For research use only. Not for therapeutic Use.
DPM-1001 trihydrochloride is a potent, specific, orally active and non-competitive inhibitor of protein-tyrosine phosphatase (PTP1B) with an IC50 of 100 nM. DPM-1001 trihydrochloride is an analog of the specific PTP1B inhibitor MSI-1436. DPM-1001 trihydrochloride has anti-diabetic property[1].
DPM-1001 trihydrochloride inhibits the short form of PTP1B reversibly, whereas PTP1B(1–405) remained inactive over an extended period of time. DPM-1001 is against PTP1B(1–405) with no pre-incubation, the IC50 value for PTP1B(1–405) is 600 nM. However, after a 30-min pre-incubation, the potency is improved to 100 nM. In contrast, there is no obvious time-dependent change in the IC50 value for PTP1B(1–321)[1].
DPM-1001 trihydrochloride (oral or intraperitoneal administration; 5 mg/kg; once daily; 50 days) inhibits diet-induced obesity in mice by improving insulin and leptin signaling. DPM-1001 trihydrochloride-treated, high-fat diet-fed mice starts losing weight within 5 days of treatment. The weight loss continues for approximately 3 weeks, after which no further decrease in body weight is observed[1].
| Catalog Number | I045530 |
| Synonyms | methyl (4R)-4-[(3R,5R,7R,8R,9S,10S,13R,14S,17R)-7-hydroxy-10,13-dimethyl-3-[4-(pyridin-2-ylmethylamino)butylamino]-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoate;trihydrochloride |
| Molecular Formula | C35H60Cl3N3O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C35H57N3O3.3ClH/c1-24(10-13-32(40)41-4)28-11-12-29-33-30(15-17-35(28,29)3)34(2)16-14-26(21-25(34)22-31(33)39)37-20-8-7-18-36-23-27-9-5-6-19-38-27;;;/h5-6,9,19,24-26,28-31,33,36-37,39H,7-8,10-18,20-23H2,1-4H3;3*1H/t24-,25-,26-,28-,29+,30+,31-,33+,34+,35-;;;/m1.../s1 |
| InChIKey | VMETYCIJFJYNQW-NIETXTDOSA-N |
| SMILES | CC(CCC(=O)OC)C1CCC2C1(CCC3C2C(CC4C3(CCC(C4)NCCCCNCC5=CC=CC=N5)C)O)C.Cl.Cl.Cl |
| Reference | [1]. Krishnan N, et al. A potent, selective, and orally bioavailable inhibitor of the protein-tyrosine phosphatase PTP1B improves insulin and leptin signaling in animal models. J Biol Chem. 2018 Feb 2;293(5):1517-1525. |
