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PF 06424439 - ≥98%(HPLC), high purity , CAS No.1469284-79-4

    Grade & Purity:
  • ≥98%(HPLC)
In stock
Item Number
P286969
Grouped product items
SKU Size
Availability
Price Qty
P286969-1mg
1mg
3
$48.90
P286969-5mg
5mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$68.90
P286969-10mg
10mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$117.90
P286969-25mg
25mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$246.90
P286969-50mg
50mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$439.90

Potent and selective DGAT2 inhibitor

Basic Description

Synonyms [(3R)-1-[2-[1-(4-Chloro-1H-pyrazol-1-yl)cyclopropyl]-3H-imidazo[4,5-b]pyridin-5-yl]-3-piperidinyl]-1-pyrrolidinylmethanone methanesulfonate | PF-06424439 methanesulfonate
Specifications & Purity ≥98%(HPLC)
Biochemical and Physiological Mechanisms Potent and selective DGAT2 inhibitor (IC50= 14 nM). Exhibits no significant activity at MGAT1-3 or DGAT1. Reduces triglyderide synthesis in human hepatocytesin vitro. Reduces plasma triglyceride and cholesterol levels in a rat dyslipidemia model. Orally b
Storage Temp Store at -20°C,Desiccated
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Product Description

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

to study its effects on HeLa cells

to study its inhibitory effects on neutral lipid synthesis in HT-1080 cells

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Organoheterocyclic compounds
Class Imidazopyridines
Subclass Not available
Intermediate Tree Nodes Not available
Direct Parent Imidazopyridines
Alternative Parents Piperidinecarboxamides  N-acylpyrrolidines  Dialkylarylamines  Aminopyridines and derivatives  Imidolactams  Aryl chlorides  Tertiary carboxylic acid amides  Sulfonyls  Pyrazoles  Organosulfonic acids  Alkanesulfonic acids  Methanesulfonates  Imidazoles  Heteroaromatic compounds  Azacyclic compounds  Carbonyl compounds  Hydrocarbon derivatives  Organic oxides  Organochlorides  
Molecular Framework Not available
Substituents Imidazopyridine - 3-piperidinecarboxamide - Piperidinecarboxamide - N-acylpyrrolidine - Dialkylarylamine - Aminopyridine - Aryl chloride - Aryl halide - Imidolactam - Piperidine - Pyridine - Azole - Imidazole - Methanesulfonate - Heteroaromatic compound - Alkanesulfonic acid - Tertiary carboxylic acid amide - Pyrazole - Sulfonyl - Pyrrolidine - Organic sulfonic acid or derivatives - Organosulfonic acid or derivatives - Organosulfonic acid - Carboxamide group - Azacycle - Carboxylic acid derivative - Organochloride - Organohalogen compound - Organic oxygen compound - Organonitrogen compound - Organooxygen compound - Organosulfur compound - Organic oxide - Amine - Carbonyl group - Organic nitrogen compound - Hydrocarbon derivative - Aromatic heteropolycyclic compound
Description This compound belongs to the class of organic compounds known as imidazopyridines. These are organic polycyclic compounds containing an imidazole ring fused to a pyridine ring. Imidazole is 5-membered ring consisting of three carbon atoms, and two nitrogen centers at the 1- and 3-positions. Pyridine is a 6-membered ring consisting of five carbon atoms and one nitrogen center.
External Descriptors Not available

Associated Targets(Human)

DGAT2 Tchem Diacylglycerol O-acyltransferase 2 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
CYP3A4 Tclin Cytochrome P450 3A4 (53859 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

Canis familiaris (36305 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

IUPAC Name [(3R)-1-[2-[1-(4-chloropyrazol-1-yl)cyclopropyl]-1H-imidazo[4,5-b]pyridin-5-yl]piperidin-3-yl]-pyrrolidin-1-ylmethanone;methanesulfonic acid
INCHI 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
InChIKey ZSTFDNQQOJUJFL-XFULWGLBSA-N
Smiles CS(=O)(=O)O.C1CCN(C1)C(=O)C2CCCN(C2)C3=NC4=C(C=C3)NC(=N4)C5(CC5)N6C=C(C=N6)Cl
Isomeric SMILES CS(=O)(=O)O.C1CCN(C1)C(=O)[C@@H]2CCCN(C2)C3=NC4=C(C=C3)NC(=N4)C5(CC5)N6C=C(C=N6)Cl
WGK Germany 3
PubChem CID 89854212
Molecular Weight 536.05

Certificates(CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Find and download the COA for your product by matching the lot number on the packaging.

5 results found

Lot Number Certificate Type Date Item
D2304287 Certificate of Analysis Nov 23, 2022 P286969
D2304279 Certificate of Analysis Nov 23, 2022 P286969
D2418083 Certificate of Analysis Nov 23, 2022 P286969
K2211795 Certificate of Analysis Oct 12, 2022 P286969
K2211783 Certificate of Analysis Oct 12, 2022 P286969

Chemical and Physical Properties

Solubility Solvent:water, Max Conc. mg/mL: 53.6, Max Conc. mM: 100; Solvent:DMSO, Max Conc. mg/mL: 53.6, Max Conc. mM: 100
Molecular Weight 536.000 g/mol
XLogP3
Hydrogen Bond Donor Count 2
Hydrogen Bond Acceptor Count 8
Rotatable Bond Count 4
Exact Mass 535.177 Da
Monoisotopic Mass 535.177 Da
Topological Polar Surface Area 146.000 Ų
Heavy Atom Count 36
Formal Charge 0
Complexity 777.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 1
Undefined Atom Stereocenter Count 0
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 2

Solution Calculators

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