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GPCR

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Cat. No. Product Name Field of Application Chemical Structure
DC72638 AL-3138 AL-3138 (11-Deoxy-16-fluoro PGF2α) is a prostaglandin F2 alpha (PGF2alpha) analogue that antagonises FP prostaglandin receptor-mediated inositol phosphate production.
DC72639 I-SAP I-SAP is a radioiodinated TXA2/PGH2 receptor antagonist. The bind between I-SAP and the receptors, is inhibited by the histidine modifying reagent diethyl-pyrocarbonate (DEPC).
DC72640 Fingolimod phosphate Fingolimod phosphate (FTY720 phosphate) is an orally active sphingosine 1-phosphate (S1P) receptor agonist. Fingolimod phosphate can promote the neuroprotective effects of microglia. Fingolimod phosphate can be used for the research of multiple sclerosis and neurologic diseases.
DC72641 ONO-0740556 ONO-0740556 is a potent Gi-coupled human lysophosphatidic acid receptor 1 (LPA1) agonist with an EC50 value of 0.26 nM.
DC72765 Evocalcet Featured Evocalcet (KHK7580) is an novel oral calcimimetic agent which acts via allosteric activation of the calcium sensing receptor (CaSR). Evocalcet (0, 20 and 60 nM) dose-dependently increases cytoplasmic [Ca2+] concentrations with an EC50 value of 92.7 nM in hCaR-HEK293 cells.
DC72766 PF-07054894 Featured PF-07054894 is a potent CCR6 antagonist. PF-07054894 targets G protein-coupled receptor (GPCR). PF-07054894 can be used in research of inflammatory bowel disease.
DC72808 UCM-1306 Featured UCM1306 is a potent and orally active human dopamine D1 receptor allosteric modulator (PAM). UCM-1306 increases the endogenous dopamine (DA) maximal effect both in human and mouse D1 receptors. UCM-1306 is not only for improving motor symptoms but also for addressing the key comorbid cognitive impairment associated with long-term Parkinson’s disease (PD).
DC72820 Macimorelin acetate Macimorelin (EP-1572) acetate, a GH secretagogue, is an orally active GHSR agonist. Macimorelin acetate stimulates GH release. Macimorelin acetate can be used in the research of adult growth hormone deficiency (AGHD), and Cancer anorexia-cachexia syndrome (CACS).
DC72833 Muscarine Featured Muscarine ((+)-Muscarine) is a toxin that can stimulate the parasympathetic nervous system. Muscarine is an agonist of muscarinic acetylcholine receptor (mAChR).
DC72851 FR 113680 FR 113680 is a tripeptide substance P antagonist that interacts selectively with the NK1 neurokinin receptor.
DC72869 JNJ-40411813 JNJ-40411813 is a novel potent positive allosteric modulator of mGlu2 with EC50 of 147 nM. JNJ-40411813 displays >30-fold selectivity over mGlu1 and mGlu3-8, 10-fold over 5-HT2A. JNJ-40411813 displays an optimal interplay between potency, selectivity, favorable ADMET/PK and cardiovascular safety profile, and central EEG activity; has been investigated in the clinic for schizophrenia and anxious depression disorders.
DC72880 Norepinephrine hydrochloride Featured Norepinephrine (Levarterenol; L-Noradrenaline) hydrochloride is a potent agonist of adrenergic receptor (AR). Norepinephrine activates α1, α2, β1 receptors.
DC72881 MEN 11270 MEN 11270, a cyclic decapeptide, is a B2 kinin receptor antagonist. MEN 11270 bound with high-affinity to the B2 kinin receptor constitutively expressed by WI38 human fibroblasts, inhibiting 3H-bradykinin (BK) with pKi of 10.3.
DC72882 MR120 MR120 (CCR6 antagonist 1b) is a potent, selective CCR6 antagonist, disrupts the CCL20-induced chemotaxis of CCR6+CD4+ T cells.
DC72907 CB-25 CB-25 is a ligand of CB1 cannabinoid receptors, acting as a partial agonist. CB-25 enhances Forskolin-induced cAMP formation in cancer cells but not hCB1-CHO cells.
DC73359 25B-NBOMe 25B-NBOMe is a highly selective 5-HT2A receptor agonist with Ki of 0.05 nM, 100-fold selective over 5-HT2C (Ki=4.6 nM).
DC73360 AS2030680 AS2030680 is a potent, selective and brain-penetrating 5-HT5A receptor antagonist with Ki of 0.58, 1.1 and 2.6 nM against human, rat, mouse 5-HT5A receptors, respectively.
DC73361 AS2674723 AS2674723 is a potent, selective and brain-penetrating 5-HT5A receptor antagonist with Ki of 0.75, 0.67 and 1.9 nM against human, rat, mouse 5-HT5A receptors, respectively.
DC73362 ASP5736 AS5736 is a potent, selective and brain-penetrating 5-HT5A receptor antagonist with Ki of 3.6, 1.7 and 4.4 nM against human, rat, mouse 5-HT5A receptors, respectively.
DC73363 CSTI-300 CSTI-300 (SMP-100) is a potent, selective 5-HT3 receptor partial agonist with high affinity for human and rat 5-HT3 receptor (Ki=2.0 nM).
DC73364 E-6801 E-6801 is a potent, selective 5-HT6 receptor partial agonist of 5-HT6 receptor with pKi of 8.46, cAMP formation EC50 of 8.02.
DC73365 NH300094 NH300094 is a potent antagonist of 5-HT receptors and dopamine receptors with IC50 of 0.47 nM, 1.04 nM, 11.71 nM and 31.55 nM for 5-HT2A, D2L, D2S and D3 receptors, respectively.
DC73366 NU-1223 NU-1223 is a β carboline analog of alstonine and serotonin 5-HT2C receptor agonist, blocks phencyclidine and amphetamine-induced hyperactivity in subchronic phencyclidine mice.
DC73367 PZ-1922 PZ-1922 is a potent, triple-acting 5-HT6R/5-HT3R antagonist and MAO-B reversible inhibitor with Ki of 17/0.45 nM (5-HT6R/5-HT3R), and pIC50 of 8.93 for MAO-B.
DC73368 TZB-30878 TZB-30878 is a potent, selective, orally bioavailable 5-HT1A agonist and 5-HT3 antagonist, selectively binds to human 5-HT1A and 5-HT) receptors with Kd values of 0.68 and 8.90 nM, respectively.
DC73369 VU6047534 VU6047534 is a selective, peripherally restricted 5-HT2B partial agonist with IC50 of 480 nM in radioligand binding assays.
DC73370 BnOCPA BnOCPA is a potent and powerful analgesic and a highly selective and potent, full agonist at human adenosine A1 receptors (A1Rs) with pEC50 of 7.23 in a NanoBRET agonist binding assay.
DC73371 I-ABOPX I-ABOPX (BW-A522) is a potent, selective A3 adenosine receptor antagonist with high affinity for both the ovine (Ki=3 nM) and human (Ki=19 nM) A3 receptors.
DC73372 KF-26777 KF-26777 (KF26777) is a potent and selective adenosine A3 receptor antagonist with Ki of 0.2 nM (human A3 receptor).
DC73373 MRS7935 MRS7935 is a potent, selective positive allosteric modulator (PAM) of A1 adenosine receptor (A1AR) with EC50 of 1.43 uM.
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