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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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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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Vorapaxar (SCH 530348)

Catalog No. A12832
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PAR-1 拮抗剂

Vorapaxar (SCH 530348)是一种有效的口服活性凝血酶受体（PAR-1）拮抗剂，Ki为8.1 nM。了解更多

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- Cansu Tekin, .et al. Macrophage-secreted MMP9 induces mesenchymal transition in pancreatic cancer cells via PAR1 activation, Cell Oncol (Dordr), 2020, Aug 18 PMID: 32809114
- Cansu Tekin, .et al. PAR1 signaling on tumor cells limits tumor growth by maintaining a mesenchymal phenotype in pancreatic cancer, Oncotarget, 2018, Aug 10; 9(62): 32010-32023 PMID: 30174793
- Claushuis TA, .et al. Thrombin contributes to protective immunity in pneumonia-derived sepsis via fibrin polymerization and platelet-neutrophil interactions, J Thromb Haemost, 2017, Apr;15(4):744-757 PMID: 28092405
- Maaike Waasdorp, .et al. Plasmin reduces fibronectin deposition by mesangial cells in a protease-activated receptor-1 independent manner, Biochem Biophys Rep, 2017, Jul; 10: 152-156 PMID: 29114573
- Joseph C. Mudd, .et al. Inflammatory Function of CX3CR1+ CD8+ T Cells in Treated HIV Infection Is Modulated by Platelet Interactions, J Infect Dis, 2016, Dec 15; 214(12): 1808-1816 PMID: 27703039
- Corey E. Tabit, .et al. Elevated Angiopoietin-2 Level in Patients With Continuous-Flow Left Ventricular Assist Devices Leads to Altered Angiogenesis and Is Associated With Higher Non-Surgical Bleeding, Circulation, 2016, Jul 12; 134(2): 141-152 PMID: 27354285
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Rolapitant

Catalog No. A13680
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NK1 receptor 拮抗剂

Rolapitant，也称为SCH-619734，是一种选择性的，可生物利用的CNS渗透性神经激肽NK1受体拮抗剂，在呕吐动物模型中显示出行为效应。了解更多

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- Bubak AN, .et al. Varicella Zoster Virus Induces Nuclear Translocation of the Neurokinin-1 Receptor, Promoting Lamellipodia Formation and Viral Spread in Spinal Astrocytes, J Infect Dis, 2018, Sep 8;218(8):1324-1335 PMID: 29788447
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Imatinib (Gleevec)

Catalog No. A10259
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PDGFR 抑制剂

Imatinib (Gleevec)是一种多靶点酪氨酸激酶抑制剂，抑制v-Abl、c-Kit和PDGFR的IC50分别为0.6，0.1和0.1 μM。了解更多

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- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Takafumi Shima, .et al. Glucose transporter-1 inhibition overcomes imatinib resistance in gastrointestinal stromal tumor cells, Oncol Rep, 2022, 47: 7 PMID: 34738628
- 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
- BM Duggan, .et al. RIPK2 Dictates Insulin Responses to Tyrosine Kinase Inhibitors in Obese Male Mice, Endocrinology, 2020, May 30;bqaa086 PMID: 32473019
- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
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AMD 070

Catalog No. A11315
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CXCR4 拮抗剂

AMD 070是CXCR4趋化因子受体拮抗剂。了解更多

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- Uchida D, .et al. Effect of a novel orally bioavailable CXCR4 inhibitor, AMD070, on the metastasis of oral cancer cells, Oncol Rep, 2018, Jul;40(1):303-308 PMID: 29749473
- Mamoru Morimoto, .et al. Enhancement of the CXCL12/CXCR4 axis due to acquisition of resistance in pancreatic cancer: effect of CXCR4 antagonists, BMC Cancer, 2016, 16: 305 PMID: 27175473
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GSK-3787

Catalog No. A12391
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PPAR 拮抗剂

GSK-3787是一种有效的选择性过氧化物酶体增殖物激活受体δ（PPARδ）拮抗剂（pIC50 = 6.6）。了解更多

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Labetalol HCl

Catalog No. A14239
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alpha1/beta adrenergic receptors 拮抗剂

Labetalol HCl是选择性α1-肾上腺素能受体和非选择性β-肾上腺素能受体的双重拮抗剂。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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Vicriviroc Malate

Catalog No. A10971
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CCR5 拮抗剂

Vicriviroc Malate是CCR5拮抗剂，也是HIV-1进入靶细胞的有效抑制剂，对HIV分离株的平均IC50 = 0.46 nM，IC50 = 1?10 nM（n = 52）。了解更多

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- Tomohiro Nabekura, .et al. Effects of Antiviral Drugs on Organic Anion Transport in Human Placental BeWo Cells, Antimicrob Agents Chemother, 2015, Dec; 59(12): 7666-7670 PMID: 26416870
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17 alpha-propionate

Catalog No. A10009
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Androgen 拮抗剂

17 alpha-propionate是一种新型的局部和外周选择性雄激素拮抗剂。了解更多

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PD 123319 ditrifluoroacetate

Catalog No. A13201
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angiotensin AT2 receptor 拮抗剂

