CX08005
SIGMA/SML1739 - ≥98% (HPLC)
Synonym: 2-
CAS Number: 1256341-22-6
Empirical Formula (Hill Notation): C28H39NO4
Molecular Weight: 453.61
Linear Formula: C28H39NO4
Product Type: Chemical
assay | ≥98% (HPLC) |
color | white to beige |
form | powder |
Quality Level | 100 |
SMILES string | O=C(O)C1=C(C(NC2=C(OCCCCC |
solubility | DMSO: 20 mg/mL, clear |
storage temp. | 2-8°C |
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). |
Packaging: | 5, 25 mg in glass bottle |
RIDADR | NONH for all modes of transport |
WGK Germany | WGK 3 |
Flash Point(F) | Not applicable |
Flash Point(C) | Not applicable |
Purity | ≥98% (HPLC) |
Storage Temp. | 2-8°C |
UNSPSC | 12352200 |