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| SKU | Size | Availability |
Price | Qty |
|---|---|---|---|---|
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P286969-1mg
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1mg |
3
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$48.90
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P286969-5mg
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5mg |
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
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$68.90
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P286969-10mg
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10mg |
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
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$117.90
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P286969-25mg
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25mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
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$246.90
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P286969-50mg
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50mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
|
$439.90
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Potent and selective DGAT2 inhibitor
| 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 |
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 |
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| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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| 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 |
Find and download the COA for your product by matching the lot number on the packaging.
| Lot Number | Certificate Type | Date | Item |
|---|---|---|---|
| Certificate of Analysis | Nov 23, 2022 | P286969 | |
| Certificate of Analysis | Nov 23, 2022 | P286969 | |
| Certificate of Analysis | Nov 23, 2022 | P286969 | |
| Certificate of Analysis | Oct 12, 2022 | P286969 | |
| Certificate of Analysis | Oct 12, 2022 | P286969 |
| 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 |
Starting at $129.90