SML1739
CX08005
≥98% (HPLC)
Synonym(s):
2-(((2-(Tetradecyloxy)phenyl)amino)carbonyl)benzoic acid
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About This Item
Empirical Formula (Hill Notation):
C28H39NO4
CAS Number:
Molecular Weight:
453.61
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
Quality Level
Assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 20 mg/mL, clear
storage temp.
2-8°C
SMILES string
O=C(O)C1=C(C(NC2=C(OCCCCCCCCCCCCCC)C=CC=C2)=O)C=CC=C1
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).
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
新产品
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