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

MTP-IN-1是微粒体甘油三酯转移蛋白 (microsomal triglyceride transfer protein (MTP)) 抑制剂,IC50 值为0.77±0.29 nM。

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PF-02575799 Chemical Structure

PF-02575799 Chemical Structure

CAS No. : 863491-70-7

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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

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]

细胞效力
(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]
体外研究
(In Vitro)

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

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

体内研究
(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].

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

分子量

680.77

Formula

C42H37FN4O4

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
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.

参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • 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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产品名称:
PF-02575799
目录号:
HY-100333
需求量: