1. Metabolic Enzyme/Protease
  2. Cytochrome P450
  3. Pradefovir mesylate

Pradefovir mesylate (Synonyms: Remofovir mesylate)

製品番号: HY-112690A 純度: 99.83%
取扱説明書

Pradefovir mesylate is a good substrate for liver CYP3A4. Pradefovir is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with a Km of 60 μM.

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Pradefovir mesylate 構造式

Pradefovir mesylate 構造式

CAS 番号 : 625095-61-6

容量 価格(税別) 在庫状況 数量
10 mM * 1 mL in DMSO USD 629 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 550 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 850 在庫あり
Estimated Time of Arrival: December 31
25 mg USD 1700 在庫あり
Estimated Time of Arrival: December 31
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製品説明

Pradefovir mesylate is a good substrate for liver CYP3A4. Pradefovir is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with a Km of 60 μM.

体外実験

Pradefovir is a cyclodiester prodrug of PMEA. It is one of the HepDirect prodrugs, which are designed to be efficiently and specifically activated through an oxidative reaction catalyzed by CYP3A4, which is located mainly in the liver. Pradefovir is converted to PMEA in human liver microsomes with a Km of 60 μM, a maximum rate of metabolism of 228 pmol/min/mg protein, and an intrinsic clearance of about 359 L/min[1].

体内実験

Daily oral dosing of Pradefovir (300 mg/kg) to rats for 8 days does not affect body weight; liver weight; liver weight-body weight ratio; liver microsomal protein content; total CYP content; enzyme activities for CYP1A, CYP2B, and CYP3A; and apoprotein contents for CYP1A1, CYP2B1/2, CYP3A1/2, and CYP4A1/3, indicating that Pradefovir is not a CYP inducer in rats[1].

臨床実験
分子量

519.90

分子式

C₁₈H₂₃ClN₅O₇PS

CAS 番号

625095-61-6

SMILES

NC1=C2N=CN(CCOC[[email protected]]3(OCC[[email protected]@H](C4=CC=CC(Cl)=C4)O3)=O)C2=NC=N1.CS(=O)(O)=O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

H2O : ≥ 125 mg/mL (240.43 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9234 mL 9.6172 mL 19.2345 mL
5 mM 0.3847 mL 1.9234 mL 3.8469 mL
10 mM 0.1923 mL 0.9617 mL 1.9234 mL
*Please refer to the solubility information to select the appropriate solvent.
参考文献
動物実験
[1]

Rats[1]
Five rats receive Pradefovir (300 mg/kg/day) orally for 8 days. At 24 h after administration of the last dose, the rats are killed and liver samples are collected. Body weight, liver weight, liver protein content, and liver microsomal P450 contents are determined. The apoprotein levels for CYP1A1, CYP2B1/2B2, CYP3A1/3A2, and CYP4A1/4A3 and the enzyme activities for CYP1A, CYP2B, and CYP3A are also determined by Western blot and LC analysis, respectively[1].

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参考文献
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Keywords:

PradefovirRemofovirCytochrome P450CYPsInhibitorinhibitorinhibit

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製品名:
Pradefovir mesylate
製品番号:
HY-112690A
数量:
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