GPR81 agonist 1 |
| Katalog-Nr.GC61625 |
GPR81-Agonist 1 ist ein potenter und hochselektiver GPR81-Agonist mit EC50-Werten von 58 nM bzw. 50 nM fÜr menschliches bzw. Maus-GPR81.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1620992-67-7
Sample solution is provided at 25 µL, 10mM.
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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]. Animal Model: Nine-week-old male C57/Bl6 mice (fed and fasted mice)[1]
[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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