DPM-1001trihydrochloride
PRODUCTS SPECIFICATIONS
DESCRIPTION
Overview
| MDL | - |
|---|---|
| Molecular Weight | 677.23 |
| Molecular Formula | C35H60Cl3N3O3 |
| SMILES | O[C@H]1[C@]2([H])[C@](CC[C@]3(C)[C@@]2([H])CC[C@@]3([H])[C@H](C)CCC(OC)=O)([H])[C@]4(C)[C@@](C[C@H](NCCCCNCC5=CC=CC=N5)CC4)([H])C1.Cl.Cl.Cl |
Summary
DPM-1001 trihydrochloride is a potent, specific, orally active and non-competitive inhibitor of protein-tyrosine phosphatase (PTP1B) with an IC 50 of 100 nM. DPM-1001 trihydrochloride is an analog of the specific PTP1B inhibitor MSI-1436. DPM-1001 trihydrochloride has anti-diabetic property [1] .
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 IC 50 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 IC 50 value for PTP1B(1–321) [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | 18 weeks of age, high-fat diet (HFD)-fed obese male mice (C57bl6/J) |
| Dosage: | 5 mg/kg |
| Administration: | Oral or intraperitoneal administration; 5 mg/kg; once daily; 50 day |
| Result: |
Led to an 5% decrease in body weight.
Improved glucose tolerance and insulin sensitivity in glucose tolerance and insulin tolerance in vivo . |
Appearance
Solid
Shipping
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)
Solvent & Solubility
DMSO : 80 mg/mL ( 118.13 mM ; Need ultrasonic)
H 2 O : 33.33 mg/mL ( 49.22 mM ; ultrasonic and warming and heat to 60°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.4766 mL | 7.3830 mL | 14.7660 mL |
| 5 mM | 0.2953 mL | 1.4766 mL | 2.9532 mL |
| 10 mM | 0.1477 mL | 0.7383 mL | 1.4766 mL |
