TMC353121|cas:857066-90-1|西域试剂

TMC353121,98.0%

产品编号：Bellancom-11097| CAS NO：857066-90-1| 分子式：C₃₂H₄₂N₆O₃| 分子量：558.71

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	价格	库存与货期
Bellancom-11097	￥1395.00	杭州北京（现货）
Bellancom-11097	￥2604.00	杭州北京（现货）
Bellancom-11097	￥7905.00	杭州北京（现货）

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TMC353121

产品介绍

TMC353121 是一种有效的呼吸道合胞病毒 (RSV) 融合抑制剂，pEC₅₀ 为 9.9。

生物活性

TMC353121 is a potent respiratory syncytial virus (RSV) fusion inhibitor with pEC₅₀ of 9.9.

体外研究

TMC353121 shows activity against groups A and B RSV and against a panel of clinical isolates with equal potency. TMC353121 is a potent RSV fusion inhibitor in vitro. TMC353121 is active against wild-type RSV (strain LO), with a 50% effective concentration (EC₅₀) of 0.07 ng/mL in HeLaM cells.

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

体内研究

After i.v. bolus administration of a single dose of 10 mg/kg to Sprague-Dawley rats, the plasma drug concentration-time profile of TMC353121 exhibits multicompartmental pharmacokinetics. Mean plasma drug concentrations decrease rapidly during the first hours after dosing and then more slowly, with a half-life of about 12 h, as determined for the last part of the curve between 8 and 24 h postdose. TMC353121 is rapidly eliminated from plasma (CL=8.6 liters/h/kg) and extensively distributed (V_ss=55 liters/kg). TMC353121 is administered once, i.v. at 2.5 mg/kg or at 0.25 mg/kg. Drug levels are determined in lung tissue, serum, and BAL fluid at different time points. TMC353121 followed multicompartment pharmacokinetics, with a fast decay in serum within the first hour after i.v. injection, followed by a slower decay. The drug is eliminated quickly from the blood resulting in very low blood levels after 24 h. Lung concentrations are much higher than serum concentrations and in BAL fluid the drug is just above the limit of detection at 8 h after injection. Very low drug levels can still be detected in the lung 5 days after treatment.

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (89.49 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7898 mL	8.9492 mL	17.8984 mL
5 mM	0.3580 mL	1.7898 mL	3.5797 mL
10 mM	0.1790 mL	0.8949 mL	1.7898 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。-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 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (4.47 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.47 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (4.47 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (4.47 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 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。
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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.47 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.47 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。