Dapivirine 达匹维林; TMC120; R147681|cas:244767-67-7|西域试剂

Dapivirine 达匹维林; TMC120; R147681,99.90%

产品编号：Bellancom-14266| CAS NO：244767-67-7| 分子式：C₂₀H₁₉N₅| 分子量：329.40

Dapivirine(TMC 120, TMC 120 R147681)是HIV非核苷逆转录酶抑制剂（NNRTI），IC50为24 nM，能抑制包括NNRTI抗性的各种HIV-1毒株。

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-14266	￥1000.00	杭州北京（现货）
Bellancom-14266	￥1526.00	杭州北京（现货）
Bellancom-14266	￥6000.00	杭州北京（现货）
Bellancom-14266	￥10416.00	杭州北京（现货）

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Dapivirine 达匹维林; TMC120; R147681

产品介绍

Dapivirine (TMC120) 是二芳基嘧啶 (DAPY) 的原型，是具有口服活性的非核苷类逆转录酶抑制剂 (NRTI)。Dapivirine (TMC120) 可直接与 HIV 的逆转录酶结合。Dapivirine (TMC120)调节自噬并诱导 Akt、Bad 和 SAPK/JNK 的激活。

生物活性

Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations.

体外研究

Dapivirine (4-64 μM, 24, 48, 72, 96 and 120 hours) inhibits proliferation of glioma cells and induces apoptosis (16 μM, 12-48 h).
Dapivirine (8 and 16 μM, 12 h) enhances invasion of glioma cells.
Dapivirine (16 μM, 12 h, 24 h and 48 h) promotes autophagy in U87 cells.
Dapivirine (TMC120-R147681) apparently blocks infection in the primary cultures at a 10 nM concentration, but secondary cultures revealed that a 100 nM concentration was needed to completely prevent proviral integration.

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

Cell Proliferation Assay

Cell Line:	U87 glioblastoma cells.
Concentration:	4, 8, 16 μM.
Incubation Time:	24, 48, 72, 96 and 120 hours.
Result:	Inhibited proliferation of glioma cells. IC₅₀ was 10.73 μM.

Apoptosis Analysis

Cell Line:	U87 glioblastoma cells.
Concentration:	16 μM.
Incubation Time:	12h, 24h and 48h.
Result:	Induced apoptosis. Decreased caspase-3.

体内研究
(In Vivo)

Dapivirine (16 mg/kg, once every 3 days for 12 days) exhibits potent antitumor activity in human glioblastoma models in mice.
Dapivirine has been shown to have a half-life in the range of 65 to 90 h^[4].

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

Animal Model:	U87 cells were subcutaneously injected into the nude mice.
Dosage:	16 mg/kg.
Administration:	Once every 3 days for 12 days.
Result:	Significantly decreased the tumor volumes. A significant decrease in Ki67 (a marker for proliferating cells that is overexpressed in many cancers) staining in sections of dapivirine-treated tumors compared to tumors from vehicle-treated mice.

体内研究

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

Animal Model:	U87 cells were subcutaneously injected into the nude mice.
Dosage:	16 mg/kg.
Administration:	Once every 3 days for 12 days.
Result:	Significantly decreased the tumor volumes. A significant decrease in Ki67 (a marker for proliferating cells that is overexpressed in many cancers) staining in sections of dapivirine-treated tumors compared to tumors from vehicle-treated mice.

体内研究

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

Animal Model:	U87 cells were subcutaneously injected into the nude mice.
Dosage:	16 mg/kg.
Administration:	Once every 3 days for 12 days.
Result:	Significantly decreased the tumor volumes. A significant decrease in Ki67 (a marker for proliferating cells that is overexpressed in many cancers) staining in sections of dapivirine-treated tumors compared to tumors from vehicle-treated mice.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 47 mg/mL (142.68 mM)

* "≥" 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	3.0358 mL	15.1791 mL	30.3582 mL
5 mM	0.6072 mL	3.0358 mL	6.0716 mL
10 mM	0.3036 mL	1.5179 mL	3.0358 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: 2.08 mg/mL (6.31 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (6.31 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 20.8 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: ≥ 2.08 mg/mL (6.31 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.31 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*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

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

. Weiwen Liu, et al. Antitumor Activity and Mechanism of a Reverse Transcriptase Inhibitor, Dapivirine, in Glioblastoma. J Cancer. 2018 Jan 1;9(1):117-128. [Content Brief]

. Bríd Devlin, et al. Development of dapivirine vaginal ring for HIV prevention. Antiviral Res. 2013 Dec;100 Suppl:S3-8. [Content Brief]

. Yven Van Herrewege, et al. In vitro evaluation of nonnucleoside reverse transcriptase inhibitors UC-781 and TMC120-R147681 as human immunodeficiency virus microbicides. Antimicrob Agents Chemother. 2004 Jan;48(1):337-9. [Content Brief]

[4]. Michael E Halwes, et al. Pharmacokinetic modeling of a gel-delivered dapivirine microbicide in humans. Eur J Pharm Sci. 2016 Oct 10;93:410-8. [Content Brief]

化学品安全说明书(MSDS)

下载MSDS

质检证书(COA)

产品编号(Item Number)

批号(Lot Number)

1. 物质的识别

产品名：	Dapivirine
CAS号：	244767-67-7
制造商/供应商：	西域试剂网站：www.hzbp.cn 邮件：13911702513@139.com

2. 合成/成分数据

产品名：	Dapivirine
别名：	TMC120; R147681
分子式：	C20H19N5
分子量：	329.4

3. 急救措施

吸入后：	如果吸入，移至空气新鲜处，如果呼吸困难，给输氧，如呼吸停止，给予人工呼吸。
皮肤接触后：	用大量的水冲洗，移除污染的衣服和鞋子。
眼睛接触后：	检查并取下隐形眼镜，并用大量的水冲洗；呼叫医生。
吞食后：	如果吞食，用大量纯净水漱口；呼叫医生。

4. 消防措施

适当的灭火剂：	雾状水，二氧化碳，干粉或泡沫。
防护设备：	穿戴自给式呼吸器和防护服，以防止与皮肤和眼睛接触。

5. 泄漏应急处理

安全防范措施：	封锁泄漏区域；穿戴自给式呼吸器，防护服和厚橡胶手套。
清洁/收集措施：	使用液体粘合原料（硅藻土，通用粘合剂）吸取精细粉末；使用酒精擦洗表面和设备除去污渍；根据第11条处理被污染的材料。

6. 处理和储存

安全处理说明：	避免吸入和接触皮肤，眼睛及衣物；材料可能略微具有刺激性。
储存：	粉末型式 -20°C 3年；4°C 2年溶于溶剂 -80°C 6个月；-20°C 1个月

7. 接触控制和个人防护

呼吸设备：	NIOSH / MSHA认可的呼吸器。
双手保护：	耐化学腐蚀的橡胶手套。
眼睛防护：	化学安全护目镜。

8. 稳定性和反应活性

稳定性：	按照说明存储是稳定的；避免强氧化剂。
热分解/其他要避免的情况：	避免光和热。

9. 毒性资料

急性毒性：	无可用资料。
主要刺激性影响：	无可用资料。
在皮肤上：	无可用资料。
对眼睛：	无可用资料；可能具有刺激性。