Catalog No.
Product Name
Application
Product Information
Citations
- YIL 781 is a ghrelin receptor antagonist (GHS-R1a) (Ki = 17 nM)
- Lin D, .et al. , Endocrinology. , 2014, 155(7):2355-62 PMID: 24735326
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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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GLP-1 receptor agonist
Dulaglutide is a glucagon-like peptide-1 (GLP-1) receptor agonist.- Liuqing Xi, .et al. , Peptides, 2025, Mar:185:171366 PMID: 39954860
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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
- Clozapine displays a broad range of pharmacological actions; the antipsychotic effects are thought to be mediated principally by 5-HT2A/2C and dopamine receptor blockade.
- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
- Madeleine S A Tan, .et al. , Mol Pharm, 2022, Sep 23 PMID: 36149013
- Madeleine S. A. Tan, .et al. , Gels, 2022, Jan; 8(1): 38 PMID: 35049572
- Milan D Valyear, .et al. , Nat Commun, 2020, Jul 28;11(1):3764 PMID: 32724058
- Yutaro Kobayashi, .et al. , Transl Psychiatry, 2019, 9:181 PMID: 31371697
- M.D. Valyear, .et al. , bioRxiv, 2018, 2018
- Anamorelin is currently under development for the management of non-small lung cancer associated cachexia/anorexia.
- Makito Miyake, .et al. , Cancers (Basel), 2020, Jul 17;12(7):E1942 PMID: 32709007
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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
- Rimonabant is a selective antagonist of CB1 with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane.
- Marie-Eve Di Raddo, .et al. , Curr Res Neurobiol, 2023, Sep 4:5:100107 PMID: 38020805
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dopamine receptor agonist
Nalmefene hydrochloride is an opioid receptor antagonist.- Mark G Papich, .et al. , Drug Deliv Transl Res, 2022, Feb;12(2):376-383 PMID: 34817831
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SMO agonist
SAG is a chlorobenzothiophene-containing compound which acts as a SMO agonist (EC50 = 3 nM) but inhibits hedgehog signaling at high concentrations (>1 uM).- Mark van den Hurk, .et al. , NPJ Parkinsons Dis, 2022, Oct 18;8(1):134 PMID: 36258029
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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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Dopamine Receptor agonist
Rotigotine hydrochloride is a dopamine D2 and D3 receptor agonist. Ki values are 13 and 0.71 nM for D2 and D3 respectively.- Mattia Ferraiolo, .et al. , Neuropharmacology, 2022, 207: 108942 PMID: 35026287
- Mattia Ferraiolo, .et al. , Eur J Pharmacol, 2021, Nov 15;911:174557 PMID: 34626593
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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
- Prostaglandin F2α is a naturally occurring prostaglandin used in medicine to induce labor and as an abortifacient.
- Michel R Corboz, .et al. , Prostaglandins Other Lipid Mediat, 2020, Oct 1;152:106486 PMID: 33011365
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CB2 inverse agonist
SR 144528 is a selective peripheral cannabinoid receptor inverse agonist that displays a Ki value of 0.6 nM for rat spleen and human recombinant CB2 receptors and a Ki value of 400 nM for rat brain and human recombinant CB1 receptors.- Ming Tang, .et al. , Cell Death Dis, 2018, Jun; 9(6): 601 PMID: 29789558
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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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CXCL8/CXCR1/2 Inhibitor
Reparixin is a potent inhibitor of both CXCL8 receptors CXCR1/2, it inhibits weakly CXCR2-mediated cell migration (IC50=100 nM), whereas it strongly blocks CXCR1-mediated chemotaxis (IC50=1 nM).- Naour AL, .et al. , J Mol Cell Biol, 2019, Sep 3 PMID: 31504643
- Wigenstam E, .et al. , Toxicology, 2015, Feb 3;328:40-7 PMID: 25497111
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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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5-HT Receptor agonist
Prucalopride is a selective, high affinity 5-HT4 receptor agonist which targets the impaired motility associated with chronic constipation, thus normalising bowel movements.- Pierre Meschin, .et al. , Cell Calcium, 2015, Dec;58(6):549-57 PMID: 26427584
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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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Adenosine A2A Receptor Agonist
CGS 21680 is a specific adenosine A2A subtype receptor agonist.- Qian Wang, .et al. , Neuropharmacology, 2019, 148: 229-243 PMID: 30659840
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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
- Prazosin HCl is an α1 and α2B-adrenoceptor antagonist. Also a potent antagonist at the melatonin MT3 receptor (Ki = 10.2 nM).
