PF 06424439

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Cat.No. 6348 - PF 06424439 | C22H26ClN7O.CH4O3S | CAS No. 1469284-79-4
Description: Potent and selective DGAT2 inhibitor
Chemical Name: [(3R)-1-[2-[1-(4-Chloro-1H-pyrazol-1-yl)cyclopropyl]-3H-imidazo[4,5-b]pyridin-5-yl]-3-piperidinyl]-1-pyrrolidinylmethanone methanesulfonate
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

Potent and selective DGAT2 inhibitor (IC50 = 14 nM). Exhibits no significant activity at MGAT1-3 or DGAT1. Reduces triglyderide synthesis in human hepatocytes in vitro. Reduces plasma triglyceride and cholesterol levels in a rat dyslipidemia model. Orally bioavailable.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data

M. Wt 536.05
Formula C22H26ClN7O.CH4O3S
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 1469284-79-4
PubChem ID 89854212
InChI Key ZSTFDNQQOJUJFL-XFULWGLBSA-N
Smiles ClC(C=N1)=CN1C2(CC2)C3=NC4=CC=C(N5C[C@H](C(N6CCCC6)=O)CCC5)N=C4N3.O=S(C)(O)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 53.6 100
DMSO 53.6 100

Preparing Stock Solutions

The following data is based on the product molecular weight 536.05. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.87 mL 9.33 mL 18.65 mL
5 mM 0.37 mL 1.87 mL 3.73 mL
10 mM 0.19 mL 0.93 mL 1.87 mL
50 mM 0.04 mL 0.19 mL 0.37 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the biological activity of the product.

Futatsugi et al (2015) Discovery and optimization of imidazopyridine-based inhibitors of diacylglycerol acyltransferase 2 (DGAT2). J.Med.Chem. 58 7173 PMID: 26349027


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Keywords: PF 06424439, PF 06424439 supplier, PF06424439, diacylglyercol, O-Acyltransferases, DGAT2, inhibitors, inhibits, potent, selective, orally, bioavailable, dyslipidemia, Diacylglycerol, O-Acyltransferase, 6348, Tocris Bioscience

Citations for PF 06424439

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Literature in this Area

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