SML1739

CX08005

≥98% (HPLC)

• Synonym(e): 2-(((2-(Tetradecyloxy)phenyl)amino)carbonyl)benzoic acid
• Empirische Formel (Hill-System): C₂₈H₃₉NO₄
• CAS-Nummer: 1256341-22-6
• Molekulargewicht: 453.61
• UNSPSC-Code: 12352200
• PubChem Substanz-ID: 329826047
• NACRES: NA.77

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥98% (HPLC)
• Form: powder
• Farbe: white to beige
• Löslichkeit: DMSO: 20 mg/mL, clear
• Lagertemp.: 2-8°C
• SMILES String: O=C(O)C1=C(C(NC2=C(OCCCCCCCCCCCCCC)C=CC=C2)=O)C=CC=C1
• InChIKey: WOEDXTWDPRNPMZ-UHFFFAOYSA-N

Beschreibung

Biochem./physiol. Wirkung

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 (C_max = 7425.9 ng/mL, T_max = 6.67 h,  t_1/2 = 2.5 h).

CX08005 is a cell-permeable, potent and substrate-competitive PTP1B/TCPTP dual inhibitor with anti-diabetic efficacy both in vitro and in vivo.

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable