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SML1739 Sigma-Aldrich

CX08005

≥98% (HPLC)

Synonym: 2-(((2-(Tetradecyloxy)phenyl)amino)carbonyl)benzoic acid

  • CAS Number 1256341-22-6

  • Empirical Formula (Hill Notation) C28H39NO4

  • Molecular Weight 453.61

  •  PubChem Substance ID 329826047

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Properties

Related Categories Cell Biology, Cell Signaling and Neuroscience, Kinase/Phosphatase Biology, Phosphatase Inhibitors
assay   ≥98% (HPLC)
form   powder
color   white to beige
solubility   DMSO: 20 mg/mL, clear
storage temp.   2-8°C

Description

Packaging

5, 25 mg in glass bottle

Biochem/physiol Actions

CX08005 is a cell-permeable benzoic acid based compound, potent and substrate-competitive PTP1B/TCPTP dual inhibitor with anti-diabetic efficacy both in vitro and in vivo. CX08005 targets protein tyrosine phosphatase 1B (PTP1B) catalytic P-loop and acts as a substrate-competitive inhibitor against PTP1B and TCPTP (IC50 = 781 and 475 nM, respectively) with much reduced potency toward LAR, SHP1, and VHR (by 52%, 89%, and 60%, respectively, at 10 μM). CX08005 enhances insulin-dependent cellular signaling (Eff. conc. 10 nM; HepG2 cells) and glucose uptake (Eff. conc. 100-500 nM; 3T3-L1 adipocityes and C2C12 myoblasts) in vitro, as well as improves glucose tolerance and insulin sensitivity in diet-induced obesity (DIO) mice and KKAy type 2 diabetes mice (50-200 mg/kg/day i.p.) in vivo with good pharmacokinetics in SD rats (Cmax = 7425.9 ng/mL, Tmax = 6.67 h,  t1/2 = 2.5 h).

Safety & Documentation

Safety Information

RIDADR 
NONH for all modes of transport

Documents

Certificate of Analysis

Protocols & Articles
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