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Cat. No.: HY-136993

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(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

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

(S)-PF-04445597 Chemical Structure

CAS No.: 949099-81-4

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- Parmacokinetics
Chemical Information
Purity & Documentation
References
Calculators
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Biological Activity

Description

All Cytochrome P450 Isoforms :

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.

Related Protocols :

Research Protocol for Cardiovascular Diseases

Parmacokinetics

Species	Dose	Route	CL_plasma	V_dss	AUC_0-∞	T_1/2	C_max	T_max	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

CAS No. 949099-81-4
Molecular Weight 666.59
Formula C₂₉H₃₁F₉N₆O₂
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Kalgutkar AS, et al. Identification of a novel, non-tetrahydroquinoline variant of the cholesteryl ester transfer protein (CETP) inhibitor torcetrapib, with improved aqueous solubility. Xenobiotica; the fate of foreign compounds in biological systems. 2014 Jul;44(7):591-605.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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