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Catalog No.
Product Name
Application
Product Information
Citations
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PAR-1 Antagonist
Vorapaxar (SCH 530348) is a potent and orally active thrombin receptor (PAR-1) antagonist with Ki of 8.1 nM.- Arundhasa Chandrabalan, .et al. , Am J Physiol Cell Physiol, 2023, Jul 1;325(1):C272-C285 PMID: 37273236
- Arundhasa Chandrabalan, .et al. , Sci Rep, 2023, Jan 20;13(1):1124 PMID: 36670151
- Cansu Tekin, .et al. , Cell Oncol (Dordr), 2020, Aug 18 PMID: 32809114
- Cansu Tekin, .et al. , Oncotarget, 2018, Aug 10; 9(62): 32010-32023 PMID: 30174793
- Claushuis TA, .et al. , J Thromb Haemost, 2017, Apr;15(4):744-757 PMID: 28092405
- Maaike Waasdorp, .et al. , Biochem Biophys Rep, 2017, Jul; 10: 152-156 PMID: 29114573
- Joseph C. Mudd, .et al. , J Infect Dis, 2016, Dec 15; 214(12): 1808-1816 PMID: 27703039
- Corey E. Tabit, .et al. , Circulation, 2016, Jul 12; 134(2): 141-152 PMID: 27354285
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NK1 receptor antagonist
Rolapitant, also known as SCH-619734, is a selective, bioavailable, CNS penetrant neurokinin NK1 receptor antagonist that shows behavioral effects in animals models of emesis.- Bubak AN, .et al. , J Infect Dis, 2018, Sep 8;218(8):1324-1335 PMID: 29788447
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Smo Antagonist
LDE225 (NVP-LDE225) is a potent, selective and orally bioavailable Smoothened (SMO) antagonist that inhibits hedgehog (Hh) signaling pathway via antagonism of the Smoothened receptor (SMO).- Daniel Doheny, .et al. , Oncogene, 2020, Oct;39(42):6589-6605 PMID: 32929154
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angiotensin AT2 receptor antagonist
PD 123319 ditrifluoroacetate is a potent, selective, non-peptide angiotensin AT2 receptor antagonist. IC50 values are 34 and 210 nM in rat adrenal tissue and brain respectively.- Dao-Lai Zhang, .et al. , eLife, 2018, 7: e33432 PMID: 29393851
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CXCR4 antagonist
Plerixafor is an immunostimulant used to multiply hematopoietic stem cells and it is a chemokine receptor-4 antagonist for mobilization of hematopoietic stem cells for transplantation.- Federico Antoniciello, .et al. , Front Mol Biosci, 2023, May 11;9:887564 PMID: 35647033
- Mei Zheng, .et al. , Biomed Pharmacother, 2022, Jun;150:112996 PMID: 35462338
- Asiedu KO, .et al. , EJNMMI Res, 2018, Dec 13;8(1):109 PMID: 30547233
- Kingsley O. Asiedu, .et al. , Clin Cancer Res, 2017, Jun 1; 23(11): 2759-2768 PMID: 27965305
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CXCR4 antagonist
Plerixafor is an immunostimulant used to multiply hematopoietic stem cells and it is a chemokine receptor-4 antagonist for mobilization of hematopoietic stem cells for transplantation.- Helen C Wang, .et al. , Cell Rep, 2024, Aug 27;43(8):114542 PMID: 39046877
- Hitoshi Maeda, .et al. , Int J Biol Macromol, 2022, Sep 17;221:1439-1452 PMID: 36126807
- Jingying Chen, .et al. , Development, 2022, Jul 1;149(13) PMID: 35694896
- Narubhorn Ongprakobkul, .et al. , Am J Orthod Dentofacial Orthop, 2022, Mar 2;S0889-5406(22)00107-X PMID: 35248418
- Chunliang Liu, .et al. , J Trace Elem Med Biol, 2022, Jan 10;71:126927 PMID: 35030482
- Eri Watanabe, .et al. , Angiogenesis, 2020, Jul 22 PMID: 32699964
- Alessandra Esposito, .et al. , Bone, 2020, Jul 3;139:115521 PMID: 32629173
- Kentaro Suzuki, .et al. , Sci Rep, 2019, 9: 15284
- Ichimizu S, .et al. , J Control Release, 2019, May 10;304:156-163 PMID: 31082432
