Morphothiadin 莫非赛定; GLS4|cas:1092970-12-1|西域试剂

Morphothiadin 莫非赛定; GLS4,99.84%

产品编号：Bellancom-108917| CAS NO：1092970-12-1| 分子式：C₂₁H₂₂BrFN₄O₃S| 分子量：509.39

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货号	价格	库存与货期
Bellancom-108917	￥1200.00	杭州北京（现货）
Bellancom-108917	￥3600.00	杭州北京（现货）
Bellancom-108917	￥5700.00	杭州北京（现货）

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Morphothiadin 莫非赛定; GLS4

产品介绍

Morphothiadin 是野生型和阿德福韦耐药 HBV 复制的有效抑制剂，其 IC₅₀ 值为 12 nM。

生物活性

Morphothiadin is a potent inhibitor on the replication of both wild-type and adefovir-resistant HBV with an IC₅₀ of 12 nM.

体外研究

Morphothiadin is a potent inhibitor on the replication of both wild-type and adefovir-resistant HBV with an IC₅₀ of 12 nM. Morphothiadin (GLS4) shows no toxicity up to 25 μM. The cytotoxic dose whereby 50% of cells die (CC₅₀) for primary hepatocytes is 115 μM for Morphothiadin (P<0.001). The CC₉₀ is 190 μM for Morphothiadin (P<0.01) in HepAD38 cells. Morphothiadin strongly inhibits virus accumulation in the supernatant of HepAD38 cells at 25 nM to 100 nM (P<0.02). Results show a concentration-dependent decrease of core protein in cells treated with Morphothiadin.

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

体内研究

The area under the concentration-time curve from 0 to 24 h (AUC_0-24) of Morphothiadin (GLS4) is 556 h•ng/mL. After intravenous administration of 10 mg/kg Morphothiadin, the total plasma clearance and apparent volume distribution are 4.2 liters/h/kg and 7.38 liters/kg, respectively. The bioavailability of Morphothiadin is 25.5%. It is found that virus titers have increased 83.5-fold in mice treated with 3.75 mg/kg per day of Morphothiadin, 28.3-fold among mice treated with 7.5 mg/kg per day, but only 3- to 6-fold among mice treated with the higher doses of Morphothiadin. There is generally an inverse relationship between Morphothiadin dose and virus titer, with the greatest rebound seen in mice treated with 3.75 mg/kg per day of Morphothiadin (540-fold) and the smallest rebound in mice treated with 60 mg/kg per day (23-fold) (P<0.001). The Morphothiadin doses of >7.5 mg/kg per day significantly suppresses the virus replication cycle throughout the treatment period, while Morphothiadin doses of >15 mg/kg per day suppresses virus for up to 2 weeks after the end of 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 : 62.5 mg/mL (122.70 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	1.9631 mL	9.8157 mL	19.6313 mL
5 mM	0.3926 mL	1.9631 mL	3.9263 mL
10 mM	0.1963 mL	0.9816 mL	1.9631 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: ≥ 3 mg/mL (5.89 mM); Clear solution

此方案可获得 ≥ 3 mg/mL (5.89 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 30.0 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% corn oil
Solubility: ≥ 3 mg/mL (5.89 mM); Clear solution

此方案可获得 ≥ 3 mg/mL (5.89 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 30.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。