DPM-1001 trihydrochloride

Name: DPM-1001 trihydrochloride
Brand: MedChemExpress
SKU: HY-121515A
Rating: 4.5 (1 reviews)

Cat. No.: HY-121515A Purity: 98.48%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

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
100 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of DPM-1001 trihydrochloride:

DPM-1001 Get quote

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Biological Activity
Purity & Documentation
References
Customer Review

Description

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].

MedChemExpress (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].

MedChemExpress (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

Appearance

Solid

Color

Off-white to light yellow

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

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

In Vitro:

DMSO : 80 mg/mL (118.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 33.33 mg/mL (49.22 mM; ultrasonic and warming and heat to 60°C)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 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

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (7.38 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 98.48%

Select Batch:

Data Sheet (271 KB) SDS (251 KB)

COA (246 KB) HNMR (288 KB) RP-HPLC (224 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	1.4766 mL	7.3830 mL	14.7660 mL	36.9151 mL
	5 mM	0.2953 mL	1.4766 mL	2.9532 mL	7.3830 mL
	10 mM	0.1477 mL	0.7383 mL	1.4766 mL	3.6915 mL
	15 mM	0.0984 mL	0.4922 mL	0.9844 mL	2.4610 mL
	20 mM	0.0738 mL	0.3692 mL	0.7383 mL	1.8458 mL
	25 mM	0.0591 mL	0.2953 mL	0.5906 mL	1.4766 mL
	30 mM	0.0492 mL	0.2461 mL	0.4922 mL	1.2305 mL
	40 mM	0.0369 mL	0.1846 mL	0.3692 mL	0.9229 mL
DMSO	50 mM	0.0295 mL	0.1477 mL	0.2953 mL	0.7383 mL
	60 mM	0.0246 mL	0.1231 mL	0.2461 mL	0.6153 mL
	80 mM	0.0185 mL	0.0923 mL	0.1846 mL	0.4614 mL
	100 mM	0.0148 mL	0.0738 mL	0.1477 mL	0.3692 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.