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GPR81 agonist 1

Chemical Structure : GPR81 agonist 1

CAS No.: 1620992-67-7

GPR81 agonist 1

Catalog No.: PC-25930Not For Human Use, Lab Use Only.

GPR81 agonist 1 is a potent and highly selective GPR81 agonist with EC50 of 58 nM and 50 nM for human and mouse GPR81 respectively, also is an agonist-positive allosteric modulator (Ago-PAM) for HCAR1.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GPR81 agonist 1 is a potent and highly selective GPR81 agonist with EC50 of 58 nM and 50 nM for human and mouse GPR81 respectively, also is an agonist-positive allosteric modulator (Ago-PAM) for HCAR1.
GPR81 agonist 1 displays remarkable selectivity for GPR81 over GPR109a.
GPR81 agonist 1 inhibits lipolysis in differentiated 3T3-L1 adipocytes.
GPR81 agonist 1 suppresses lipolysis in mice without cutaneous flushing.

Physicochemical Properties

M.Wt 446.63
Formula C22H30N4O2S2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

trans-4-Methyl-N-[5-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]-4-(2-thienyl)-1,3-thiazol-2-yl]cyclohexanecarboxamide

References

1. Sakurai T, et al. Eur J Pharmacol. 2014;727:1-7.

2. Lind S, et al. Br J Pharmacol. 2025 Dec 23. doi: 10.1111/bph.70312.

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