LMPTP inhibitor 1 dihydrochloride

Name: LMPTP inhibitor 1 dihydrochloride
Brand: MedChemExpress
SKU: HY-111489B
Rating: 4.5 (1 reviews)

Cat. No.: HY-111489B Purity: 99.83%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

LMPTP INHIBITOR 1 (dihydrochloride) is a selective inhibitor of low molecular weight protein tyrosine phosphatase (LMPTP), with an IC₅₀ of 0.8 μM LMPTP-A.

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

LMPTP inhibitor 1 dihydrochloride Chemical Structure

CAS No. : 2310135-46-5

Size	Price	Stock	Quantity
Free Sample (0.1 - 0.5 mg)		Apply Now
5 mg	USD 210	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 340	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1000	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1650	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 1 publication(s) in Google Scholar

Other Forms of LMPTP inhibitor 1 dihydrochloride:

LMPTP inhibitor 1 Get quote
LMPTP inhibitor 1 hydrochloride Get quote

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

LMPTP INHIBITOR 1 (dihydrochloride) is a selective inhibitor of low molecular weight protein tyrosine phosphatase (LMPTP), with an IC₅₀ of 0.8 μM LMPTP-A.

IC₅₀ & Target

IC50: 0.8 μM (LMPTP-A)^[1]

In Vitro

LMPTP INHIBITOR 1 (dihydrochloride) is a selective inhibitor of low molecular weight protein tyrosine phosphatase, with an IC₅₀ of 0.8 μM LMPTP-A and shows more potent effect on LMPTP-A versus LMPTP-B. LMPTP inhibitor 1 (Compound 23; 10 μM) also enhances HepG2 IR phosphorylation after insulin stimulation in human HepG2 hepatocytes^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

LMPTP inhibitor 1 is orally bioavailable, and results in appr 680 nM mean serum concentration after treatment of 0.03% w/w, while treatment with 0.05% w/w results in >3 μM; also reverses diabetes in obese mice. LMPTP inhibitor 1 (0.05% w/w) inhibits LMPTP activity, significantly improves glucose tolerance and decreases fasting insulin levels of diabetic DIO mice, without affecting body weight^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

517.53

Formula

C₂₈H₃₈Cl₂N₄O

CAS No.

2310135-46-5

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(N(CC)CC)C1=CC=C(C2=NC3=CC=CC=C3C(NCCCN4CCCCC4)=C2)C=C1.Cl.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : ≥ 64 mg/mL (123.66 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 50 mg/mL (96.61 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9323 mL	9.6613 mL	19.3225 mL
5 mM	0.3865 mL	1.9323 mL	3.8645 mL
10 mM	0.1932 mL	0.9661 mL	1.9323 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 (sealed storage, away from moisture). 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: ≥ 2.5 mg/mL (4.83 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (4.83 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (4.83 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 100 mg/mL (193.23 mM); Clear solution; Need ultrasonic

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: 99.83%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (250 KB) LCMS (107 KB)

Handling Instructions (2659 KB)

References

[1]. Stanford SM1, et al. Diabetes reversal by inhibition of the low-molecular-weight tyrosine phosphatase. Nat Chem Biol. 2017 Jun;13(6):624-632. [Content Brief]

