2. Anti-infection
  3. HCV
  4. HCV-IN-38

HCV-IN-38 是一种有效、具有选择性与口服活性的丙型肝炎病毒 (HCV) 抑制剂 (EC50=15 nM, SI=431)。HCV-IN-38 有较高的抗 HCV 活性和较低的细胞毒性。HCV-IN-38 具有良好的安全性和口服药代动力学。

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HCV-IN-38 Chemical Structure

HCV-IN-38 Chemical Structure

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HCV-IN-38 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

HCV-IN-38 is a potent, selective and orally active HCV inhibitor (EC50=15 nM, SI=431). HCV-IN-38 has high anti-HCV activity and low cytotoxicity. HCV-IN-38 has a good safety and oral pharmacokinetic profile[1].

IC50 & Target

EC50: 15 nM (HCV) in Huh7.5 cells[1]
体外研究
(In Vitro)

HCV-IN-38 (compound 80) (0-20 μM; 72 hours) exhibits high anti-HCV activity with EC50=15 nM and low cytotoxicity with CC50=6.47 μM in Huh7.5 cells[1].
HCV-IN-38 (2 μM; 2 hours) has moderate permeability (0.5 < Papp < 2.5 (×10-6 cm/s))[1].

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

HCV-IN-38 相关抗体:

Cell Cytotoxicity Assay

Cell Line: Huh7.5 cells[1]
Concentration: 0-20 μM
Incubation Time: 72 hours
Result: Exhibited low cytotoxicity with CC50=6.47 μM.
体内研究
(In Vivo)

HCV-IN-38 (2 μM; 4 hours) has decent plasma stability (t1/2, rat=16.9 h and t1/2, human=19.9 h)[1].
HCV-IN-38 (2 mg/kg for i.p., 10 mg/kg for p.o., single) exhibits satisfying PK properties with an oral total exposure (AUC) of 1502 ng h/mL, medium in vivo clearance (38.3 mL/min/kg), Cmax of 452 ng/mL, and moderate bioavailability of 34%[1].
HCV-IN-38 (50-200 mg/kg; i.p., single) has modest safety profiles with LD50 values higher than 150 mg/kg[1].
Pharmacokinetic Parameters of HCV-IN-38 in Sprague-Dawley rats[1].

IV (2 mg/kg) PO (10 mg/kg)
AUC0-last (ng·h/mL) 889 ± 179 1502 ± 342
AUC0-inf (ng·h/mL) 898 ± 184 1525 ± 360
MRT0-last (h) 1.36 ± 0.182 2.95 ± 0.276
MRT0-inf (h) 1.45 ± 0.211 3.10 ± 0.290
Cmax (ng/mL) 452 ± 149
T1/2 (h) 1.24 ± 0.101 1.90 ± 0.492
Tlast (h) 8.00 12.0
Tmax (h) 1.00
Vdss (L/kg) 3.26 ± 0.426
Cl (mL/min/kg) 38.3 ± 8.89
F (%) 34

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

Animal Model: SD rats (180-220 g, n=3)[1]
Dosage: 2 or 10 mg/kg
Administration: i.v. and p.o., single (Pharmacokinetic Analysis)
Result: Exhibited satisfying PK properties with an oral total exposure (AUC) of 1502 ng h/mL, medium in vivo clearance (38.3 mL/min/kg), Cmax of 452 ng/mL, and moderate bioavailability of 34%.
Animal Model: Kunming mice (n=6)[1]
Dosage: 50, 100, 150, and 200 mg/kg
Administration: i.p., single
Result: Demonstrated modest safety profiles with LD50 values higher than 150 mg/kg.
分子量

500.90

Formula

C22H24ClF3N4O4
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

HCV-IN-38 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:

HCV-IN-38HCVHepatitis C virusBiaryl amideOralSelectivityHuh7.5 cellsSD ratsInhibitorinhibitorinhibit

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