PF-06424439 methanesulfonate

Name: PF-06424439 methanesulfonate
Brand: MedChemExpress
SKU: HY-108341A
Rating: 5.0 (12 reviews)

Cat. No.: HY-108341A Purity: 99.85%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

PF-06424439 methanesulfonate is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC₅₀ of 14 nM. PF-06424439 methanesulfonate is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate.

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

PF-06424439 methanesulfonate Chemical Structure

CAS No. : 1469284-79-4

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 83	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 83	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 70	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 400	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 650	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 12 publication(s) in Google Scholar

Other Forms of PF-06424439 methanesulfonate:

PF-06424439 Get quote

12 Publications Citing Use of MCE PF-06424439 methanesulfonate

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•Related Screening Libraries:

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View All Acyltransferase Isoform Specific Products:

View All Isoforms

ACAT1 ACAT2 MGAT2 ACAT

Biological Activity
Purity & Documentation
References
Customer Review

Description

PF-06424439 methanesulfonate is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC₅₀ of 14 nM^[1]. PF-06424439 methanesulfonate is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate^[2].

IC₅₀ & Target

IC50: 14 nM (DGAT2)^[1]

In Vivo

PF-06424439 methanesulfonate (p.o.; 60 mg/kg/day; for 3 days) reduces plasma TG and cholesterol levels and decreases nonsignificant in circulating lipids in mice (Ldlr^-/-)^[1].
PF-06424439 methanesulfonate (i.v.; 1 mg/kg) shows moderate clearance in rats following intravenous administration and moderate steady-state volume of distribution (Vd_ss) results in a short half-life^[1].

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

Animal Model:	Male low-density lipoprotein receptor (Ldlr) knockout mice (Ldlr^-/-)^[1]
Dosage:	60 mg/kg
Administration:	P.o.; daily; for 3 days
Result:	Reduced plasma TG and cholesterol levels and decreased nonsignificant in circulating lipids.

Animal Model:	Male Wistar-Han rats^[1]
Dosage:	1 mg/kg
Administration:	I.v.
Result:	Showed moderate clearance and a short half-life with t_1/2=1.39 h.

Molecular Weight

536.05

Formula

C₂₃H₃₀ClN₇O₄S

CAS No.

1469284-79-4

Appearance

Solid

Color

White to yellow

SMILES

O=C([C@H]1CN(C2=CC=C3C(NC(C4(N5N=CC(Cl)=C5)CC4)=N3)=N2)CCC1)N6CCCC6.CS(=O)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL (466.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 50 mg/mL (93.27 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8655 mL	9.3275 mL	18.6550 mL
5 mM	0.3731 mL	1.8655 mL	3.7310 mL
10 mM	0.1865 mL	0.9327 mL	1.8655 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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* 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: ≥ 2.08 mg/mL (3.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (3.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (3.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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: Saline
Solubility: 50 mg/mL (93.27 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

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: 99.85%

Select Batch:

Data Sheet (278 KB) SDS (252 KB)

COA (254 KB) HNMR (148 KB) LCMS (107 KB)

Handling Instructions (2659 KB)

References

[1]. Futatsugi K, et al. Discovery and Optimization of Imidazopyridine-Based Inhibitors of Diacylglycerol Acyltransferase 2 (DGAT2). J Med Chem. 2015 Sep 24;58(18):7173-85. [Content Brief]

[2]. Pabst B, et al. Mechanistic Characterization of Long Residence Time Inhibitors of Diacylglycerol Acyltransferase 2 (DGAT2). Biochemistry. 2018 Dec 26;57(51):6997-7010. [Content Brief]

Complete Stock Solution Preparation Table

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

H₂O / DMSO	1 mM	1.8655 mL	9.3275 mL	18.6550 mL	46.6374 mL
	5 mM	0.3731 mL	1.8655 mL	3.7310 mL	9.3275 mL
	10 mM	0.1865 mL	0.9327 mL	1.8655 mL	4.6637 mL
	15 mM	0.1244 mL	0.6218 mL	1.2437 mL	3.1092 mL
	20 mM	0.0933 mL	0.4664 mL	0.9327 mL	2.3319 mL
	25 mM	0.0746 mL	0.3731 mL	0.7462 mL	1.8655 mL
	30 mM	0.0622 mL	0.3109 mL	0.6218 mL	1.5546 mL
	40 mM	0.0466 mL	0.2332 mL	0.4664 mL	1.1659 mL
	50 mM	0.0373 mL	0.1865 mL	0.3731 mL	0.9327 mL
	60 mM	0.0311 mL	0.1555 mL	0.3109 mL	0.7773 mL
	80 mM	0.0233 mL	0.1166 mL	0.2332 mL	0.5830 mL
DMSO	100 mM	0.0187 mL	0.0933 mL	0.1865 mL	0.4664 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.