Kinase Assay ^[1]	Phosphatase assays are performed in buffer containing 50 mM Bis-Tris, pH 6.0, 1 mM DTT and 0.01% Triton X-100 at 37°C. For assays conducted with 3-O-methylfluorescein phosphate (OMFP) as substrate, fluorescence is monitored continuously at λ_ex = 485 and λ_em = 525 nm. For assays conducted with para-nitrophenylphosphate (pNPP) as substrate, the reaction is stopped by addition of 2X reaction volume of 1 M NaOH, and absorbance is measured at 405 nm. IC₅₀ values are determined from plots of LMPTP inhibitor 1 concentration versus percentage of enzyme activity. For inhibitor selectivity assays, each PTP is incubated with either 0.4 mM OMFP or 5 mM pNPP in the presence of 40 μM LMPTP inhibitor 1 or DMSO. Equal units of enzyme activity, comparable to the activity of 10 nM human LMPTP-A, are used. For the inhibitor reversibility assay, 50 nM human LMPTP-A is pre-incubated with 10 μM LMPTP inhibitor 1 or DMSO for 5 min. The enzyme is diluted 100X in phosphatase assay buffer containing 0.4 mM OMFP and fluorescence is measured at the indicated time points^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	Human HepG2 cells are cultured in Eagle’s Minimal Essential Medium (ATCC) containing 10% fetal bovine serum (FBS), 100 U/mL penicillin and 100 μg/mL streptomycin. The absence of Mycoplasma contamination in HepG2 cultures is confirmed using the Lonza MycoAlert Mycoplasma Detection Kit. Cells are treated with 10 μM LMPTP inhibitor 1 in serum-starvation media (0.1% FBS) overnight, following which cells are stimulated with 10 nM bovine insulin for 5 min at 37°C. For detection of IR tyrosine phosphorylation by immunoprecipitation/Western blotting, cells are lysed in radioimmunoprecipitation assay buffer containing 1 mM phenylmethylsulfonyl fluoride, 10 μg/mL aprotinin/leupeptin, 10 mM sodium orthovanadate, 5 mM sodium fluoride, and 2 mM sodium pyrophosphate, and the IR is immunoprecipitated using the anti-IRβ Ab. IR tyrosine phosphorylation of immunoprecipitates is determined by Western blotting with the anti-pIR/pIGFR-Y1162/Y1163 Ab^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] LMPTP inhibitor 1 is administered to male B6 or Acp1^fl/fl albumin-Cre⁺ DIO mice at 0.05% w/w in high-fat diet (HFD) rodent chow. Control groups consist of male B6 or Acp1^fl/fl albumin-Cre⁺ littermate mice administered HFD rodent chow alone. Mice are allowed food and water ad libitum and weighed daily. Randomization is not used in these experiments; rather littermate mice are assigned to treatment or control groups in a manner to maintain similar mean body weights between the 2 groups at the start of the study. Insulin-induced liver IR phosphorylation, IPGTT and fasting insulin levels are assessed after treatment. Diabetic (displaying overnight [13 hr] fasting blood glucose levels ≥140 mg/dL) B6 DIO mice are used in experiments to assess IPGTT and fasting insulin levels^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Stanford SM1, et al. Diabetes reversal by inhibition of the low-molecular-weight tyrosine phosphatase. Nat Chem Biol. 2017 Jun;13(6):624-632. [Content Brief]

Complete Stock Solution Preparation Table

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

H₂O / DMSO	1 mM	1.9323 mL	9.6613 mL	19.3226 mL	48.3064 mL
	5 mM	0.3865 mL	1.9323 mL	3.8645 mL	9.6613 mL
	10 mM	0.1932 mL	0.9661 mL	1.9323 mL	4.8306 mL
	15 mM	0.1288 mL	0.6441 mL	1.2882 mL	3.2204 mL
	20 mM	0.0966 mL	0.4831 mL	0.9661 mL	2.4153 mL
	25 mM	0.0773 mL	0.3865 mL	0.7729 mL	1.9323 mL
	30 mM	0.0644 mL	0.3220 mL	0.6441 mL	1.6102 mL
	40 mM	0.0483 mL	0.2415 mL	0.4831 mL	1.2077 mL
	50 mM	0.0386 mL	0.1932 mL	0.3865 mL	0.9661 mL
	60 mM	0.0322 mL	0.1610 mL	0.3220 mL	0.8051 mL
	80 mM	0.0242 mL	0.1208 mL	0.2415 mL	0.6038 mL
DMSO	100 mM	0.0193 mL	0.0966 mL	0.1932 mL	0.4831 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.