- Nan Li, .et al. , Diagn Pathol, 2019, Jan 12;14(1):3 PMID: 30636642
- Thida W, .et al. , Biochem Biophys Res Commun, 2018, Nov 20. pii: S0006-291X(18)32477-X PMID: 30470571
- Henry R. Hampton, .et al. , Nat Commun, 2015, 6: 7139 PMID: 25972253
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5-HT2A receptor antagonist
Volinanserin is a highly selective 5-HT2A receptor antagonist.- Hugo R Arias, .et al. , Eur J Pharmacol, 2024, Mar 5:966:176329 PMID: 38253116
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somatostatin receptor antagonist
Octreotide is a peptide agonist for sst2, sst3 and sst5 somatostatin receptors. IC50/Kd values (nM) at cloned human somatostatin receptors are: 290 - 1140 (sst1), 0.4 - 2.1 (sst2), 4.4 - 34.5 (sst3), > 1000 (sst4), and 5.6 - 32 (sst5).- Ida Vang Andersen, .et al. , Nucl Med Biol, 2024, May-Jun:132-133:108905 PMID: 38555651
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OX1 receptor antagonist
SB 334867 is a selective non-peptide orexin OX1 receptor antagonist. pKb values are 7.2 and < 5 for inhibition of intracellular Ca2+ release in CHO cells expressing human OX1 and OX2 receptors respectively. Blocks orexin-A induced grooming and feeding following systemic administration in vivo.- Ines M Amaral, .et al. , Psychopharmacology (Berl), 2024, Sep 20 PMID: 39302438
- Tony Ngo, .et al. , Nat Chem Biol, 2017, Feb; 13(2): 235-242 PMID: 27992882
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Histamine H2-receptor antagonist
Ranitidine is a potent, selective and orally active histamine H2-receptor antagonist with an IC50 of 3.3 μM that inhibits gastric secretion.- Jingyeong Shin, .et al. , Chemical Engineering Journal, 2023, December
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H2-receptor antagonist
Cimetidine is a histamine H2-receptor antagonist that inhibits stomach acid production.- Jingyeong Shin, .et al. , Chemical Engineering Journal, 2023, December
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α2C antagonist
JP 1302 2HCl is a potent and selective α2C antagonist.- Junya Maruoka, .et al. , Int J Neuropsychopharmacol, 2026, Apr 6;29(4):pyag007 PMID: 41717785
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Histamine Antagonist
JNJ7777120 is a potent, selective non-imidazole H4?histamine receptor antagonist.- K Yamamoto, .et al. , Naunyn-Schmiedeberg's Arch Pharmacol, 2019, pp 1-12 PMID: 30919010
- Yamamoto K, .et al. , Neurosci Lett, 2018, May 29;676:103-107 PMID: 29655943
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CysLT1 receptor antagonist
MK-571 is a potent CysLT1 (LTD4) leukotriene receptor inverse agonist with EC50 value of 1.3 nM.- Kaito Yamashiro, .et al. , J Toxicol Sci, 2026, 51(2):141-147 PMID: 41621859
- Jung-Hung Chen, .et al. , Biomed Pharmacother, 2022, Oct;154:113613 PMID: 36058146
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5-HT1C receptor antagonist
Clozapine N-oxide is a major metabolite of Clozapine noted to decrease SR-2A (5-HT2 serotonin receptor) density in vitro.- Kazuhei Niitani, .et al. , J Pharmacol Sci, 2025, Sep;159(1):1-7 PMID: 40713343
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H1 antagonist
Asenapine shows high affinity (pKi) for numerous receptors, including the serotonin 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), and 5-HT7 (9.9) receptors, the adrenergic α1 (8.9), α2A (8.9), α2B (9.5), and α2C (8.9) receptors, the dopamine D1 (8.9), D2 (8.9), D3 (9.4), and D4 (9.0) receptors, and the histamine H1 (9.0) and H2 (8.2) receptors.- Keisuke Obara, .et al. , Biol Pharm Bull, 2021, 44, 1140-1150 PMID: 34334499
