LMPTP INHIBITOR 1 dihydrochloride 是选择性的低分子量蛋白酪氨酸磷酸酶(LMPTP)抑制剂,抑制 LMPTP-A 活性的IC50为 0.8 μM。
产品描述
LMPTP INHIBITOR 1 dihydrochloride is a selective inhibitor of low molecular weight protein tyrosine phosphatase (LMPTP), with an IC50 of 0.8 μM LMPTP-A.
体外活性
LMPTP INHIBITOR 1 dihydrochloride is a selective inhibitor of low molecular weight protein tyrosine phosphatase, with an IC50?of 0.8 μM LMPTP-A and shows more potent effect on LMPTP-A versus LMPTP-B. LMPTP inhibitor 1 dihydrochloride (10 μM) also enhances HepG2 IR phosphorylation after insulin stimulation in human HepG2 hepatocytes[1].
体内活性
LMPTP inhibitor 1 dihydrochloride is orally bioavailable, and results in appr 680 nM mean serum concentration after treatment of 0.03% w/w, while treatment with 0.05% w/w results in >3 μM; also reverses diabetes in obese mice. LMPTP inhibitor 1 dihydrochloride (0.05% w/w) inhibits LMPTP activity, significantly improves glucose tolerance and decreases fasting insulin levels of diabetic DIO mice, without affecting body weight[1].
Cas No.
2310135-46-5
分子式
C28H38Cl2N4O
分子量
517.54
储存和溶解度
DMSO:64 mg/mL (123.66 mM)
H2O:50 mg/mL (96.61 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years