2. Anti-infection
  3. HCV
  4. Amphihevir

Amphihevir 是一种具有口服活性的 HCV NS4B 抑制剂。Amphihevir 对 HCV 1a 和 1b 基因型复制子具有活性，可降低 HCV RNA 水平。Amphihevir 可用于慢性丙型肝炎的研究。

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Amphihevir

Amphihevir Chemical Structure

CAS No. : 1890171-61-5

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Amphihevir 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Amphihevir is an orally active HCV NS4B inhibitor. Amphihevir exhibits activity against HCV genotype 1a and 1b replicons and reduces HCV RNA levels. Amphihevir can be used in the research of chronic hepatitis C[1].

体外研究
(In Vitro)

Amphihevir 可强效抑制 HCV GT1a (H77) 复制子细胞，EC50 为 0.34 nM；抑制 HCV GT1b (Con1) 复制子细胞的 EC50 值分别为 1.97 nM (荧光素酶法) 和 1.12 nM (qRT-PCR 法)；还可中度抑制 HCV GT2a (JFH-1) HCVcc，EC50 为 186 nM；且随着人血清浓度的升高，其抗病毒活性会降低[1]。
Amphihevir (12-300 nM; 9 h) 可抑制 HCV GT1b (Con1) 复制子稳定细胞的 RNA 复制[1]。
Amphihevir 在 HCV GT1b (Con1) 复制子细胞中与其他直接作用抗病毒药物表现出相加至高度协同的抗 HCV 作用[1]。

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

Amphihevir 相关抗体:

Real Time qPCR[1]

Cell Line: HCV genotype 1b (Con1) replicon stable cells
Concentration: 12 nM, 60 nM, 300 nM
Incubation Time: 9 h
Result: Caused a continuous, concentration-dependent decline in HCV-1b replicon RNA over 9 days, with no RNA rebound observed.
Reduced replicon RNA by nearly 6,300-fold (3.8 Log10) at 300 nM (25× EC90).
药代动力学
(Parmacokinetics)
Species Dose Route C0 T1/2 Vdss CL AUC0-last AUC0-inf Cmax Tmax MRT0-last MRT0-inf Bioavailability
Rat[1] 1 mg/kg i.v. 673 ng/mL 1.15 h 1.67 L/kg 17.8 mL/min/kg 959 ng·h/mL 965 ng·h/mL / / / / /
Rat[1] 3 mg/kg p.o. / 2.74 h / / 1610 ng·h/mL 1630 ng·h/mL 311 ng/mL 2.00 h / / 65.1 %
Rat[1] 10 mg/kg p.o. / 4.16 h / / 3820 ng·h/mL 3900 ng·h/mL 507 ng/mL 1.50 h / / 40.1 %
Rat[1] 10 mg/kg p.o. / 4.7 h / / 3205 ng·h/mL 3510 ng·h/mL 345 ng/mL 3.84 h / / /
Rat[1] 30 mg/kg p.o. / 8.98 h / / 10600 ng·h/mL 12700 ng·h/mL 899 ng/mL 2.67 h / / 43.1 %
Dog[1] 1 mg/kg i.v. 555 ng/mL 4.45 h 2.30 L/kg 9.30 mL/min/kg 1880 ng·h/mL 1930 ng·h/mL / / / / /
Dog[1] 3 mg/kg p.o. / 4.38 h / / 758 ng·h/mL 787 ng·h/mL 145 ng/mL 1.25 h 5.33 h 6.18 h 13.8 %
Dog[1] 10 mg/kg p.o. / 4.72 h / / 3520 ng·h/mL 4260 ng·h/mL 438 ng/mL 1.50 h 7.61 h 10.7 h 18.5 %
Dog[1] 10 mg/kg p.o. / 4.51 h / / 2560 ng·h/mL 2880 ng·h/mL 371 ng/mL 1.50 h 7.19 h 9.27 h 13.3 %
Dog[1] 30 mg/kg p.o. / 11.3 h / / 7150 ng·h/mL 10400 ng·h/mL 681 ng/mL 1.33 h 8.17 h 16.8 h 12.6 %
体内研究
(In Vivo)

Amphihevir (1-200 mg/kg；静脉注射；口服；单次/每日；1-4 周) 在 SD 大鼠、Beagle 犬中表现出中等至良好的口服吸收性，重复给药后无明显药物蓄积[1]。

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

Animal Model: Sprague-Dawley (SD) rats (male and female)[1]
Dosage: 1; 3; 10 ; 20 ; 60 ; 200 mg/kg
Administration: i.v.; single dose; p.o.; single dose; p.o.; daily; 7 days; p.o.; daily; 4 weeks
Result: Exhibited moderate to favorable oral absorption.
分子量

448.40

Formula

C21H19F3N4O4
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

Amphihevir 相关分类

  • 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 *
= × ×

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.

Keywords:

Amphihevir1890171-61-5HCVHepatitis C virushuman-derived cell linesNS5B inhibitorsHepatitis C virus NS4BBeagle dogsSD ratsNS5A inhibitorsHepatitis C viral RNAHepatitis C virus genotype 1aHepatitis C virus genotype 1bNS3/4A inhibitorsInhibitorinhibitorinhibit

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