452 PMID: 36126807
- Jingying Chen, .et al. Brain vascular damage-induced lymphatic ingrowth is directed by Cxcl12b/Cxcr4a, Development, 2022, Jul 1;149(13) PMID: 35694896
- Narubhorn Ongprakobkul, .et al. Effects of local vs systemic administration of CXCR4 inhibitor AMD3100 on orthodontic tooth movement in rats, Am J Orthod Dentofacial Orthop, 2022, Mar 2;S0889-5406(22)00107-X PMID: 35248418
- Chunliang Liu, .et al. Positive effects of selenium supplementation on selenoprotein S expression and cytokine status in a murine model of acute liver injury, J Trace Elem Med Biol, 2022, Jan 10;71:126927 PMID: 35030482
- Eri Watanabe, .et al. Stromal cell-derived factor 1 (SDF1) attenuates platelet-derived growth factor-B (PDGF-B)-induced vascular remodeling for adipose tissue expansion in obesity, Angiogenesis, 2020, Jul 22 PMID: 32699964
- Alessandra Esposito, .et al. Role of Prx1-expressing skeletal cells and Prx1-expression in fracture repair, Bone, 2020, Jul 3;139:115521 PMID: 32629173
- Kentaro Suzuki, .et al. C-terminal?Cmodifed LY2510924: a versatile scafold for targeting C-X-C chemokine receptor type 4, Sci Rep, 2019, 9: 15284
- Ichimizu S, .et al. Cell-penetrating mechanism of intracellular targeting albumin: Contribution of macropinocytosis induction and endosomal escape, J Control Release, 2019, May 10;304:156-163 PMID: 31082432
- Nan Li, .et al. LPS-induced CXCR7 expression promotes gastric Cancer proliferation and migration via the TLR4/MD-2 pathway, Diagn Pathol, 2019, Jan 12;14(1):3 PMID: 30636642
- Thida W, .et al. The role of conventional antibodies targeting the CD4 binding site and CD4-induced epitopes in the control of HIV-1 CRF01_AE viruses, Biochem Biophys Res Commun, 2018, Nov 20. pii: S0006-291X(18)32477-X PMID: 30470571
- Henry R. Hampton, .et al. Microbe-dependent lymphatic migration of neutrophils modulates lymphocyte proliferation in lymph nodes, Nat Commun, 2015, 6: 7139 PMID: 25972253
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Exherin (ADH-1)

Catalog No. A13689
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N-cadherin 拮抗剂

Exherin (ADH-1)是一种小的环状五肽血管靶向药物，具有潜在的抗肿瘤和抗血管生成活性。了解更多

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- CM Madl, .et al. Matrix Remodeling Enhances the Differentiation Capacity of Neural Progenitor Cells in 3D Hydrogels, Adv Sci, 2019, 1801716
- Christopher M. Madl, .et al. Maintenance of Neural Progenitor Cell Stemness in 3D Hydrogels Requires Matrix Remodeling, Nat Mater, 2017, Dec; 16(12): 1233-1242 PMID: 29115291
- Andrew J. Lindsay, .et al. Rab coupling protein mediated endosomal recycling of N-cadherin influences cell motility, Oncotarget, 2017, Dec 1; 8(62): 104717-104732 PMID: 29285208
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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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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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GANT61

Catalog No. A13252
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GLI 拮抗剂

GANT61是GLI1和GLI2诱导的转录的抑制剂，以5μM的IC50抑制hedgehog，对其他途径（例如TNF和糖皮质激素受体基因反式激活）表现出选择性。了解更多

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- Cheng Zhou, .et al. GLI1 reduces drug sensitivity by regulating cell cycle through PI3K/AKT/GSK3/CDK pathway in acute myeloid leukemia, Cell Death Dis, 2021, Mar 3;12(3):231 PMID: 33658491
- Hui Liang, .et al. Targeting the PI3K/AKT pathway via GLI1 inhibition enhanced the drug sensitivity of acute myeloid leukemia cells, Sci Rep, 2017, 7: 40361 PMID: 28098170
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SB-222200

Catalog No. A15230
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NK3 receptor 拮抗剂

