PZ0299

PF-05175157

≥98% (HPLC)

• Synonym(s): 1,4-Dihydro-1′-[(2-methyl-1H-benzimidazol-6-yl)carbonyl]-1-(1-methylethyl)-spiro[5H-indazole-5,4′-piperidin]-7(6H)-one, 1-Isopropyl-1-(2-methyl-1H-benzo[d]imidazole-6-carbonyl)-1,4-dihydrospiro[indazole-5,4-piperidin]-7(6H)-one
• Empirical Formula (Hill Notation): C₂₃H₂₇N₅O₂
• CAS Number: 1301214-47-0
• Molecular Weight: 405.49
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 5 mg/mL, clear (warmed)
• storage temp.: room temp
• SMILES string: CC(C)N(N=C1)C2=C1CC3(CCN(C(C4=CC(NC(C)=N5)=C5C=C4)=O)CC3)CC2=O

Description

Application

PF-05175157 has been used as an acetyl-Coenzyme A carboxylase (ACC) inhibitor to study its effects on the infection of flavivirus.

Biochem/physiol Actions

PF-05175157 is a potent and selective inhibitor of both acetyl-CoA carboxylase isoform ACC1 located primarily in liver and adipose tissue and isoform ACC2 dominant in skeletal and heart muscle, with IC₅₀ values of 27 nM and 33 nM, respectively. Acetyl CoA carboxylase (ACC) generates malonyl CoA, which is a substrate for de novo lipogenesis and is also an inhibitor of mitochondrial fatty acid β-oxidation through inihbition of carnitine-palmitoyl transferase I (CPT-1), responsible for the transport of long-chain fatty acyl-CoAs across the mitochondrial membrane. ACC inihibitors are hoped to inhibit de novo lipogenesis and increase β-oxidation of long-chain fatty acids with potential for treatment of type 2 diabetes, hepatic steatosis, and cancer. In Phase I clinical studies for diabetes treatment, PF-05175157 inhibited de novo lipogenesis and increased net whole-body fatty acid utilization.

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable