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Cat. No.: HY-11088

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PF-3052334

PF-3052334 is an orally active, hepatically selective HMG-CoA reductase inhibitor with an IC₅₀ of 1.9 nM. PF-3052334 inhibits cholesterol synthesis, with IC₅₀ values of 0.9 and 730 nM in hepatocytes and muscle cells, respectively. PF-3052334 can be used to study hypercholesterolemia.

For research use only. We do not sell to patients.

CAS No.: 887702-61-6
Formula: C₂₈H₃₃FN₃NaO₅
Molecular Weight:533.57

Storage:

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

Data Sheet (271 KB)

PF-3052334 Chemical Structure

CAS No.: 887702-61-6

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Use of MCE Products

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

Biological Activity
- Description
- Cellular Effect
- In Vivo
Chemical Information
Protocols (1)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Cellular Effect

Cell Line	Type	Value	Description	References
Hepatocyte	IC₅₀	0.9 nM Compound: 35, PF-3052334	Inhibition of cholesterol synthesis in rat hepatocytes Inhibition of cholesterol synthesis in rat hepatocytes	[PMID: 18072721]
L6	IC₅₀	730 nM Compound: 35, PF-3052334	Inhibition of cholesterol synthesis in rat L6 cells Inhibition of cholesterol synthesis in rat L6 cells	[PMID: 18072721]

In Vivo

PF-3052334 (10 mg/kg, p.o., single dose) PF-3052334 significantly inhibits cholesterol synthesis at both 2-4 h and 4-6 h in hamsters^[1].
PF-3052334 (20 mg/kg, p.o., once daily for 7 days) causes low density lipoprotein (LDL) reduction in guinea pigs with an ED₅₀ of 3.6 mg/kg^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Acute cholesterol synthesis inhibition model established in Male Syrian hamster (Golden hamster)^[1]
Dosage:

10 mg/kg
Administration:

Oral administration (p.o.), single dose
Result:

Significantly inhibited cholesterol synthesis at both 2-4 h and 4-6 h.

Animal Model:

Chronic LDL-C reduction experiment established in male Hartley guinea pig^[1]
Dosage:

20 mg/kg
Administration:

Oral administration (p.o.), once daily for 7 days
Result:

Reduced LDL-C by 45%

Chemical Information

CAS No. 887702-61-6
Molecular Weight 533.57
Formula C₂₈H₃₃FN₃NaO₅
SMILES

O=C(O[Na])C[C@H](O)C[C@H](O)CCC1=C(C(C)C)C(C(NCC2=CC=C(C=C2)C)=O)=NN1C3=CC=C(C=C3)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Protocols

All Cell Biology

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.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Pfefferkorn JA, et al. Substituted Pyrazoles as Hepatoselective HMG-CoA Reductase Inhibitors: Discovery of (3 R, 5 R)-7-[2-(4-Fluoro-phenyl)-4-isopropyl-5-(4-methyl-benzylcarbamoyl)-2 H-pyrazol-3-yl]-3, 5-dihydroxyheptanoic Acid (PF-3052334) as a Candidate for the Treatment of Hypercholesterolemia. Journal of medicinal chemistry. 2008 Jan 10;51(1):31-45.

Calculators

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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.

Bioz

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MOQ

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100 mg

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