SB 222200是人类NK-3受体（Ki = 4.4 nM）的选择性，可逆和竞争性拮抗剂，可有效穿越血脑屏障。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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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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TCS 1102

Catalog No. A13439
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Dual orexin receptor 拮抗剂

TCS 1102是一种有效的双重食欲素受体拮抗剂（OX2和OX1受体的Ki值分别为0.2和3 nM）。了解更多

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AM630

Catalog No. A14993
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CB2 拮抗剂

AM630是一种选择性CB2拮抗剂，Ki为31.2 nM，选择性是CB1受体的150倍以上。了解更多

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- Md Shah Sufian, .et al. Early suppression of the endocannabinoid degrading enzymes FAAH and MAGL alters locomotor development in zebrafish, J Exp Biol, 2021, 21 JUNE
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INCB 3284 dimesylate

Catalog No. A11104
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HCCR2 拮抗剂

INCB 3284 dimesylate是一种有效的选择性hCCR2拮抗剂，对单核细胞趋化因子分子与hCCR2的结合和趋化活性表现出强烈的拮抗作用。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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AMG517

Catalog No. A12727
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TRPV1 拮抗剂

AMG 517是有效的选择性TRPV1拮抗剂。了解更多

Product Citations (2)

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- Jun Hai, .et al. Intragastric administration of AMG517, a TRPV1 antagonist, enhanced activity-dependent energy metabolism via capsaicin-sensitive sensory nerves in mice, Biosci Biotechnol Biochem, 2020, Jul 7;1-7 PMID: 32633621
- Hai J, .et al. Differences in the effects of TRPV1 antagonists on energy metabolism in mice, Biomed Res, 2018, 39(6):279-286 PMID: 30531157
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FPS-ZM1

Catalog No. A15806
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RAGE 拮抗剂

FPS-ZM1抑制表达RAGE的细胞中Aβ40和Aβ42诱导的细胞应激。了解更多

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Flumazenil

Catalog No. A10397
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Benzodiazepine 拮抗剂

Flumazenil是竞争性抑制GABA/苯二氮卓受体复合物上苯二氮卓识别位点的活性。Flumazenil在一些活性动物模型中是弱部分激动剂，但在人类中很少或没有激动剂活性。了解更多

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Sitaxsentan sodium (TBC-11251)

Catalog No. A11564
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ETA receptor 拮抗剂

Sitaxsentan sodium (TBC-11251)是一种选择性内皮素受体A拮抗剂，IC50和Ki分别为1.4 nM和0.43 nM。了解更多

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AZD1981

Catalog No. A13186
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CRTH2 receptor 拮抗剂

AZD1981作为疾病相关细胞系统的有效拮抗剂，可抑制DK-PGD2诱导的人嗜酸性粒细胞CD11b表达，IC50为10 nM。了解更多

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T0070907

Catalog No. A11588
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PPAR-γ 拮抗剂

T0070907是一种有效的选择性PPARγ拮抗剂，无细胞试验中IC50为1 nM，比作用于PPARα和PPARδ选择性高800倍以上。了解更多

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Istradefylline (KW-6002)

Catalog No. A11451
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A2A 拮抗剂

Istradefylline (KW-6002)是A2A受体的选择性拮抗剂。了解更多

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- PU Hamor, .et al. The Role of Glutamate mGlu5 and Adenosine A2a Receptor Interactions in Regulating Working Memory Performance and Persistent Cocaine Seeking in Rats, Prog Neuropsychopharmacol Biol Psychiatry, 2020, Dec 20;103:109979 PMID: 32470496
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Octreotide Acetate

Catalog No. A12782
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somatostatin receptor 拮抗剂

Octreotide是sst2，sst3和sst5生长抑素受体的肽激动剂。克隆的人类生长抑素受体的IC50/Kd值（nM）为：290-1140（sst1），0.4-2.1（sst2），4.4-34.5（sst3），> 1000（sst4）和5.6-32（sst5）。了解更多

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SB 399885 HCl

Catalog No. A14102
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5-HT6 拮抗剂

