Description
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.
Product information
CAS Number: 1620992-67-7
Molecular Weight: 446.63
Formula: C22H30N4O2S2
Chemical Name: 4-methyl-N-{5-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]-4-(thiophen-2-yl)-1,3-thiazol-2-yl}cyclohexane-1-carboxamide
Smiles: CN1CCN(CC1)C(=O)CC1SC(NC(=O)C2CCC(C)CC2)=NC=1C1=CC=CS1
InChiKey: ZLQAEANISSHOLB-UHFFFAOYSA-N
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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 50 mg/mL (111.95 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
GPR81 agonist 1 (compound 2) (1-1000 nM) inhibits lipolysis in differentiated 3T3-L1 adipocytes.
In Vivo:
GPR81 agonist 1 (100 mg/kg; i.p.) suppresses lipolysis in mice without cutaneous flushing. GPR81 agonist 1 (10 mg/kg; i.p.) shows good bioavailability (71%) and Cmax (6.3 μM).
Products are for research use only. Not for human use.
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