PF 05175157
PF 05175157 Basic information
- Product Name:
- PF 05175157
- Synonyms:
-
- 1-isopropyl-1'-(2-methyl-1H-benzo[d]imidazole-5-carbonyl)-4,6-dihydrospiro[indazole-5,4'-piperidin]-7(1H)-one
- 1,4-Dihydro-1'-[2-methyl-1H-benzimidazol-6-yl)carbonyl]-1-(1-methylethyl)-spiro[5H-indazole-5,4'-piperidin]-7(6H)-one
- CS-2573
- PF 05175157;PF-05175157
- PF 05175157
- Spiro[5H-indazole-5,4'-piperidin]-7(6H)-one,1,4-dihydro-1'-[(2-methyl-1H-benzimidazol-6-yl)carbonyl]-1-(1-methylethyl)-
- PF-05175157 >=98% (HPLC)
- 1'-(2-methyl-1H-1,3-benzodiazole-6-carbonyl)-1-(pr opan-2-yl)-1,4,6,7-tetrahydrospiro[indazole-5,4'-pi peridin]-7-one
- CAS:
- 1301214-47-0
- MF:
- C23H27N5O2
- MW:
- 405.49
- Product Categories:
-
- API
- Mol File:
- 1301214-47-0.mol
PF 05175157 Chemical Properties
- Boiling point:
- 692.0±55.0 °C(Predicted)
- Density
- 1.38±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:20.0(Max Conc. mg/mL);49.38(Max Conc. mM)
- form
- A crystalline solid
- pka
- 11.47±0.10(Predicted)
- color
- White to off-white
PF 05175157 Usage And Synthesis
Uses
PF-05175157 has been used as an acetyl-Coenzyme A carboxylase (ACC) inhibitor to study its effects on the infection of flavivirus.
Biological Activity
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.
in vivo
Oral administration (3 mg/kg) to rats and dogs show bioavailability of 40% and 54%, respectively, consistent with the low microsomal clearance and good solubility at low pH. Formation of the direct product of ACC, malonyl-CoA, in the skeletal muscle and liver of lean rats is assessed 1 h following an acute oral dose of PF-05175157, showing concentration-dependent reductions in both skeletal muscle and liver malonyl-CoA. At the nadir, quadriceps and liver malonyl-CoA levels are reduced by 76% and 89%, respectively. The EC50s for inhibition of quadriceps and liver malonyl-CoA are 870 and 540 nM, respectively, determined from unbind plasma concentrations of PF-05175157. Acute oral administration of PF-05175157 inhibits hepatic DNL in rats in an unbind plasma drug concentration-dependent manner. PF-05175157 inhibits up to 82% of the incorporation of [14C]acetate into [14C]lipids with an EC50 of 326 nM[1].
storage
Store at +4°C
PF 05175157Supplier
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- +86-21-20908456
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- 021-58955995
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- 025-846993838003-8003 18013301590
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- 020-39119399 18927568969
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- Tel
- 18149758185
- sales-cpd@caerulumpharma.com
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