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PZ0233

Sigma-Aldrich

PF-06424439

≥98% (HPLC)

Synonym(s):

[(3R)-1-[2-[1-(4-Chloro-1H-pyrazol-1-yl)cyclopropyl]-3H-imidazo[4,5-b]pyridin-5-yl]-3-piperidinyl]-1-pyrrolidinyl-methanone methanesulfonate

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About This Item

Empirical Formula (Hill Notation):
C22H26ClN7O · CH3SO3H
CAS Number:
Molecular Weight:
536.05
UNSPSC Code:
12352200
PubChem Substance ID:

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Quality Level

assay

≥98% (HPLC)

form

powder

optical activity

[α]/D +7 to +11°, c = 1.0 in methanol

color

white to light brown

solubility

H2O: 10 mg/mL, clear

storage temp.

room temp

SMILES string

O=C([C@@H]1CCCN(C2=NC(NC(C3(CC3)N4N=CC(Cl)=C4)=N5)=C5C=C2)C1)N6CCCC6.CS(=O)(O)=O

InChI

1S/C22H26ClN7O.CH4O3S/c23-16-12-24-30(14-16)22(7-8-22)21-25-17-5-6-18(26-19(17)27-21)29-11-3-4-15(13-29)20(31)28-9-1-2-10-28;1-5(2,3)4/h5-6,12,14-15H,1-4,7-11,13H2,(H,25,26,27);1H3,(H,2,3,4)/t15-;/m1./s1

InChI key

ZSTFDNQQOJUJFL-XFULWGLBSA-N

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1 of 4

This Item
PZ0296PZ0300PZ0324
form

powder

form

powder

form

powder

form

powder

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

storage temp.

room temp

storage temp.

room temp

storage temp.

room temp

storage temp.

room temp

solubility

H2O: 10 mg/mL, clear

solubility

DMSO: 5 mg/mL, clear

solubility

DMSO: 20 mg/mL, clear

solubility

DMSO: 5 mg/mL, clear

color

white to light brown

color

white to beige

color

white to beige

color

white to beige

Application

PF-06424439 has been used as a diacylglycerol acyltransferase 2 (DGAT2) inhibitor:
  • to study its effects on cell mortality and lipid synthesis in epithelial colon cells and colorectal cancer stem cells[1]
  • to study its effects on HeLa cells[2]
  • to study its inhibitory effects on neutral lipid synthesis in HT-1080 cells[3]

Biochem/physiol Actions

PF-06424439 functions in reducing the hepatic lipid levels in dyslipidemic rats.[4]
PF-06424439 is a potent and selective inhibitor of diacylglycerol acyltransferase 2 (DGAT2).
PF-06424439 is a potent, selective DGAT2 inhibitor.

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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Questions

1–3 of 3 Questions  
  1. What is the storage temperature once reconstituted in water?

    1 answer
    1. The solution stability is not determined. However, the literature suggests that the material is stable in solution at -80°C is for approximately 6 months; and -20°C for approximately 1 month.

      Helpful?

  2. I need the pharmacokinetics and pharmacodynamic study of PF-06424439 product, what is the half life of this DGAT 2 inhibitor please.

    1 answer
    1. Unfortunately, pharmacokinetic, pharmacodynamic, and half-like information on this product are not available. The compound was developed by Pfizer, however, this product is intended for research use only. Some publications may be of interest.

      See the link below for one such article.
      https://pubs.acs.org/doi/10.1021/acs.jmedchem.5b01006#

      Helpful?

  3. Hi, I want to inquire that if the PF-06424439 product could be dissolved into DMSO? Thanks.

    1 answer
    1. The solubility of this compound is tested in water. The use of DMSO as a solvent has not been determined. However, external sources state that PF-06424439 can be solubilized in DMSO at approximately 50 mg/mL. This information has not been verified.

      Helpful?

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