Catalog No.
Product Name
Application
Product Information
Citations
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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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Smoothened inhibitor
BMS-833923 (or XL-139) is an orally bioavailable small-molecule SMO (Smoothened) inhibitor with potential antineoplastic activity.- Valérian Pasche, .et al. , Parasit Vectors, 2018, 11: 298 PMID: 29764454
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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
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CB receptor agonist
WIN 55,212-2 is a potent cannabinoid receptor agonist that has been found to be a potent analgesic in a rat model of neuropathic pain. It activates p42 and p44 MAP kinase via receptor-mediated signaling.- Vida Mirzaie, .et al. , Iran J Basic Med Sci, 2025, 28(9):1171-1179 PMID: 40809175
- Vida mirzaie, .et al. , Research Square, 2024, October
- Greish K, .et al. , J Control Release, 2018, Dec 10;291:184-195 PMID: 30367922
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CXCR2/CXCR1 antagonist
SCH 563705 is a potent dual CXCR2(IC50= 1.3 nM)/CXCR1(IC50= 7.3 nM) antagonist.- Yael Derdikman Ofir, .et al. , Mol Ther Oncol, 2026, Jul 1;34(3):201288 PMID: 42519390
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GPR agonist
TAK-875 is a potent, selective, and orally bioavailable GPR40 agonist.- Ying Liu, .et al. , Nucleic Acids Res, 2018, Oct 12; 46(18): 9864-9874 PMID: 30219861
- Deborah A. Goldspink, .et al. , Mol Metab, 2018, Jan; 7: 90-101 PMID: 29167062
- Hodaka Yamada, .et al. , Sci Rep, 2016, 6: 25912 PMID: 27180622
- Glucagon-Like Peptide 1 (7-36) Amide is a potent glucose-dependent insulinotropic peptide produced by post-translational processing of proglucagon in intestinal L-cells.
- Ying Zhou, .et al. , Adv Biol (Weinh), 2022, Nov 14 PMID: 36373695
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D2 dopamine receptor antagonist
L-741626 is a potent and selective antagonist for the dopamine receptor D2. It has good selectivity over the related D3 and D4 subtypes and other receptors.- Yoon-Jin Kim, .et al. , Sci Adv, 2021, Feb 19;7(8) PMID: 33608268
- Clenbuterol Hydrochloride is a sympathomimetic β2-adrenoceptor agonist that has been used as a bronchodilator in the treatment of pulmonary diseases such as asthma. At higher doses, clenbuterol acts as an anabolic steroid, favoring skeletal muscle protein synthesis at the expense of fat deposition.
- Younian Xu, .et al. , J Inflamm Res, 2022, Jan 14;15:295-309 PMID: 35058704
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EPAC2 antagonist
ESI-05 (NSC 116966) is a specific antagonist of EPAC2 (exchange protein directly activated by cAMP 2), with an IC50 of 0.4 ?M. ESI-05 (NSC 116966) inhibits cAMP-mediated activation of EPAC2 as well as EAPC2 mediated Rap1 activation.- Yuri A Blednov, .et al. , Neuropharmacology, 2024, Jun 13:257:110035 PMID: 38876310
- Tirzepatide (LY3298176, GIP/GLP-1 RA, TZP) is a dual GIP/GLP-1 receptor agonist. Tirzepatide differentially induces internalization of the GIP and GLP-1 receptors with EC50 values of 18.2 nM and 18.1 nM, respectively.
- Zhenhuan Zheng, .et al. , Mol Metab, 2026, Mar 14;106:102340 PMID: 41833222
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GPR4 antagonist
GPR4 antagonist 1 is a GPR4 antagonist, with an IC50 of 189 nM. -
Dopamine receptor antagonist
cis-(Z)-Flupentixol dihydrochloride is a dopamine receptor antagonist, antipsychotic, neuroleptic agent. - Desmopressin is a synthetic vasopressin analog that acts as an agonist at V1B and V2 receptors (EC50 values are 11.4 and 23.9 nM and Ki values are 5.84 and 65.9 nM respectively).
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PAFR inhibitor/H1 receptor inhibitor
Rupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 and 102 nM, respectively. -
antagonist of melanin concentrating hormone receptor 1
MCHr1 antagonist 2 is an antagonist of melanin concentrating hormone receptor 1, with an IC50 of 65 nM; MCHr1 antagonist 2 also inhibits hERG, with an IC50 of 4.0 nM in IMR-32 cells. -
sGC activator
YC-1 is a direct activator of soluble Guanylyl Cyclase (sGC), independent of Nitric Oxide. -
mGluR5 positive allosteric modulator
BMT-145027 is an mGluR5 positive allosteric modulator without inherent agonist activity, exhibits an EC50 of 47 nM. -
GPR35/CXCR8 agonist
GPR35 agonist 1 (compound 50) is a potent and specific G protein-coupled receptor-35 (GPR35)/CXCR8 agonist with an EC50 of 5.8 nM, displays good druggability. -
mGlu4 receptors modulator
VU 0361737 is a selective positive allosteric modulator at mGluR-4 (EC50 values are 240 and 110 nM at human and rat receptors respectively). -
Sigma-2 receptor agonist
Siramesine Hydrochloride is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo. -
OX Antagonist
Almorexant(ACT078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively. -
sigma-1 receptor antagonist
S1RA is a selective sigma-1 receptor antagonist, with a reported binding affinity of Ki = 17.0 ?? 7.0 nM, selective over the sigma-2 receptor and against a panel of other 170 receptors, enzymes, transporters and ion channels. -
5-HT6R antagonist
Lu AE58054 is a potent and selective 5-HT6 receptor antagonist. - Pramipexole dihydrochloride is a dopamine receptor agonist exhibiting selectivity for the D3 receptor.
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A2A adenosine agonist
Regadenoson was selective agonist for the A2A adenosine receptor versus the A1, A2B, and A3 receptors in binding and functional studies. Regadenoson was also found to be a full and potent agonist to cause coronary vasodilation, a response that has a very large A2A receptor reserve? -
adenosine A2A/A1 receptor antagonist
A2A receptor antagonist 1 (CPI-444 analog) is an antagonist of both adenosine A2A receptor and A1 receptor with Kis of 4 and 264 nM, respectively. -
CXCR4 Inhibitor
MSX-122 is an orally bioavailable inhibitor of CXCR4 (IC50 = ~10 nM) with potential antineoplastic and antiviral activities. CXCR4 inhibitor MSX-122 binds to the chemokine receptor CXCR4, preventing the binding of stromal derived factor-1 (SDF-1) to the CXCR4 receptor and receptor activation, which may result in decreased tumor cell proliferation and migration. -
5-HT Receptor modulator
Lu-AA21004 is an oral multimodal serotonergic agent, inhibits 5-HT(1A), 5-HT(1B), 5-HT(3A), 5-HT(7) and SERT with IC50 of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively. -
SphK2 inhibitor
ABC294640 is an orally available, aryladamantane compound and selective inhibitor of sphingosine kinase-2 (SK2) with potential antineoplastic activity. -
serotonin/dopamine/norepinephrine reuptake inhibitior
SPD-473 citrate is a serotonin/dopamine/norepinephrine reuptake inhibitior.
