1. Metabolic Enzyme/Protease
  2. Microsomal Triglyceride Transfer Protein (MTP)
  3. PF-02575799

PF-02575799 is a microsomal triglyceride transfer protein (MTP) inhibitor with an IC50 of 0.77±0.29 nM.

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

PF-02575799 Chemical Structure

PF-02575799 Chemical Structure

CAS No. : 863491-70-7

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Description

PF-02575799 is a microsomal triglyceride transfer protein (MTP) inhibitor with an IC50 of 0.77±0.29 nM.

IC50 & Target

IC50: 0.77±0.29 nM (MTP)[1]

Cellular Effect
Cell Line Type Value Description References
HepG2 IC50
0.77 nM
Compound: 13, PF-02575799
Inhibition of MTP in human HepG2 cells assessed as inhibition of apoB secretion after 40 hrs by ELISA
Inhibition of MTP in human HepG2 cells assessed as inhibition of apoB secretion after 40 hrs by ELISA
[PMID: 21684740]
HepG2 IC50
2 pM
Compound: 13, PF-02575799
Inhibition of MTP in human HepG2 cells assessed as unbound drug level causing inhibition of apoB secretion after 40 hrs by ELISA
Inhibition of MTP in human HepG2 cells assessed as unbound drug level causing inhibition of apoB secretion after 40 hrs by ELISA
[PMID: 21684740]
In Vitro

PF-02575799 is compound 13 from the reference[1].

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

In Vivo

PF-02575799 produces appreciable triglyceride effects at its minimally effective dose (10 mg/kg). PF-02575799 significant increase alanine transaminase at 100 mg/kg[1].

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

Molecular Weight

680.77

Formula

C42H37FN4O4

CAS No.
SMILES

O=C(C1=CC=C2N=C(NC(C3=CC=CC=C3C4=CC=C(OC(C)C)C=C4)=O)C=CC2=C1)N[C@@H](C5=CC=CC=C5)C(N(CC6=CC=C(F)C=C6)C)=O

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
References
Animal Administration
[1]

Rats[1]

Spray-dried dispersions formulated PF-02575799 is tested in a seven-day rat model. Food intake, body weight, liver TG, as well as serum alanine transaminase (ALT) are measured. In the definitive study, dose effect relationships are examined (PF-02575799 1, 3, 10, 30 and 100 mg/kg q.d.) and systemic exposures are measured[1].

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

References
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
PF-02575799
Cat. No.:
HY-100333
Quantity:
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