Description
DPM-1001 is a potent, specific, orally active and non-competitive inhibitor of protein-tyrosine phosphatase (PTP1B) with an IC50 of 100 nM. DPM-1001 is an analog of the specific PTP1B inhibitor MSI-1436. DPM-1001 has anti-diabetic property.
Product information
CAS Number: 1471172-27-6
Molecular Weight: 567.85
Formula: C35H57N3O3
Chemical Name: methyl (4R)-4-[(1R,3aS,3bR,4R,5aR,7R,9aS,9bS,11aR)-4-hydroxy-9a,11a-dimethyl-7-[(4-{[(pyridin-2-yl)methyl]amino}butyl)amino]-hexadecahydro-1H-cyclopenta[a]phenanthren-1-yl]pentanoate
Smiles: 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: RVANDQULNPITCN-MCVYBXALSA-N
InChi: InChI=1S/C35H57N3O3/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/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)
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 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 (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-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.
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