1. Metabolic Enzyme/Protease
  2. Phosphatase
  3. DPM-1001 trihydrochloride

DPM-1001 trihydrochloride 

Cat. No.: HY-121515A Purity: ≥98.0% ee.: 100%
Handling Instructions

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.

For research use only. We do not sell to patients.

DPM-1001 trihydrochloride Chemical Structure

DPM-1001 trihydrochloride Chemical Structure

Size Price Stock Quantity
5 mg USD 480 In-stock
Estimated Time of Arrival: December 31
10 mg USD 810 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

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].

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)[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.
Molecular Weight

677.23

Formula

C₃₅H₆₀Cl₃N₃O₃

SMILES
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under argon

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under argon)

Solvent & Solubility
In Vitro: 

DMSO : 80 mg/mL (118.13 mM; Need ultrasonic)

Preparing
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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 5 mg/mL (7.38 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 5 mg/mL (7.38 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 5 mg/mL (7.38 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

DPM-1001 trihydrochloridePhosphataseInhibitorinhibitorinhibit

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Product Name:
DPM-1001 trihydrochloride
Cat. No.:
HY-121515A
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