1. Anti-infection
  2. HCV
  3. Daclatasvir dihydrochloride

Daclatasvir dihydrochloride  (Synonyms: 盐酸达拉他韦; BMS-790052 dihydrochloride; EBP 883 dihydrochloride)

目录号: HY-10465 纯度: 99.68%
COA 产品使用指南

Daclatasvir dihydrochloride (BMS-790052 dihydrochloride) 是一种有效的具有口服活性的 HCV NS5A 蛋白抑制剂,多种 HCV 复制子基因型的 EC50 范围为 9-146 pM。Daclatasvir dihydrochloride 也是有机阴离子转运多肽 1B (OATP1B) 和 OATP1B3 抑制剂,IC50 分别为 1.5 µM 和 3.27 µM。

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Daclatasvir dihydrochloride Chemical Structure

Daclatasvir dihydrochloride Chemical Structure

CAS No. : 1009119-65-6

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10 mM * 1 mL in DMSO ¥500
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Customer Review

Other Forms of Daclatasvir dihydrochloride:

MCE 顾客使用本产品发表的 44 篇科研文献

WB

    Daclatasvir dihydrochloride purchased from MCE. Usage Cited in: Eur J Med Chem. 2018 Jan 1;143:1053-1065.  [Abstract]

    GS4.3 cells are treated with 7f (20 μM), or Telaprevir (0.5μM), Sofosbuvir (0.8 μM), Daclatasvir (0.15 μM) or solvent control for 6 days.

    Daclatasvir dihydrochloride purchased from MCE. Usage Cited in: Eur J Med Chem. 2018 Jan 1;143:1053-1065.  [Abstract]

    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.

    Daclatasvir dihydrochloride purchased from MCE. Usage Cited in: PLoS Pathog. 2018 Sep 18;14(9):e1007284.  [Abstract]

    Polyprotein expression efficiency is determined by Western-Blot using an antibody against NS3 and beta actin as loading control.

    Daclatasvir dihydrochloride purchased from MCE. Usage Cited in: Open Virol J. 2014 Mar 7;8:1-8.  [Abstract]

    The PKR activation block is not unique to CypI, DAAs also prevent the IFN-induced PKR activation in HCV-infected cells. JFH-1-infected Huh7.5.1 cells are treated with or without CypI (cyclosporine A and alisporivir), DAAs (the HCV NS5A inhibitor daclatasvir and the HCV protease inhibitor telaprevir) and an HIV-1 inhibitor (reverse transcriptase inhibitor emtricitabine). Results are representative of 4 independent experiments.
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Daclatasvir dihydrochloride (BMS-790052 dihydrochloride) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir dihydrochloride is also an organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively[1][2][3].

    IC50 & Target

    EC50: 50 pM (HCV replicon genotype 1a), 9 pM (HCV replicon genotype 1b), 71 pM (HCV replicon genotype 2a), 146 pM (HCV replicon genotype 3a), 12 pM (HCV replicon genotype 4a) and 33 pM (HCV replicon genotype 5a)[1]
    Kd: 8 nM (NS5A33-202) and 210 nM (NS5A26-202)[2]
    IC50: 1.5 µM (OATP1B) and 3.27 µM (OATP1B3)[3]

    体外研究
    (In Vitro)

    Daclatasvir (BMS-790052) demonstrates potent inhibitory activity towards all genotypes tested, with EC50 values ranging from 9 pM to 146 pM. Daclatasvir inhibits HCV replicon genotype 1a, 1b, 2a, 3a, 4a and 5a with EC50 values of 50 pM, 9 pM, 71 pM, 146 pM, 12 pM and 33 pM, respectively. Daclatasvir is a potent inhibitor of the JFH-1 genotype 2a infectious virus that replicates in cell culture (EC50=28 pM)[1]. Daclatasvir (BMS-790052) binds tightly to NS5A33-202 and NS5A26-202 with Kds of 8 nM and 210 nM, respectively[2].

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

    体内研究
    (In Vivo)

    Daclatasvir (BMS-790052; 30 mg/kg; oral administration; daily; for 27 days) treatment reduces serum HCV RNA titers very rapidly by ~1.5 log10 at day 3[4].

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

    Animal Model: NOD/SCID male mice (5 weeks of age, 18-20 g) bearing HCV RNA-transfected cells[4]
    Dosage: 30 mg/kg
    Administration: Oral administration; daily; for 27 days
    Result: Reduced serum HCV RNA titers very rapidly by ~1.5 log10 at day 3.
    Clinical Trial
    分子量

    811.80

    Formula

    C40H52Cl2N8O6

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    盐酸达卡他韦;达卡他韦二盐酸盐;盐酸达拉他韦

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    溶解性数据
    细胞实验: 

    DMSO 中的溶解度 : ≥ 56 mg/mL (68.98 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    H2O 中的溶解度 : 50 mg/mL (61.59 mM; 超声助溶)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.2318 mL 6.1592 mL 12.3183 mL
    5 mM 0.2464 mL 1.2318 mL 2.4637 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    • 摩尔计算器

    • 稀释计算器

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

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 1 mg/mL (1.23 mM); 澄清溶液

      此方案可获得 ≥ 1 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 1 mg/mL (1.23 mM); 澄清溶液

      此方案可获得 ≥ 1 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
    您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
    纯度 & 产品资料

    纯度: 99.68%

    参考文献

    Daclatasvir dihydrochloride 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 1.2318 mL 6.1592 mL 12.3183 mL 30.7958 mL
    5 mM 0.2464 mL 1.2318 mL 2.4637 mL 6.1592 mL
    10 mM 0.1232 mL 0.6159 mL 1.2318 mL 3.0796 mL
    15 mM 0.0821 mL 0.4106 mL 0.8212 mL 2.0531 mL
    20 mM 0.0616 mL 0.3080 mL 0.6159 mL 1.5398 mL
    25 mM 0.0493 mL 0.2464 mL 0.4927 mL 1.2318 mL
    30 mM 0.0411 mL 0.2053 mL 0.4106 mL 1.0265 mL
    40 mM 0.0308 mL 0.1540 mL 0.3080 mL 0.7699 mL
    50 mM 0.0246 mL 0.1232 mL 0.2464 mL 0.6159 mL
    60 mM 0.0205 mL 0.1027 mL 0.2053 mL 0.5133 mL

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    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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