TMC647055 Choline salt,98.06%

产品编号:Bellancom-15591A| 分子式:C37H53N5O8S| 分子量:727.91

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用,

货号 包装 价格 库存与货期 购买量 操作
Bellancom-15591A
2000.00 杭州 北京(现货)
Bellancom-15591A
3000.00 杭州 北京(现货)
Bellancom-15591A
4500.00 杭州 北京(现货)
Bellancom-15591A
13000.00 杭州 北京(现货)
Bellancom-15591A
21000.00 杭州 北京(现货)

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TMC647055 Choline salt

产品介绍 TMC647055 (Choline salt) 是一种有效的 HCV 复制的非核苷 NS5B 聚合酶抑制剂。TMC647055 Choline salt 具有较强的 HCV 结合活性,其 IC50 值为 82 nM。TMC647055 Choline salt 可用于丙型肝炎病毒 (HCV) 的研究。
生物活性

TMC647055 (Choline salt) is a potent nonnucleoside NS5B polymerase inhibitor of HCV replication. TMC647055 Choline salt has potent HCV combine activity with an IC50 value of 82 nM. TMC647055 Choline salt can be used for the research of Hepatitis C virus (HCV).

体外研究

TMC647055 (Choline salt) has antiviral activity with an EC90 value of 0.3 μM in Huh7-Luc cells.
TMC647055 Choline salt has potent combine activity with an EC50 value of 82 nM in cellular HCV assays.

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

体内研究

TMC647055 Choline salt (compound 18a) (2 mg/kg, iv.; 10mg/kg, po.) shows an acceptable PK profile, characterized by high oral bioavailability and high systemic exposure after single oral dosing of 10 mg/kg, combined with a moderate plasma clearanceand low volume of distribution.

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

Animal Model: Rats
Dosage: 2 mg/kg; 10mg/kg
Administration: 2 mg/kg, iv.; 10mg/kg, po.; singel
Result:
No. Cl (L/h/kg) Cmax(ng/mL) [Liver] (ng/mL) L/P F (%)
TMC647055 (compound 18a) 3.2 440 7800 46 >66
体内研究

TMC647055 Choline salt (compound 18a) (2 mg/kg, iv.; 10mg/kg, po.) shows an acceptable PK profile, characterized by high oral bioavailability and high systemic exposure after single oral dosing of 10 mg/kg, combined with a moderate plasma clearanceand low volume of distribution.

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

Animal Model: Rats
Dosage: 2 mg/kg; 10mg/kg
Administration: 2 mg/kg, iv.; 10mg/kg, po.; singel
Result:
No. Cl (L/h/kg) Cmax(ng/mL) [Liver] (ng/mL) L/P F (%)
TMC647055 (compound 18a) 3.2 440 7800 46 >66
性状Solid
溶解性数据
In Vitro: 

DMSO : 62.5 mg/mL (85.86 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.3738 mL 6.8690 mL 13.7380 mL
5 mM 0.2748 mL 1.3738 mL 2.7476 mL
10 mM 0.1374 mL 0.6869 mL 1.3738 mL
*

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。

In Vivo:

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

  • 1.

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

    Solubility: ≥ 2.08 mg/mL (2.86 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.86 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 西域 网站选购。
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)

参考文献

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