GPR81 agonist 1_product_DataBase

Bioactivity

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].

Invitro

GPR81 agonist 1 (compound 2) (1-1000 nM) inhibits lipolysis in differentiated 3T3-L1 adipocytes[1].

In Vivo

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]. Animal Model:

Name

GPR81 agonist 1

CAS

1620992-67-7

Formula

C22H30N4O2S2

Molar Mass

446.63

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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.

PeptideDB

GPR81 agonist 1

CAS: 1620992-67-7 F: C22H30N4O2S2 W: 446.63