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CXCR4 antagonist
AMD 3465 is a potent, selective CXCR4 antagonist.- Kentaro Suzuki, .et al. , Sci Rep, 2019, 9: 15284
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orexin receptor antagonist
Nemorexant (ACT-541468) is a potent orexin receptor antagonist extracted from patent WO2015083094A1, compound example 7, has IC50s of 2 nM and 3 nM for Ox1 receptor and Ox2 receptor, respectively.- Koichi Aoyama, .et al. , Forensic Toxicol, 2026, Jan;44(1):130-140 PMID: 41396382
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Opioid Receptor antagonist
JTC-801 is a selective antagonist for the nociceptin receptor, also known as the ORL-1 receptor.- Lihao Gu, .et al. , Cosmetics, 2017, 4(4), 48
- Toshio Yawata, .et al. , Mol Cell Biochem, 2016, Jan;411(1-2):201-11 PMID: 26427671
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bradykinin B1 receptor antagonist
SSR240612 is a new antagonist of the bradykinin B1 receptor.- Ling Qin, .et al. , Arthritis Res Ther, 2019, 21:12 PMID: 30621761
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Orexin receptor antagonist
MK6096, also known as filorexant, is an orally bioavailable potent and selective reversible antagonist of OX(1)R and OX(2)R currently in clinical development for insomnia. MK-6096 demonstrated potent binding and antagonism of both human OX(1)R and OX(2)R (<3 nM in binding, 11 nM in FLIPR), with no significant off-target activities against a panel of >170 receptors and enzymes.- Mahtab Moshirpour, .et al. , Neuroscience, 2025, May 14:574:114-123 PMID: 40194656
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somatostatin receptor 2 antagonist
CYN-154806 is a potent selective somatostatin receptor 2 (sst2) antagonist.- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
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LPA1 receptor antagonist
AM966 is a high affinity, selective, oral antagonist of LPA1 receptor (lysophosphatidic acid receptor) with an IC50 value of 17 nM.- Maria F Fernandes, .et al. , Int J Mol Sci, 2022, Apr 9;23(8):4163 PMID: 35456981
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LPA Receptor Antagonist
Ki16425 is a LPA receptor antagonist with selectivity for LPA1 and LPA3 and exhibits Ki values of 0.34, 6.5, and 0.93 μM for the human LPA1, LPA2, and LPA3 receptors, respectively.- Maria F Fernandes, .et al. , Int J Mol Sci, 2022, Apr 9;23(8):4163 PMID: 35456981
- Rieko Suenaga, .et al. , PLoS One, 2022, Feb 3;17(2):e0263296 PMID: 35113924
- Inoue A, .et al. , Cell, 2019, Jun 13;177(7):1933-1947 PMID: 31160049
- Taniguchi R, .et al. , Nature, 2017, Aug 17;548(7667):356-360 PMID: 28792932
- T. HASHIMOTO, .et al. , Br J Dermatol., 2015, Nov;173(5):1334-6 PMID: 26122943
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CGRP Receptor antagonist
MK 3207 hydrochloride is a potent CGRP receptor antagonist with IC50 of 0.12 nM.- Marlene Dallmayer, .et al. , Cell Death Dis, 2019, Feb 11;10(2):116 PMID: 30741933
- Marlene Dallmayer, .et al. , bioRxiv, 2018, 2018
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neurokinin-1 receptor antagonist
Aprepitant is classified as an NK1 antagonist. Aprepitant has been shown to inhibit both the acute and delayed emesis induced by cytotoxic chemotherapeutic drugs by blocking substance P landing on receptors in the brains neurons. It has also been shown to increase the activity of the 5-HT3 receptor antagonists ondansetron and the corticosteroid dexamethasone, which are also used to prevent nausea and vomiting caused by chemotherapy.
