(S)-PF-04445597
(S)-PF-04445597 is an orally active cholesteryl ester transfer protein (CETP) inhibitor with an IC50 of 0.07 μM. (S)-PF-04445597 inhibits CETP-mediated transfer of cholesteryl esters from HDL to non-HDL lipoproteins. (S)-PF-04445597 can be used for research on coronary heart disease.
For research use only. We do not sell to patients.
- CAS No.: 949099-81-4
- Formula: C29H31F9N6O2
- Molecular Weight:666.59
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
(S)-PF-04445597 (0-30 μM; 5-30 min) reversibly inhibits human CYP1A2 and CYP3A4 with IC50 values of 28.2 μM and 8.2 μM, respectively, and does not significantly inhibit CYP2C9, 2C19, and 2D6 in human liver microsomes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
| Species | Dose | Route | CLplasma | Vdss | AUC0-∞ | T1/2 | Cmax | Tmax | Bioavailability |
|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 1.0 mg/kg | i.v. | 8.6 mL/min/kg | 2.3 L/kg | 2040 ng·h/mL | 4.7 h | / | / | / |
| Cynomolgus Monkey[1] | 1.0 mg/kg | i.v. | 1.35 mL/min/kg | 0.64 L/kg | 13600 ng·h/mL | 4.9 h | / | / | / |
| Rat[1] | 6.0 mg/kg | p.o. | / | / | 5600.0 ng·h/mL | / | 830.0 ng/mL | 2.00 h | 62 % |
| Cynomolgus Monkey[1] | 6.0 mg/kg | p.o. | / | / | 43500 ng·h/mL | / | 2860 ng/mL | 2.70 h | 53 % |
Chemical Information
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CAS No. 949099-81-4
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Molecular Weight 666.59
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Formula C29H31F9N6O2
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SMILES
[C@H](C(C)C)(C1=C(CN(CC2=CC(C(F)(F)F)=CC(C(F)(F)F)=C2)C=3N=NN(C)N3)C=C(C(F)(F)F)C=C1)N4CCC(C(O)=O)CC4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Cardiovascular Diseases
Cardiovascular disease can be modeled as maladaptive cardiac remodeling, where ischemic injury or pressure overload activates inflammatory signaling, fibroblast activation, extracellular-matrix deposition, cardiomyocyte hypertrophy, vascular remodeling, and progressive ventricular dysfunction. The TGF-β/SMAD axis is a central profibrotic pathway after myocardial injury and pressure overload, while innate immune and cytokine pathways regulate leukocyte recruitment, scar formation, and adverse remodeling. Key unresolved questions include which inflammatory signals are reparative versus harmful, when fibrosis is protective versus maladaptive, and whether pathway inhibition improves function without weakening necessary infarct healing or compensatory remodeling.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
(S)-PF-04445597 Related Classifications
HY-136993 Related Classifications
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