PF 429242 dihydrochloride
Tocris Bioscience, part of Bio-Techne | Catalog # 3354
Competitive inhibitor of SREBP site 1 protease
Key Product Details
Description
Competitive inhibitor of SREBP site 1 protease
Product Description
PF 429242 dihydrochloride is a reversible, competitive inhibitor of sterol regulatory element-binding protein (SREBP) site 1 protease (IC50 = 0.175 μM). Selective for site 1 protease against a panel of serine proteases. Inhibits rate of cholesterol synthesis in CHO cells (IC50 = 0.53 μM). Also displays antiviral activity. Cell permeable.Licensing Information
Sold for research purposes under agreement from Pfizer Inc.Product Specifications
Molecular Weight
482.49
Formula
C25H35N3O2.2HCl
Storage
Desiccate at RT
Purity
≥97% (HPLC)
Chemical Name
4-[(Diethylamino)methyl]-N-[2-(2-methoxyphenyl)ethyl]-N-(3R)-3-pyrrolidinylbenzamide dihydrochloride
CAS Number
2248666-66-0
PubChem ID
90488837
InChI Key
GSUZWFZKTIOWTI-MQWQBNKOSA-N
SMILES
O=C(C2=CC=C(CN(CC)CC)C=C2)N(CCC3=CC=CC=C3OC)[C@@H]1CCNC1.Cl.Cl
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 24.12 | 50 | |
| DMSO | 24.12 | 50 |
Preparing Stock Solutions
for PF 429242 dihydrochloride
The following data is based on the product molecular weight 482.49
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 4.15 mL | 20.73 mL | 41.45 mL |
| 2.5 mM | 0.83 mL | 4.15 mL | 8.29 mL |
| 5 mM | 0.41 mL | 2.07 mL | 4.15 mL |
| 25 mM | 0.08 mL | 0.41 mL | 0.83 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Olmstead Human subtilase SKI-1/S1P is a master regulator of the HCV lifecycle and a potential host cell target for developing indirect-acting antiviral agents. PLoS.Pathog. 2012 PMID: 22241994
- Hawkins Pharmacologic inhibition of site 1 protease activity inhibits sterol regulatory element-binding protein processing and reduces lipogenic enzyme gene expression and lipid synthesis in cultured cells and experimental animals. J.Pharmacol.Exp.Ther. 2008 PMID: 18577702
- Urata Antiviral activity of a small-molecule inhibitor of arenavirus glycoprotein processing by the cellular site 1 protease. J.Virol. 2011 PMID: 21068251
- Hay Aminopyrrolidineamide inhibitors of site-1 protease. Bioorg.Med.Chem.Lett. 2007 PMID: 17583500
Product Specific Notices for PF 429242 dihydrochloride
For research use only
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