| Identification | Back Directory | [Name]
TRANS-4-METHYL-N-[5-[2-(4-METHYLPIPERAZIN-1-YL)-2-OXOETHYL]-4-(2-THIENYL)-1,3-THIAZOL-2-YL]CYCLOHEXANECARBOXAMIDE | [CAS]
1620992-67-7 | [Synonyms]
TRANS-4-METHYL-N-[5-[2-(4-METHYLPIPERAZIN-1-YL)-2-OXOETHYL]-4-(2-THIENYL)-1,3-THIAZOL-2-YL]CYCLOHEXANECARBOXAMIDE
Cyclohexanecarboxamide, 4-methyl-N-[5-[2-(4-methyl-1-piperazinyl)-2-oxoethyl]-4-(2-thienyl)-2-thiazolyl]-, trans- | [Molecular Formula]
C22H30N4O2S2 | [MDL Number]
MFCD28502089 | [MOL File]
1620992-67-7.mol | [Molecular Weight]
446.63 |
| Hazard Information | Back Directory | [Uses]
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]. | [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: | Nine-week-old male C57/Bl6 mice (fed and fasted mice)[1] | | 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.
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| Animal Model: | Male C57/Bl6 mice[1] | | Dosage: | 10 mg/kg (Pharmacokinetic Analysis) | | Administration: | I.p.(Pharmacokinetic Analysis) | | Result: | Showed good bioavailability (71%) and Cmax (6.3 μM).
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| [References]
[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. DOI:10.1016/j.ejphar.2014.01.029 |
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Biorbyt Ltd.
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+44 (0)1223 859 353 |
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http://www.biorbyt.com |
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