ChemicalBook > CAS DataBase List > TRANS-4-METHYL-N-[5-[2-(4-METHYLPIPERAZIN-1-YL)-2-OXOETHYL]-4-(2-THIENYL)-1,3-THIAZOL-2-YL]CYCLOHEXANECARBOXAMIDE

TRANS-4-METHYL-N-[5-[2-(4-METHYLPIPERAZIN-1-YL)-2-OXOETHYL]-4-(2-THIENYL)-1,3-THIAZOL-2-YL]CYCLOHEXANECARBOXAMIDE

Product Name
TRANS-4-METHYL-N-[5-[2-(4-METHYLPIPERAZIN-1-YL)-2-OXOETHYL]-4-(2-THIENYL)-1,3-THIAZOL-2-YL]CYCLOHEXANECARBOXAMIDE
CAS No.
1620992-67-7
Chemical Name
TRANS-4-METHYL-N-[5-[2-(4-METHYLPIPERAZIN-1-YL)-2-OXOETHYL]-4-(2-THIENYL)-1,3-THIAZOL-2-YL]CYCLOHEXANECARBOXAMIDE
Synonyms
GPR81 agonist 1;GPR81 agonist 1, 10 mM in DMSO;4-Methyl-N-[5-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]-4-thiophen-2-yl-1,3-thiazol-2-yl]cyclohexane-1-carboxamide;Cyclohexanecarboxamide, 4-methyl-N-[5-[2-(4-methyl-1-piperazinyl)-2-oxoethyl]-4-(2-thienyl)-2-thiazolyl]-, trans-;TRANS-4-METHYL-N-[5-[2-(4-METHYLPIPERAZIN-1-YL)-2-OXOETHYL]-4-(2-THIENYL)-1,3-THIAZOL-2-YL]CYCLOHEXANECARBOXAMIDE
CBNumber
CB74923951
Molecular Formula
C22H30N4O2S2
Formula Weight
446.63
MOL File
1620992-67-7.mol
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TRANS-4-METHYL-N-[5-[2-(4-METHYLPIPERAZIN-1-YL)-2-OXOETHYL]-4-(2-THIENYL)-1,3-THIAZOL-2-YL]CYCLOHEXANECARBOXAMIDE Property

Density 
1.263±0.06 g/cm3(Predicted)
form 
Solid
pka
8.08±0.70(Predicted)
color 
White to off-white
InChIKey
ZLQAEANISSHOLB-WKILWMFISA-N
SMILES
[C@@H]1(C(NC2=NC(C3SC=CC=3)=C(CC(N3CCN(C)CC3)=O)S2)=O)CC[C@@H](C)CC1
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Hazard and Precautionary Statements (GHS)

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TRANS-4-METHYL-N-[5-[2-(4-METHYLPIPERAZIN-1-YL)-2-OXOETHYL]-4-(2-THIENYL)-1,3-THIAZOL-2-YL]CYCLOHEXANECARBOXAMIDE Chemical Properties,Usage,Production

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.
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).

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

TRANS-4-METHYL-N-[5-[2-(4-METHYLPIPERAZIN-1-YL)-2-OXOETHYL]-4-(2-THIENYL)-1,3-THIAZOL-2-YL]CYCLOHEXANECARBOXAMIDE Preparation Products And Raw materials

Raw materials

Preparation Products

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TRANS-4-METHYL-N-[5-[2-(4-METHYLPIPERAZIN-1-YL)-2-OXOETHYL]-4-(2-THIENYL)-1,3-THIAZOL-2-YL]CYCLOHEXANECARBOXAMIDE Suppliers

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1620992-67-7, TRANS-4-METHYL-N-[5-[2-(4-METHYLPIPERAZIN-1-YL)-2-OXOETHYL]-4-(2-THIENYL)-1,3-THIAZOL-2-YL]CYCLOHEXANECARBOXAMIDERelated Search:


  • 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-
  • GPR81 agonist 1
  • GPR81 agonist 1, 10 mM in DMSO
  • 4-Methyl-N-[5-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]-4-thiophen-2-yl-1,3-thiazol-2-yl]cyclohexane-1-carboxamide
  • 1620992-67-7