2. Metabolic Enzyme/Protease
  3. Acyltransferase
  4. PF-06424439 methanesulfonate

PF-06424439 methanesulfonate 

Cat. No.: HY-108341A Purity: 99.92%
COA Handling Instructions

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

PF-06424439 methanesulfonate Chemical Structure

CAS No. : 1469284-79-4

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 83 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 83 In-stock
Solid
1 mg USD 50 In-stock
5 mg USD 70 In-stock
10 mg USD 120 In-stock
25 mg USD 250 In-stock
50 mg USD 400 In-stock
100 mg USD 650 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of PF-06424439 methanesulfonate:

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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 (Vdss) results in a short half-life[1].

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 t1/2=1.39 h.
Molecular Weight

536.05

Appearance

Solid

Formula

C23H30ClN7O4S
CAS No.
SMILES

O=C([[email protected]]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, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (466.37 mM; Need ultrasonic)

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

  • 2.

    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

  • 3.

    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

  • 4.

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

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

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.92%

COA (253 KB) LCMS (267 KB)

Handling Instructions (2659 KB)
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Keywords:

PF-064244391469284-79-4PF06424439PF 06424439AcyltransferaseDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseInhibitorinhibitorinhibit

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