- Maya Tokumoto, .et al. , Connect Tissue Res, 2022, Jul 20;1-11 PMID: 35856812
- Kodji X, .et al. , FASEB J, 2018, Sep 11:fj201800395RR PMID: 30204499
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β2 adrenergic receptor antagonist
ICI-118551 is a selective beta2 adrenergic receptor (adrenoreceptor) antagonist.- Moon Jain, .et al. , Tropical Journal of Pharmaceutical Research, 2020, Vol. 19 No. 4
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EndothelinA receptor antagonist
Ambrisentan functions as an endothelin receptor antagonist, and is selective for the type A endothelin receptor (ETA).- Naoki Dohi, .et al. , PLoS One, 2021, 16(8): e0255656 PMID: 34343209
- Tony Ngo, .et al. , Nat Chem Biol, 2017, Feb; 13(2): 235-242 PMID: 27992882
- Toshiaki Okamoto, .et al. , World J Hepatol, 2016, Aug 8; 8(22): 933-941 PMID: 27574547
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RAAS antagonist
Candesartan is an angiotensin receptor blocker (also called an angiotensin-II receptor antagonist or an AIIRA).- Naomi Fukazawa, .et al. , Pharm Res, 2024, May;41(5):849-861 PMID: 38485855
- Hideki Kobara, .et al. , Molecular Medicine Reports, 2020, 22(2) PMID: 32626983
- Dao-Lai Zhang, .et al. , eLife, 2018, 7: e33432 PMID: 29393851
- Toshihide Kashihara, .et al. , J Physiol, 2017, Jul 1; 595(13): 4207-4225 PMID: 28295363
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5-HT2C serotonin receptor antagonist
N-Desmethylclozapine is a potent and selective 5-HT2C serotonin receptor antagonist- Orwa Albitar, .et al. , Separation Science Plus, 2022, March 27
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A2A antagonist
Istradefylline (KW-6002) is a selective antagonist at the A2A receptor. It has been found to be useful in the treatment of Parkinson's disease.- PU Hamor, .et al. , Prog Neuropsychopharmacol Biol Psychiatry, 2020, Dec 20;103:109979 PMID: 32470496
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5HT1A antagonist
WAY-100635 was originally believed to act as a selective 5-HT1A receptor antagonist, but subsequent research showed that it also acts as potent full agonist at the D4 receptor.
- Qi Liu, .et al. , Environ Sci Technol, 2024, Apr 30;58(17):7577-7587 PMID: 38630542
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H1-receptor antagonist
Astemizole is a potent antihistamine (H1-receptor antagonist, IC50 = 4 nM) that displays selectivity over dopamine, 5-HT, and muscarinic acetylcholine receptors. This compound has shown potent hERG K+ channel blocking activity (IC50 = 0.9 nM), antimalarial activity in multidrug resistant strains in vitro (IC50 = 227 - 734 nM), and has been used as a chaperone to correct folding defects and restore protein function for some mutated forms of hERG channels.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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alpha1/beta adrenergic receptors antagonist
Labetalol HCl is a dual antagonist for both selective alpha1-adrenergic and nonselective beta-adrenergic receptors.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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dopamine D2 receptor antagonist
Metoclopramide HCl is a selective dopamine D2 receptor antagonist.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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Histamine Receptor antagonist
Bepotastine Beslilate (Bepreve) is a histamine H1 receptor anatagonist.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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Dopamine Receptor antagonist
