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GPR81 agonist 1

CAS No. 1620992-67-7

GPR81 agonist 1( —— )

Catalog No. M35660 CAS No. 1620992-67-7

GPR81 agonist 1 is a potent and selective GPR81 agonist with high affinity for human and mouse GPR81, inhibiting lipolysis of differentiated 3T3-L1 adipocytes, improving insulin sensitivity and glycaemic control in mouse models of insulin resistance and diabetes, and can be used in the study of diabetes and obesity.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    GPR81 agonist 1
  • Note
    Research use only, not for human use.
  • Brief Description
    GPR81 agonist 1 is a potent and selective GPR81 agonist with high affinity for human and mouse GPR81, inhibiting lipolysis of differentiated 3T3-L1 adipocytes, improving insulin sensitivity and glycaemic control in mouse models of insulin resistance and diabetes, and can be used in the study of diabetes and obesity.
  • Description
    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.
  • In Vitro
    ——
  • In Vivo
    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 Cmax (6.3 μM).
  • Synonyms
    ——
  • Pathway
    Cell Cycle/DNA Damage
  • Target
    GPR
  • Recptor
    GPR
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1620992-67-7
  • Formula Weight
    446.63
  • Molecular Formula
    C22H30N4O2S2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 50 mg/mL (111.95 mM; Ultrasonic )
  • SMILES
    C[C@H]1CC[C@@H](CC1)C(=O)Nc1nc(c(CC(=O)N2CCN(C)CC2)s1)-c1cccs1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

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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