DPM-1001
DPM-1001 Basic information
- Product Name:
- DPM-1001
- Synonyms:
-
- DPM-1001
- DPM-1001 (DPM1001)
- Cholan-24-oic acid, 7-hydroxy-3-[[4-[(2-pyridinylmethyl)amino]butyl]amino]-, methyl ester, (3α,5α,7α)-
- CAS:
- 1471172-27-6
- MF:
- C35H57N3O3
- MW:
- 567.86
- Mol File:
- 1471172-27-6.mol
DPM-1001 Chemical Properties
- Boiling point:
- 656.4±50.0 °C(Predicted)
- Density
- 1.10±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- form
- Solid
- pka
- 14.83±0.70(Predicted)
- color
- Light yellow to brown
DPM-1001 Usage And Synthesis
Uses
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[1].
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[1].
| Animal Model: | 18 weeks of age, high-fat diet (HFD)-fed obese male mice (C57bl6/J)[1] |
| Dosage: | 5 mg/kg |
| Administration: | Oral or intraperitoneal administration; 5 mg/kg; once daily; 50 days |
| Result: | Led to an 5% decrease in body weight.Improved glucose tolerance and insulin sensitivity in glucose tolerance and insulin tolerance in vivo. |
References
[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. DOI:10.1074/jbc.C117.819110
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