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Description: Potent acetyl-CoA carboxylase (ACC) 1 and 2 inhibitor
Chemical Name: 1,4-Dihydro-1'-[2-methyl-1H-benzimidazol-6-yl)carbonyl]-1-(1-methylethyl)-spiro[5H-indazole-5,4'-piperidin]-7(6H)-one
Purity: ≥98% (HPLC)
Biological Activity for PF 05175157
PF 05175157 is an potent acetyl-CoA carboxylase (ACC) 2 and 1 inhibitor (IC50 values are 45 and 98 nM, respectively). Reduces hepatic and skeletal muscle malonyl-CoA levels in rats. Also inhibits hepatic de novo lipogenesis and reduces whole body respiratory exchange ratio in rats. Orally bioavailable.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Technical Data for PF 05175157
| M. Wt | 405.49 |
| Formula | C23H27N5O2 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1301214-47-0 |
| PubChem ID | 52934180 |
| InChI Key | BDXXSFOJPYSYOC-UHFFFAOYSA-N |
| Smiles | O=C(C4=CC=C(N=C(C)N5)C5=C4)N1CCC(CC(C=NN3C(C)C)=C3C(C2)=O)2CC1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for PF 05175157
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 20.27 | 50 | |
| ethanol | 8.11 | 20 |
Preparing Stock Solutions for PF 05175157
The following data is based on the product molecular weight 405.49. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 4.93 mL | 24.66 mL | 49.32 mL |
| 2.5 mM | 0.99 mL | 4.93 mL | 9.86 mL |
| 5 mM | 0.49 mL | 2.47 mL | 4.93 mL |
| 25 mM | 0.1 mL | 0.49 mL | 0.99 mL |
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Product Datasheets for PF 05175157
References for PF 05175157
References are publications that support the biological activity of the product.
Griffith et al (2014) Decreasing the rate of metabolic ketone reduction in the discovery of a clinical acetyl-CoA carboxylase inhibitor for the treatment of diabetes. J.Med.Chem. 57 10512 PMID: 25423286
If you know of a relevant reference for PF 05175157, please let us know.
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Keywords: PF 05175157, PF 05175157 supplier, PF05175157, Acetyl, CoA, carboxylase, 1, 2, inhibitors, inhibits, ACC1, ACC2, potent, orally, bioavailable, type, diabetes, mellitus, Other, Ligases, Lipid, Metabolism, 5790, Tocris Bioscience
1 Citation for PF 05175157
Citations are publications that use Tocris products. Selected citations for PF 05175157 include:
Lien et al (2021) Low glycaemic diets alter lipid metabolism to influence tumour growth. Nature 599 302 PMID: 34671163
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