1. Anti-infection
    Metabolic Enzyme/Protease
  2. HCV
    HCV Protease
  3. Simeprevir

Simeprevir (Synonyms: TMC435)

製品番号: HY-10241 純度: 99.34%
取扱説明書

Simeprevir (TMC435) is an oral and potent HCV NS3/4A protease inhibitor with a Ki of 0.36 nM, and inhibits HCV replication with an EC50 of 7.8 nM.

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Simeprevir 構造式

Simeprevir 構造式

CAS 番号 : 923604-59-5

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
10 mM * 1 mL in DMSO USD 82 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 50 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 70 在庫あり
Estimated Time of Arrival: December 31
25 mg USD 100 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 150 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 250 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 30 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Simeprevir purchased from MCE. Usage Cited in: Int J Radiat Oncol Biol Phys. 2016 Nov 15;96(4):867-876.

    Simeprevir inhibits DNA damage repair following irradiation. U251, BT474, and HepG2 cells are pretreated with Simeprevir or DMSO and irradiated at a dose of 6 Gy. After 6 hours, prolongation of γH2AX foci is detected in Simeprevir-treated cells along with decreased phosphorylation of DNA-PKcs, indicating impaired nonhomologous end-joining repair.

    Simeprevir purchased from MCE. Usage Cited in: J Med Chem. 2016 Nov 23;59(22):10268-10284.

    Huh7.5 cells are infected with HCV (45 IU/cell) and simultaneously treated with Simeprevir (A, 0.025 μM), Sofosbuvir (B, 0.1 μM), or Daclatasvir (C, 16 pM) alone or with 1 (6.25 μM).

    Simeprevir purchased from MCE. Usage Cited in: Biomed Res Int. 2017;2017:1236801.

    Huh7.5 (HCV+) cells are treated with 1 μM of Simeprevir or solvent control. At 24 hours, the cells are washed and continuously incubated with fresh culture media containing drugs again for 48 hours. The cultural supernatants are then harvested and directly incubated to naïve Huh7.5 cells. After been passaged 1~3 times, the newly infected cells are treated with 1 μM of Simeprevir for 72 hours. Intracellular proteins are extracted and detected with WB.

    Simeprevir purchased from MCE. Usage Cited in: Eur J Med Chem. 2018 Jan 1;143:1053-1065.

    Huh7.5 cells are infected with HCV and simultaneously treated with 7f (10 μM) or DAA (0.04 μM Simeprevir, 0.08 μM Sofosbuvir, or 16 pM Daclatasvir) or 7f plus DAA.

    Simeprevir purchased from MCE. Usage Cited in: College of Medicine/School of Medicine. Seoul National University. 2016 Aug.

    Pharmacologic inhibition of PI4KIIIα using Simeprevir increases the radiosensitivity in U251 cells.
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    製品説明

    Simeprevir (TMC435) is an oral and potent HCV NS3/4A protease inhibitor with a Ki of 0.36 nM, and inhibits HCV replication with an EC50 of 7.8 nM[1].

    IC50 & Target

    Ki: 0.36 nM (HCV NS3/4A protease)[1]
    EC50: 7.8 nM (HCV replication)[1]

    体外実験

    In Huh7-Luc cells, antiviral activity of simeprevir (TMC435) is dose dependent, and the EC50 and EC90 values determined for simeprevir (TMC435) are 8 nM and 24 nM, respectively[2].
    simeprevir (TMC435) inhibits NS3/4A proteases from HCV genotypes 1 to 6 with IC50s of 1/0.9/7/30/1.5/2.2/1.6 nM for 1a/1b/2b/3a/4/5/6, respectively[3].

    体内実験

    Simeprevir (TMC435) has moderate terminal elimination half-life (t1/2=1.5 h and 4.1 h for rat (3 mg/kg, p.o.), monkey (3 mg/kg, p.o.))[3].

    Animal Model: Sprague-Dawley (SD) rats and cynomolgus monkeys[3]
    Dosage: 3 mg/kg
    Administration: Oral administration
    Result: Time at which peak concentration (Tmax) of 1 hour and 2 hour for rat and monkey, respectively.
    Concentration at 24 h after dosing (C24 h) of 0.9 and 2.3 ng/mL for rat and monkey, respectively.
    AUC0-24h=1173 and1409 ng • h/mL for rat and monkey, respectively.
    臨床実験
    分子量

    749.94

    分子式

    C₃₈H₄₇N₅O₇S₂

    CAS 番号

    923604-59-5

    SMILES

    COC1=C(C)C2=C(C(O[[email protected]]3C[[email protected]@H](C(N(C)CCCC/C=C\[[email protected]](C4)[[email protected]]4(C(NS(=O)(C5CC5)=O)=O)N6)=O)[[email protected]](C6=O)C3)=CC(C7=NC(C(C)C)=CS7)=N2)C=C1

    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: 

    DMSO : 14.29 mg/mL (19.05 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.3334 mL 6.6672 mL 13.3344 mL
    5 mM 0.2667 mL 1.3334 mL 2.6669 mL
    10 mM 0.1333 mL 0.6667 mL 1.3334 mL
    *Please refer to the solubility information to select the appropriate solvent.
    体内:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 1.43 mg/mL (1.91 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 1.43 mg/mL (1.91 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    参考文献
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    Keywords:

    SimeprevirTMC435TMC 435TMC-435HCVHCV ProteaseHepatitis C virusInhibitorinhibitorinhibit

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    製品名:
    Simeprevir
    製品番号:
    HY-10241
    数量:
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