DPM-1001 trihydrochloride

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.

Product information

Molecular Weight: 677.23

Formula: C35H60Cl3N3O3

Chemical Name: methyl (4R)-4-[(1S,3aS,3bR,4R,5aR,7R,9aS,9bR,11aS)-4-hydroxy-9a,11a-dimethyl-7-[(4-{[(pyridin-2-yl)methyl]amino}butyl)amino]-hexadecahydro-1H-cyclopenta[a]phenanthren-1-yl]pentanoate trihydrochloride

Smiles: Cl.Cl.Cl.C[C@H](CCC(=O)OC)[C@@H]1CC[C@H]2[C@@H]3[C@H](O)C[C@H]4C[C@@H](CC[C@]4(C)[C@@H]3CC[C@]21C)NCCCCNCC1=CC=CC=N1

InChiKey: VMETYCIJFJYNQW-KFWJFULESA-N

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

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 80 mg/mL (118.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO). H2O : 33.33 mg/mL (49.22 mM; ultrasonic and warming and heat to 60°C).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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).

In Vivo:

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.

Products are for research use only. Not for human use.