LMPTP inhibitor 1 dihydrochloride

• CAT Number: I020094
• CAS Number: 2310135-46-5
• Molecular Formula: C28H38Cl2N4O
• Molecular Weight: 517.53
• Purity: ≥95%
• Synonyms: N,N-diethyl-4-[4-(3-piperidin-1-ylpropylamino)quinolin-2-yl]benzamide;dihydrochloride
• InChI: InChI=1S/C28H36N4O.2ClH/c1-3-32(4-2)28(33)23-15-13-22(14-16-23)26-21-27(24-11-6-7-12-25(24)30-26)29-17-10-20-31-18-8-5-9-19-31;;/h6-7,11-16,21H,3-5,8-10,17-20H2,1-2H3,(H,29,30);2*1H
• InChIKey: YDTJMPCNLMSGEO-UHFFFAOYSA-N
• SMILES: CCN(CC)C(=O)C1=CC=C(C=C1)C2=NC3=CC=CC=C3C(=C2)NCCCN4CCCCC4.Cl.Cl

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.
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 (Compound 23; 10 μM) also enhances HepG2 IR phosphorylation after insulin stimulation in human HepG2 hepatocytes[1].
LMPTP inhibitor 1 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) inhibits LMPTP activity, significantly improves glucose tolerance and decreases fasting insulin levels of diabetic DIO mice, without affecting body weight[1].

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.
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