PF-06424439 (methanesulfonate)

Name: PF-06424439 methanesulfonate
Brand: MedChemExpress
SKU: HY-108341A
Rating: 5.0 (25 reviews)

製品番号: HY-108341A 純度: 99.93%: Data Sheet SDS COA 取扱説明書
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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.

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CAS 番号 : 1469284-79-4

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 83	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 83	在庫あり	Estimated Time of Arrival: December 31
Solid
1 mg	$50	在庫あり	Estimated Time of Arrival: December 31
5 mg	$70	在庫あり	Estimated Time of Arrival: December 31
10 mg	$120	在庫あり	Estimated Time of Arrival: December 31
25 mg	$250	在庫あり	Estimated Time of Arrival: December 31
50 mg	$400	在庫あり	Estimated Time of Arrival: December 31
100 mg	$650	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 25 publication(s) in Google Scholar

Other Forms of PF-06424439 methanesulfonate:

PF-06424439 在庫あり
PF-06424439 methanesulfonate (Standard) お問い合わせ

顧客検証

RT-PCR

Cell Imaging/Staining

Cell Proliferation/Viability Assay

: PF-06424439 methanesulfonate purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2026 Feb 9;44(2):383-404.e18. [Abstract]; Cells derived from in vivo PDX models were treated in vitro with DGAT2 inhibitor (DGAT2i, PF-06424439 methanesulfonate, 10μM) for 48 hours and cellular viability was measured by CellTiter-Glo assay.

: PF-06424439 methanesulfonate purchased from MedChemExpress. Usage Cited in: FASEB J. 2025 Nov 30;39(22):e71249. [Abstract]; Lipid droplet accumulation was detected using Oil Red O staining. Oil Red O staining revealed that HILPDA overexpression boosted lipid droplet content in the cells, an effect that was attenuated by treatment with DGAT1 and DGAT2 inhibitors (PF‑06424439).

: PF-06424439 methanesulfonate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Sep 27;15(1):8273. [Abstract]; Immunofluorescence images of HAECs treated with DMSO or DGAT inhibitors (A922500, 10 µM and PF-06424439, 5 µM) for 24 h, exposed to bovine serum albumin (BSA) or OA for 12 h, and then serum-starved for 48 h (n = 20 fields from 3 independent experiments). 200 µM OA was used to stimulate LD formation. BSA was used as a control treatment. Scale bar, 20 µm.

: PF-06424439 methanesulfonate purchased from MedChemExpress. Usage Cited in: Mol Metab. 2024 Jun:84:101953. [Abstract]; PF-06424439 methanesulfonate (10-20 μM; 24 or 48 h) inhibited the accumulation of lipid droplets during an induced ESC decidual process.

: PF-06424439 methanesulfonate purchased from MedChemExpress. Usage Cited in: J Dairy Sci. 2022 Apr;105(4):3588-3600. [Abstract]; The effect of DGAT1 and DGAT2 inhibitor on lipid synthesis in calf primary hepatocytes. Treatments were a control group (cells cultured in RPMI-1640 basic medium for 12 h), 1.2 mM fatty acids (cells treated with 1.2 mM fatty acids for 12 h), DGAT1 inhibitor (cells treated with 0.3 μM DGAT1 inhibitor 2 for 12 h), DGAT1 inhibitor + 1.2 mM fatty acids (cells treated with 0.3 μM DGAT1 inhibitor and 1.2 mM fatty acids for 12 h), DGAT2 inhibitor (cells treated with 0.3 μM PF-06424439 methanesulfonate (DGAT2 inhibitor) for 12 h), DGAT2 inhibitor + 1.2 mM fatty acids (cells treated with 0.3 μM PF-06424439 methanesulfonate and 1.2 mM fatty acids for 12 h). Representative western blots of SREBF1, FASN, DGAT1, DGAT2, MTTP, and APOB.

: PF-06424439 methanesulfonate purchased from MedChemExpress. Usage Cited in: J Dairy Sci. 2022 Apr;105(4):3588-3600. [Abstract]; The effect of the DGAT1 and DGAT2 inhibitors on immunofluorescence of lipid droplets in calf primary hepatocytes. Treatments were control group (cells cultured in RPMI-1640 basic medium for 12 h), 1.2 mM fatty acids (cells treated with 1.2 mM fatty acids for 12 h), DGAT1 inhibitor (cells treated with 0.3 μM DGAT1 inhibitor 2 for 12 h), DGAT1 inhibitor + 1.2 mM fatty acids (cells treated with 0.3 μM DGAT1 inhibitor 2 and 1.2 mM fatty acids for 12 h), DGAT2 inhibitor (cells treated with 0.3 μM PF-06424439 methanesulfonate (DGAT2i) for 12 h), and DGAT2 inhibitor + 1.2 mM fatty acids (cells treated with 0.3 μM PF-06424439 methanesulfonate and 1.2 mM fatty acids for 12 h).

: PF-06424439 methanesulfonate purchased from MedChemExpress. Usage Cited in: J Virol. 2022 Jan 26;96(2):e0147321. [Abstract]; N2a cells were incubated with DGAT1 inhibitor (DGAT1i) (A922500, 10 μg/mL), DGAT2i (PF-06424439 methanesulfonate, 40 μg/mL), or a combination (A922500 plus PF-06424439 methanesulfonate) for 48 h, and cell viability was assessed by a Cell Counting kit-8 (CCK-8) assay (n = 3).

: PF-06424439 methanesulfonate purchased from MedChemExpress. Usage Cited in: Dev Comp Immunol. 2021 Nov:124:104197. [Abstract]; After preincubation with 30 μM DGAT1 inhibitor or 40 μM DGAT2 inhibitor (PF-06424439) for 1 h, CIK cells were treated with 3 μM Gardiquimod for 24 h. mRNA expression of DGAT1 and DGAT2 in CIK cells.

Acyltransferase アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

ACAT1 ACAT2 MGAT2 ACAT DGAT1 DGAT2

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

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]

体内実験

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.

分子量

536.05

分子式

C₂₃H₃₀ClN₇O₄S

CAS 番号

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, sealed storage, away from moisture

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

溶剤 & 溶解度

体外:

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)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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).

純度とドキュメンテーション

純度: 99.93%

Select Batch:

データシート (279 KB) SDS (252 KB)

COA (254 KB) HNMR (148 KB) RP-HPLC (260 KB) MS (69 KB)

取扱説明書 (2659 KB)

参考文献

[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.