半岛bd体育手机客户端 说明
包装
5, 25 mg in glass bottle
生化/生理作用
CX08005 is a cell-permeable benzoic acid based compound, potent and substrate-competitive PTP1B/TCPTP dual inhibitor with anti-diabetic efficacy bothin vitroandin 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 vivowith good pharmacokinetics in SD rats (Cmax= 7425.9 ng/mL,Tmax= 6.67 h, t1/2= 2.5 h).
基本信息
经验(实验)分子式 | C28H39NO4 |
分子量 | 453.61 |
PubChem化学物质编号 | 329826047 |
NACRES | NA.77 |
半岛bd体育手机客户端 性质
质量水平 | 100 |
测定 | ≥98% (HPLC) |
形式 | powder |
颜色 | white to beige |
溶解性 | DMSO: 20 mg/mL, clear |
储存温度 | 2-8℃ |
SMILES string | O=C(O)C1=C(C(NC2=C(OCCCCCCCCCCCCCC)C=CC=C2)=O)C=CC=C1 |
安全信息
储存分类代码 | 13 - Non Combustible Solids |
WGK | WGK 3 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |
Sigma-Aldrich