10mM in DMSO for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
GPR81 agonist 1 is a potent and highly selective GPR81 agonist, with EC 50 s 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.
In Vitro
GPR81 agonist 1 (compound 2) (1-1000 nM) inhibits lipolysis in differentiated 3T3-L1 adipocytes. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 C max (6.3 μM) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Nine-week-old male C57/Bl6 mice (fed and fasted mice) Dosage: 100 mg/kg Administration: I.p. Result: Reduced plasma FFA content of fed and fasted mice by approximately 50% and 35%, respectively, at 15 min postdose when intraperitoneally administered at a dose of 100 mg/kg. Animal Model: Male C57/Bl6 mice Dosage: 10 mg/kg (Pharmacokinetic Analysis) Administration: I.p.(Pharmacokinetic Analysis) Result: Showed good bioavailability (71%) and C max (6.3 μM).
| Isomeric SMILES | CC1CCC(CC1)C(=O)NC2=NC(=C(S2)CC(=O)N3CCN(CC3)C)C4=CC=CS4 |
|---|---|
| PubChem CID | 86279608 |
| Molecular Weight | 446.63 |
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View spec sheet →| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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