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Inhibitors & Agonists

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Cat. No. Product Name Field of Application Chemical Structure
DC73480 (R)-YNT-3708 (R)-YNT-3708 is a potent, selective orexin 1 receptor (OX1R) agonist with EC50 of 7.48 nM and Emax 101%, 22-fold selectivity over OX2R (IC50=168 nM).
DC73481 CVN45502 CVN45502 (CVN 45502) is a potent, orally bioavailable, highly selective orexin 1 receptor (Hcrtr1, OX1R) antagonist with binding affinity (pKi) of 7.86 (human Hcrtr1), significantly reduces feeding and body weight in diet-induced obese (DIO).
DC73482 CVN766 Featured CVN766 (CVN 766) is a potent, exquisitely selective orexin 1 receptor (OX1R) antagonist with IC50 of 8 nM, 1000-fold selective over OX2R.
DC73483 OBPt-9 OBPt-9 is a potent, postivie allosteric potentiator of orexin receptor-mediated signaling, similarly potentiates the response of OXR1 and OXR2 to orexin A.
DC73484 MRS4833 MRS4833 is a potent, selective antagonist of Gi protein-coupled P2Y14 receptor (P2Y14R, GPR105) with IC50 of 5.9 nM, Ki of 3.44 nM (human P2Y14R).
DC73485 MRS4853 MRS4853 is a selective P2Y6 receptor (P2Y6R) antagonist with IC50 of 0.46 uM (hP2Y6R), displays weak affinity for mP2Y6R (IC50=6.15 uM).
DC73486 ACT-774312 ACT-774312 (ACT774312) is a potent and selective CRTH2 receptor antagonist with IC50 of 3 nM, 150-fold more potent than setipiprant in inhibiting PGD2-induced eosinophil cell shape change.
DC73487 AGN 225660 AGN 225660 is a second-generation prostanoid receptor antagonist acting at multiple receptor subtypes with IC50 of 220/70/2900/7100/70/180/1100/5 nM for DP1/EP1/EP2/EP3/EP4/FP/IP/TP receptors, respectively.
DC73488 AMX12006 AMX12006 (AMX-12006) is a potent, selective, orally active antagonist of prostaglandin E2 (PGE2) receptor 4 (EP4) with IC50 of 4.3 nM in cAMP assays, shows no activity against EP1, EP2, EP3 receptors.
DC73489 CR6086 sodium CR6086 sodium (CR-6086) is a potent, selective prostaglandin E2 receptor 4 (EP4) antagonist with Ki of 16.6 nM (hEP4 receptor), inhibits PGE2-stimulated cAMP production with IC50 of 22 nM.
DC73490 L001 L001 is a potent and selective EP4 antagonist with cAMP IC50 of 7.29 nM, impairs pancreatic cancer migration and invasion.
DC73491 LY3127760 LY3127760 is a potent, selective prostaglandin E4 (EP4) receptor antagonist with binding Ki of 58 nM (hEP4) and cAMP IC50 of 5.6 nM.
DC73492 ONO-4578 ONO-4578 (BMS-986310) is a potent, highly selective EP4 antagonist, potently inhibits the PGE2-induced cAMP production in CHO cells expressing mouse and human EP4 receptors with single-digit nM IC50.
DC73493 TG11-77 TG11-77 is a potent, selective, brain-permeable and orally available antagonist of the prostaglandin E2 (PGE2) receptor subtype EP2 with KB value of 9.7 nM.
DC73495 1-Piperidine Propionic Acid 1-Piperidine Propionic Acid (1-PPA) is an allosteric Inhibitor of protease activated receptor-2 (PAR2) with IC50 of 2.3 uM.
DC73496 NRD-21 NRD-21 is a potent, selective, reversible, negative allosteric modulator of PAR1 with IC50 of 0.37 uM in calcium mobilization assays.
DC73497 TFLLRN-NH2 TFLLRN-NH2 is a potent, PAR1-selective agonist peptide with EC50 of 1.9 uM.
DC73498 Ogremorphin Ogremorphin (OGM, OGM8345) is a highly specific, first-in-class small-molecule inhibitor of GPR68 with IC50 of 0.71 uM.
DC73499 Ogremorphin-1 Ogremorphin-1 (OGM1) is a highly specific, first-in-class small-molecule inhibitor of GPR68 with IC50 of 0.16 uM.
DC73500 DC591053 DC591053 (DC 591053) is a selective small molecule agonist of relaxin family peptide receptor 4 (RXFP4) with pEC50  of 7.24  and pKi  of  6.95, shows no activity against RXFP3.
DC73501 AZ-66 AZ-66 is a highly potent S1R/S2R antagonist with Ki of 0.31/1.76 nM, respectively.
DC73502 CM-304 CM-304 is a potent, selective sigma-1 receptor (S1R) antagonist with Ki of 3.41 nM, 100-fold selective over S2R.
DC73503 GM310 GM310 is a small molecule inhibitor of glycolysis, proteotoxicity, inflammation, and impairments in animal models of Alzheime's, Huntington's, and stroke by activation of the Sigma-1 receptor.
DC73504 JR1-157 Featured JR1-157 is a potent selective sigma 2 receptor (σ2R) ligand with Ki value of 47 nM, >10-fold selectivity over σ1R.
DC73505 MAM03055A MAM03055A is a novel bivalent sigma-2 receptor/TMEM97 ligand with cytotoxic activity, exhibits high affinity and strong preference for sigma-2 receptor with Ki of 55.9 nM.
DC73506 RC-752 RC-752 is a potent, seletive sigma-1 receptor (S1R) antagonist with Ki of 6.2 nM, 50-fold selective over S2R, shows antinociceptive activity.
DC73508 CRN02481 CRN02481 is a potent and selective SST5 receptor agonist with EC50 of 0.37 nM (human SST5), with excellent selectivity against SST1, SST2, SST3 and SST4 receptors.
DC73509 S6821 Featured S6821 (S 6821) is a potent and selective antagonist of the bitter taste receptor TAS2R8, exhibiting an IC50 value of 21 nM. It demonstrates high selectivity across a panel of 16 TAS2Rs, effectively reduces the bitterness of coffee, and shows an excellent safety profile.
DC73510 Org 274179-0 Featured Org 274179-0 is a highly potent, allosteric antagonist of the thyroid-stimulating hormone receptor (TSH receptor), inhibits bTSH-, hTSH- and M22-mediated CRE-luciferase transactivation in the CHO cell line.
DC73511 SYD5115 (SYD-5115, SYD 5115) SYD5115 (SYD-5115) is a potent, selective and orally bioavailable thyrotropin receptor (TSH-R) antagonist with IC50 of 48 and 62 nM for rTSHR and hTSHR, respectively.

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