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GPCR

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Cat. No. Product Name Field of Application Chemical Structure
DC11757 PB 28 A potent, mixed sigma2 agonist and sigma1 antagonist with Ki of 0.28 and 13.0 nM, respectively.
DC11629 NK1-IN-9 A potent, orally active, dual NK1 receptor antagonist (IC50=0.5 nM) and SERT inhibitor (IC50=5.2 nM).
DC11697 AM-1638 A potent, orally bioavailable, full agonist of GPR40/FFA1 with EC50 of 0.16 uM.
DC11979 SB 332235 A potent, selective and competitive CXCR2 inhibitor that selectively inhibits CXCR2-mediated recruitment of β-arrestin-2 with pKi of 8.92.
DC11755 L-732138 Featured A potent, selective and competitive NK1 receptor antagonist with IC50 of 2.3 nM.
DC11514 Atogepant A potent, selective and orally available CGRP receptor antagonist for the prevention of migraine. Migraine.
DC11519 Ceclazepide A potent, selective cholecystokinin receptor CCK2 antagonist for treatment of gastroesophageal reflux disease (GERD)..
DC12015 SKF 83566 hydrobromide A potent, selective dopamine D1 receptor antagonist with Ki of 0.56 nM.
DC11973 A-412997 A potent, selective dopamine D4 receptor agonist with Ki of 12.1 and 7.9 nM for rat and human D4 receptors, respectively.
DC11700 Chalcone 4 hydrate A potent, selective inhibitor of CXCL12 binding to CXCR4 and CXCR7 with IC50 of 200 nM.
DC11560 SPM-242 A potent, selective S1P3 antagonist with Ki of 0.25 nM.
DC11561 SPM-242 racemate A potent, selective S1P3 antagonist with Ki of 0.25 nM.
DC11745 BMS-22 A potent, selective, allosteric CCR2 antagonist with binding IC50 of 5.1 nM.
DC11744 CCR2-RA-[R] A potent, selective, allosteric CCR2 antagonist with IC50 of 103 nM..
DC11895 Foliglurax hydrochloride A potent, selective, brain-penetrant and orally bioavailable mGluR4 positive allosteric modulator with EC50 of 79 nM.
DC11894 Foliglurax A potent, selective, brain-penetrant and orally bioavailable mGluR4 positive allosteric modulator with EC50 of 79 nM.
DC11666 BMS-470539 A potent, selective, full agonist of human and murine MC1R with EC50 of 16.8 and 11.6 nM, respectively.
DC11746 JNJ-27141491 A potent, selective, noncompetitive, orally active CCR2 antagonist with IC50 of 172 nM.
DC11756 SR 140333 A potent, selective, non-peptide NK1 receptor antagonist with Ki of 0.74 nM, IC50 of 1.6 nM.
DC11667 PF-592379 A potent, selective, orally active agonist of dopamine D3 receptor with EC50 of 21 nM.
DC11683 LY2881835 A potent, selective, orally available GPR40 agonist with EC50 of 8 nM.
DC11682 LY2922083 A potent, selective, orally available GPR40 agonist with EC50 of 9 nM.
DC11680 LY3104607 A potent, selective, orally available GPR40 agonist with Ki of 15 nM, β-arrestin EC50 of 108 nM.
DC11623 GPR120 agonist 4x A potent, selective, orally bioavailable GPR120 agonist with EC50 of 42 nM in calcium flux assays.
DC11748 LY2033298 Featured LY2033298 is a robust allosteric potentiator that is highly selective for the human M4 muscarinic acetylcholine receptor subtype. LY2033298 enhances inhibition by oxotremorine of light-induced phase shifts in hamster circadian activity rhythms.
DC11978 SB 265610 Featured SB-265610 is a selective, competitive, nonpeptide and allosteric CXCR2 antagonist.
DC11983 CX797 A potent, specfic CXCR2 antagonist that inhibits IL8 down-regulation of forskolin-induced cAMP with IC50 of 7.79 uM.
DC11977 SX-517 A potent, specific, noncompetitive dual CXCR1 and CXCR2 antagonist with IC50 of 38 nM (vs. CXCL1) and 36 nM (vs. CXCL8), respectively.
DC11972 PNU 96415E A potential antipsychotic agent that binds selectively to D4 and 5-HT2A receptors with Ki of 3.0 and 5.8 nM, respectively.
DC11545 IPAG Featured IPAG is a prototypic selective inhibitor of sigma1 receptor that engages the unfolded protein response and induces autophagy in cancer cells.

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