DPM-1001 trihydrochloride_product_DataBase

Bioactivity	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].
Invitro	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].
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[1]. Animal Model:
Name	DPM-1001 trihydrochloride
Formula	C35H60Cl3N3O3
Molar Mass	677.23
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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.

PeptideDB

DPM-1001 trihydrochloride

CAS: F: C35H60Cl3N3O3 W: 677.23