R-10015|cas:2097938-51-5|西域试剂

R-10015,99.72%

产品编号：Bellancom-120097| CAS NO：2097938-51-5| 分子式：C₂₀H₁₉ClN₆O₂| 分子量：410.86

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货号	价格	库存与货期
Bellancom-120097	￥3000.00	杭州北京（现货）
Bellancom-120097	￥4700.00	杭州北京（现货）
Bellancom-120097	￥14000.00	杭州北京（现货）

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R-10015

产品介绍

R-10015 是一种用于 HIV 感染的广谱抗病毒化合物，是高效选择性的 LIMK 抑制剂，通过结合 ATP 结合口袋阻断 LIMK，抑制人 LIMK1 的 IC₅₀ 值为 38 nM。

生物活性

R-10015, a broad-spectrum antiviral compound for HIV infection, acts as a potent and selective inhibitor of LIM domain kinase (LIMK) and binds to the ATP-binding pocket, with an IC₅₀ of 38 nM for human LIMK1.

体外研究

R-10015 (100 μM; 0-4 hours) inhibits cofilin phosphorylation directly through blocking LIM kinase in CEM-SS T cells.
R-10015 inhibits HIV-1 DNA synthesis, nuclear migration, and virion release.
R-10015 inhibits multiple viruses, including Zaire ebolavirus (EBOV), Rift Valley fever virus (RVFV), Venezuelan equine encephalitis virus (VEEV), and herpes simplex virus 1 (HSV-1) .

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

Western Blot Analysis

Cell Line:	CEM-SS T cells
Concentration:	100 μM
Incubation Time:	0 hour,0.5 hour,1 hour,2 hours,4 hours
Result:	Inhibited cofilin phosphorylation directly through blocking LIM kinase in CEM-SS T cells.

体内研究
(In Vivo)

R-10015 (10 mg/kg; i.p.) displays none indication of toxicity. The result suggests the possibility of short-term use of LIMK inhibitors to block viral infections.

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

Animal Model:	6-8 weeks female C3H/HeN mice
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection
Result:	Displayed none indication of toxicity.

体内研究

R-10015 (10 mg/kg; i.p.) displays none indication of toxicity. The result suggests the possibility of short-term use of LIMK inhibitors to block viral infections.

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

Animal Model:	6-8 weeks female C3H/HeN mice
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection
Result:	Displayed none indication of toxicity.

体内研究

R-10015 (10 mg/kg; i.p.) displays none indication of toxicity. The result suggests the possibility of short-term use of LIMK inhibitors to block viral infections.

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

Animal Model:	6-8 weeks female C3H/HeN mice
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection
Result:	Displayed none indication of toxicity.

性状

Solid

溶解性数据

In Vitro:

DMSO : 62.5 mg/mL (152.12 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4339 mL	12.1696 mL	24.3392 mL
5 mM	0.4868 mL	2.4339 mL	4.8678 mL
10 mM	0.2434 mL	1.2170 mL	2.4339 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: ≥ 5 mg/mL (12.17 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (12.17 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 50.0 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: ≥ 5 mg/mL (12.17 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (12.17 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 50.0 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: ≥ 5 mg/mL (12.17 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (12.17 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 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。