GPR81 agonist 1

• CAT Number: I044505
• CAS Number: 1620992-67-7
• Molecular Formula: C22H30N4O2S2
• Molecular Weight: 446.63
• Purity: ≥95%
• Synonyms: 4-methyl-N-[5-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]-4-thiophen-2-yl-1,3-thiazol-2-yl]cyclohexane-1-carboxamide
• InChI: InChI=1S/C22H30N4O2S2/c1-15-5-7-16(8-6-15)21(28)24-22-23-20(17-4-3-13-29-17)18(30-22)14-19(27)26-11-9-25(2)10-12-26/h3-4,13,15-16H,5-12,14H2,1-2H3,(H,23,24,28)
• InChIKey: ZLQAEANISSHOLB-UHFFFAOYSA-N
• SMILES: CC1CCC(CC1)C(=O)NC2=NC(=C(S2)CC(=O)N3CCN(CC3)C)C4=CC=CS4

GPR81 agonist 1 is a potent and highly selective GPR81 agonist, with EC50s of 58 nM and 50 nM for human and mouse GPR81, respectively. GPR81 agonist 1 inhibits lipolysis in differentiated 3T3-L1 adipocytes. GPR81 agonist 1 suppresses lipolysis in mice without cutaneous flushing. GPR81 agonist 1 displays remarkable selectivity for GPR81 over GPR109a[1].
GPR81 agonist 1 (compound 2) (1-1000 nM) inhibits lipolysis in differentiated 3T3-L1 adipocytes[1].
GPR81 agonist 1 (100 mg/kg; i.p.) suppresses lipolysis in mice without cutaneous flushing[1].
GPR81 agonist 1 (10 mg/kg; i.p.) shows good bioavailability (71%) and Cmax (6.3 μM)[1].

Reference

[1]. Sakurai T, et al. Identification of a novel GPR81-selective agonist that suppresses lipolysis in mice without cutaneous flushing. Eur J Pharmacol. 2014;727:1-7.
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