PD 123319 ditrifluoroacetate是一种有效的，选择性的非肽血管紧张素AT2受体拮抗剂。大鼠肾上腺组织和大脑的IC50值分别为34和210 nM。了解更多

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- 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
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Netupitant

Catalog No. A14428
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NK1 receptor 拮抗剂

Netupitant是一种选择性的神经激肽1（NK1）受体拮抗剂。它竞争性地结合并阻断中枢神经系统（CNS）中人类物质P/NK1受体的活性，从而抑制内源性速激肽神经肽物质P（SP）的NK1受体结合，这可能导致预防化疗引起的恶心和呕吐（CINV）。了解更多

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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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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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Telmisartan

Catalog No. A10905
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AT1 拮抗剂

Telmisartan是一种抑制血管紧张素II AT1受体的血管紧张素II受体拮抗剂。了解更多

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Umeclidinium bromide

Catalog No. A15268
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Muscarinic receptor 拮抗剂

Umeclidinium bromide (GSK573719A)是毒蕈碱受体拮抗剂，可用于治疗慢性阻塞性肺疾病（COPD）。了解更多

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RS-127445

Catalog No. A11165
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5-HT2B receptor 拮抗剂

RS-127445是5-羟色胺5-HT2B受体的有效和选择性拮抗剂，相对于密切相关的5-HT2A和5-HT2C受体具有约1000倍的选择性。了解更多

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- Takeshi Takayanagi, .et al. Serotonin 5-HT2B receptor antagonism is fundamental for protecting PC12 cells exposed to hydrogen peroxide, Fujita Medical Journal, 2015, 1(1), 1-5, 2015
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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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N-Desmethylclozapine

Catalog No. A13762
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5-HT2C serotonin receptor 拮抗剂

N-Desmethylclozapine是一种有效的选择性5-HT2C血清素受体拮抗剂。了解更多

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Macitentan

Catalog No. A11492
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Endothelin receptor 拮抗剂

Macitentan是一种口服活性非肽双重ETA/ETB(内皮素) receptor双重拮抗剂，IC50为0.5 nM/391 nM。用于治疗特发性肺纤维化(IPF)和肺动脉高压(PAH)。了解更多

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Eprosartan

Catalog No. A11121
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AT1 receptor 拮抗剂

Eprosartan是一种用于治疗高血压的血管紧张素II受体拮抗剂。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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AM251

Catalog No. A12914
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CB1 receptor 拮抗剂

AM251是有效的CB1受体拮抗剂（IC50 = 8 nM，Ki = 7.49 nM），其选择性是CB2受体的306倍。了解更多

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- Potential for pharmacological manipulation of human embryonic stem cells. Br J Pharmacol. 2013 May; 169(2): 269–289.
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MK-571

Catalog No. A12529
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CysLT1 receptor 拮抗剂

MK-571是有效的CysLT1（LTD4）白三烯受体反向激动剂，EC50值为1.3 nM。了解更多

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- Jung-Hung Chen, .et al. Transplacental transfer of acetaminophen in pregnant rats, Biomed Pharmacother, 2022, Oct;154:113613 PMID: 36058146
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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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Tolvaptan

Catalog No. A11594
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vasopressin receptor 2 拮抗剂

Tolvaptan是一种选择性的竞争性精氨酸加压素受体2拮抗剂，IC50为1.28μM。了解更多

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Tasosartan

Catalog No. A10891
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Angiotensin II receptor 拮抗剂

Tasosartan是一种血管紧张素II受体拮抗剂。了解更多

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Flavoxate

Catalog No. A12900
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muscarinic AChR antagonist

Flavoxate结合并抑制毒蕈碱受体，从而通过改变脑干的排尿中心来抑制排尿反射并增加膀胱容量。了解更多

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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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Plerixafor 8HCl (DB06809)

Catalog No. A10913
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CXCR4 拮抗剂

Plerixafor 8HCl (DB06809)是CXCR4趋化因子受体拮抗剂，作用于CXCR4和CXCL12介导调节的趋化性， IC50分别为44 nM和5.7 nM。了解更多

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- Mei Zheng, .et al. CXCL12 inhibits hair growth through CXCR4, Biomed Pharmacother, 2022, Jun;150:112996 PMID: 35462338
- Asiedu KO, .et al. Bone marrow cell homing to sites of acute tibial fracture: 89Zr-oxine cell labeling with positron emission tomographic imaging in a mouse model, EJNMMI Res, 2018, Dec 13;8(1):109 PMID: 30547233
- Kingsley O. Asiedu, .et al. Bone marrow cell trafficking analyzed by 89Zr-oxine positron emission tomography in a murine transplantation model, Clin Cancer Res, 2017, Jun 1; 23(11): 2759-2768 PMID: 27965305
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SB 334867

Catalog No. A12786
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OX1 receptor 拮抗剂

SB 334867是一种选择性的非肽orexin OX1受体拮抗剂。对于分别表达人OX1和OX2受体的CHO细胞中的细胞内Ca2 +释放抑制，pKb值为7.2和<5。体内全身给药后，阻断orexin-A诱导的美容和进食。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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