Bioactivity | LMPTP inhibitor 1 hydrochloride is a selective inhibitor of low molecular weight protein tyrosine phosphatase (LMPTP), with an IC50 of 0.8 μM LMPTP-A. |
Target | IC50: 0.8 μM (LMPTP-A) |
Invitro | LMPTP inhibitor 1 hydrochloride 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 (Compound 23; 10 μM) hydrochloride also enhances HepG2 IR phosphorylation after insulin stimulation in human HepG2 hepatocytes[1]. |
In Vivo | LMPTP inhibitor 1 hydrochloride 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 (0.05% w/w) hydrochloride inhibits LMPTP activity, significantly improves glucose tolerance and decreases fasting insulin levels of diabetic DIO mice, without affecting body weight[1]. |
Name | LMPTP inhibitor 1 hydrochloride |
CAS | 2310135-38-5 |
Formula | C28H37ClN4O |
Molar Mass | 481.07 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Stanford SM1, et al. Diabetes reversal by inhibition of the low-molecular-weight tyrosine phosphatase. Nat Chem Biol. 2017 Jun;13(6):624-632. |