Paliperidone(Invega) is an atypical antipsychotic.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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CXCR1/CXCR2 antagonist
SCH527123 is a potent and selective antagonist of the human CXCR1 and CXCR2 receptors with IC50 of 42 nM and 3 nM, respectively.- Ruijie Zhang, .et al. , Int J Oncol, 2022, May;60(5):50 PMID: 35315502
- Fu S, .et al. , Int J Oncol, 2018, Jul;53(1):349-357 PMID: 29749433
- Fu S, .et al. , Anticancer Res, 2018, Nov;38(11):6271-6279 PMID: 30396947
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OX1/OX2 Antagonist
Almorexant HCl is an orally active, dual orexin receptor antagonist with IC50 of 6.6 nM and 3.4 nM for OX1 and OX2 receptor 3.- Ryan J Keenan, .et al. , Br J Pharmacol, 2022, Jul;179(13):3403-3417 PMID: 35112344
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Adenosine A2A antagonist
ZM-241385 is a potent and highly selective Adenosine A2A-R antagonist, with a pA2 of 9.02 for Adenosine A2A-R in cardiac vasculature and selectivities of 1000, 91 and 500,000 over Adenosine A1-R, Adenosine A2B-R and Adenosine A3-R sites, respectively.- Sheng-Tao Hou, .et al. , Research Square, 2023, Sep 28
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5-HT2C receptor antagonist
Puerarin is one of several known isoflavones. Puerarin is a 5-HT2C receptor and benzodiazepine site antagonist. Puerarin is being investigated as a self-microemulsifying drug delivery system.- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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S1P Receptor antagonist
FTY720 is a derivative of ISP-1 (myriocin), a fungal metabolite of the Chinese herb Iscaria sinclarii as well as a structural analog of sphingosine.- Tina Sepasi, .et al. , Int J Pharm, 2023, Apr 5;636:122815 PMID: 36907279
- Tina Sepasi, .et al. , BioImpacts, 2022, 28 May PMID: 37193076
- Zengzi Zhou, .et al. , Infect Immun, 2020, Oct 19;88(11):e00281-20 PMID: 32868341
- Mayu Idehara, .et al. , Traditional & Kampo Medicine, 2020, 22 July
- Luwa Yuan, .et al. , Sci Rep, 2019, 9:11156 PMID: 31371790
- Sakai Y, .et al. , Int J Biol Macromol, 2018, Nov 22;124:505-514 PMID: 30471397
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ETA-receptor Antagonist
Zibotentan (ZD4054)is an orally administered, potent and specific ETA-receptor (endothelin A receptor) antagonist (IC50 = 21 nM).- Tony Ngo, .et al. , Nat Chem Biol, 2017, Feb; 13(2): 235-242 PMID: 27992882
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Dual orexin receptor antagonist
TCS 1102 is a potent, dual orexin receptor antagonist (Ki values are 0.2 and 3 nM for OX2 and OX1 receptors respectively).- Tung-Yen Lee, .et al. , Front Psychiatry, 2023, Jun 29;14:1196994 PMID: 37457782
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CXCR4 antagonist
AMD 070 is a CXCR4 chemokine receptor antagonist.- Uchida D, .et al. , Oncol Rep, 2018, Jul;40(1):303-308 PMID: 29749473
- Mamoru Morimoto, .et al. , BMC Cancer, 2016, 16: 305 PMID: 27175473
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CB2 antagonist
AM630 is a selectivity CB2 antagonist with Ki of 31.2 nM, > 150 fold selectivity over CB1 receptor.- Vida Mirzaie, .et al. , Iran J Basic Med Sci, 2025, 28(9):1171-1179 PMID: 40809175
- Md Shah Sufian, .et al. , J Exp Biol, 2021, 21 JUNE PMID: 34435626
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CB1 receptor antagonist
AM251 is a potent CB1 receptor antagonist (IC50 = 8 nM, Ki = 7.49 nM) that displays 306-fold selectivity over CB2 receptors.- Vida Mirzaie, .et al. , Iran J Basic Med Sci, 2025, 28(9):1171-1179 PMID: 40809175
- Vida mirzaie, .et al. , Research Square, 2024, October