SB 399885 hydrochloride是一种有效的，脑渗透剂和口服活性的SR-6拮抗剂。它对SR-6的选择性比其他血清素受体高200倍（对于人类重组，天然大鼠和天然人类SR-6受体，pKi值分别为9.11、8.81和9.02）。了解更多

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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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A 740003

Catalog No. A11316
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P2X7 receptor 拮抗剂

A740003是P2X7受体的新型竞争性拮抗剂（人的IC50值= 40 nM，大鼠的IC50值= 18 nM）。了解更多

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Olanzapine (LY170053)

Catalog No. A10667
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5-HT Receptors/D2 dopamine receptor 拮抗剂

Olanzapine (LY170053)对5-HT2血清素和D2多巴胺受体拮抗剂具有高亲和力。了解更多

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BX471

Catalog No. A14409
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CCR1 拮抗剂

BX471是一种有效的选择性非肽CCR1拮抗剂（对于人CCR1，Ki = 1 nM），对CCR1的选择性是CCR2，CCR5和CXCR4的250倍。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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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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NBQX

Catalog No. A13109
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AMPA Receptor 拮抗剂

NBQX是一种有效，选择性和竞争性的AMPA受体拮抗剂。了解更多

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Clozapine N-oxide

Catalog No. A15048
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5-HT1C receptor 拮抗剂

Clozapine N-oxide是氯氮平的主要代谢产物，在体外可降低SR-2A（5-HT2血清素受体）密度。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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TCN 201

Catalog No. A11947
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NMDA Receptor 拮抗剂

TCN 201是对NR1/NR2A相对于含NR1/NR2B的受体具有选择性的NMDA受体拮抗剂。了解更多

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StemRegenin 1 (SR1)

Catalog No. A12945
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AhR 拮抗剂

StemRegenin 1 (SR1)是一种细胞可渗透的嘌呤衍生物，作为芳香烃受体的拮抗剂，促进造血干细胞(HSC)的自我更新。了解更多

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Ziprasidone

Catalog No. A15286
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5-HT/dopamine receptor 拮抗剂

Ziprasidone是5-HT（5-羟色胺）和多巴胺受体拮抗剂的组合，具有抗精神病活性。了解更多

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WAY-100635

Catalog No. A11182
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5HT1A 拮抗剂

WAY-100635最初被认为是选择性的5-HT1A受体拮抗剂，但随后的研究表明它也可作为D4受体的有效全效激动剂。了解更多

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Ketanserin (Vulketan Gel)

Catalog No. A10497
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5-HT2A serotonin receptor 拮抗剂

Ketanserin (Vulketan Gel)是大鼠和人5-HT2A血清素受体拮抗剂，Ki为2.5 nM。了解更多

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cis-(Z)-Flupentixol dihydrochloride

Catalog No. A12347
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Dopamine receptor 拮抗剂

cis-(Z)-Flupentixol dihydrochloride是多巴胺受体拮抗剂、抗精神病药物、抗精神病药物。了解更多

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ODM-201

Catalog No. A15797
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Androgen receptor 拮抗剂

ODM-201是一种有效且完全的人类AR（hAR）拮抗剂，IC50值为26 nM。了解更多

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Irbesartan (Avapro)

Catalog No. A10477
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AT1 拮抗剂

Irbesartan (Avapro)是一种血管紧张素II受体拮抗剂，IC50为1.3 nM，主要用于治疗高血压。了解更多

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Phenoxybenzamine hydrochloride

Catalog No. A10719
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α-adrenergic (AR) 拮抗剂/CaM 抑制剂

Phenoxybenzamine hydrochloride是一种细胞可渗透的，非特异性的，不可逆的α-肾上腺素（AR）拮抗剂，也可作为CaM抑制剂。了解更多

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Tandospirone

Catalog No. A13293
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5-HT Receptor 拮抗剂

Tandospirone是5HT1A受体的部分激动剂。它以剂量依赖性方式显着降低氟哌啶醇诱导的运动迟缓。了解更多

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BH3I-1

Catalog No. A16061
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Bcl-XL 拮抗剂

BH3I-1是Bcl-XL-BH3 domain interaction抑制剂，Ki值为2.4 μM。它是一种Bcl-2家族蛋白的选择性抑制剂。了解更多

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