- 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
- Risperidone(Risperdal) is an atypical antipsychotic used to treat schizophrenia (including adolescent schizophrenia), schizoaffective disorder, the mixed and manic states associated with bipolar disorder, and irritability in children with autism.
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Jaime Osuna-Luque, .et al. , J Exp Neurosci, 2018, 12: 1179069518798628 PMID: 30245571
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Serotonin reuptake inhibitor
Escitalopram oxalate ((S)-(+)Citalopram oxalate) is a selective serotonin reuptake inhibitor (SSRI) with Ki of 0.89 nM.- Reilly Taylor, .et al. , Front. Biosci. (Elite Ed), 2026, 18(1): 44075 PMID: 41914162
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5HT(1A) receptor agonist
Buspirone is a serotonergic (5HT(1A) receptor agonist) anxiolytic drug with some D(2) dopaminergic effect, used for anxiety disorders.- Reilly Taylor, .et al. , Front. Biosci. (Elite Ed), 2026, 18(1): 44075 PMID: 41914162
- Duloxetine is a serotonin-norepinephrine reuptake inhibitor (SNRI). It is effective for major depressive disorder and generalized anxiety disorder (GAD).
- Reilly Taylor, .et al. , Front. Biosci. (Elite Ed), 2026, 18(1): 44075 PMID: 41914162
- Rikun Cui, .et al. , Anal Chim Acta, 2024, Aug 22:1318:342960 PMID: 39067929
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MOR agonist
SR17018 is an mu-opioid-receptor (MOR) agonist with an EC50 of 97 nM.- Rob Hill, .et al. , Br J Pharmacol, 2023, Jul 24 PMID: 37489013
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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 A3-R agonist
IB-MECA has been shown to act as a potent and selective Adenosine A3-R agonist with Ki values of 1.1, 54 and 56 nM for Adenosine A3-R, Adenosine A1-R and Adenosine A2A-R, respectively.- Sameshima T, .et al. , Chem Res Toxicol, 2019, Aug 28 PMID: 31461269
- BP 897, is an antagonist at human dopamine D3 receptors and at rat somatodendritic dopamine D3 receptors
- Shaowen Qian, .et al. , Nat Commun, 2022, Jul 22;13(1):4229 PMID: 35869064
- Shaowen Qian, .et al. , Nature Portfolio Journal, 2021, Oct 1
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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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S1P inhibitor
PF429242 dihydrochloride is a reversible and competitive S1P inhibitor with an IC50 of 175 nM.- Shiying Xie, .et al. , FEBS J, 2024, Apr;291(7):1575-1592 PMID: 38243371
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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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GluR inhibitor
(-)-Huperzine A is a naturally occurring sesquiterpene alkaloid compound found in the firmoss Huperzia serrata.- Takuya Ohba, .et al. , PharmaNutrition, 2020, 13:100203
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Guanylate cyclase C agonist
Linaclotide is a peptide agonist of the guanylate cyclase 2C.- Tessa A Groeneweg, .et al. , Ann N Y Acad Sci, 2026, Feb;1556(1):e70152 PMID: 41400434
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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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GLP-1 agonist
Albiglutide is a glucagon-like peptide-1 agonist (GLP-1 agonist).- Tito Borner, .et al. , Cell Rep, 2020, Jun 16;31(11):107768 PMID: 32553160
