Dapivirine|244767-67-7|(达匹维林; TMC120; R147681)-陌孚医药/Medlife

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Dapivirine (Synonyms: 达匹维林; TMC120; R147681)

目录号: PL03978 纯度: ≥99%

CAS No. :244767-67-7

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中文名称	Dapivirine
中文别名	4-[[4-[(2,4,6-三甲基苯基)氨基]-2-嘧啶基]氨基]-苯腈;达匹维林
英文名称	Dapivirine
英文别名	Benzonitrile,4-[[4-[(2,4,6-trimethylphenyl)amino]-2-pyrimidinyl]amino]-;Dapivirine (TMC120);4-[[4-(2,4,6-trimethylanilino)pyrimidin-2-yl]amino]benzonitrile;4-[[4-[(2,4,6-Trimethylphenyl)amino]-2-pyrimidinyl]amino]benzonitrile;Dapivirine;TMC-120;4-({4-[(2,4,6-trimethylphenyl)amino]pyrimidin-2-yl}amino)benzenecarbonitrile;dapivirinum;R 147681;TMC120;UNII-TCN4MG2VXS;TMC 120;TMC 120R147681;R147681;Dapivirine(TMC120);TCN4MG2VXS;Benzonitrile, 4-[[4-[(2,4,6-trimethylphenyl)amino]-2-pyrimidinyl]amino]-;4-[4-(2,4,6-TRIMETHYL-PHENYLAMINO)-PYRIMIDIN-2-YLAMINO]-BENZONITRILE;AK326148;4-((4-(mesitylamino)pyrimidin-2-yl)amino)benzonitrile;4-({4-[(2,4,6-trimethylphenyl)amino]pyrimidin-2-yl}amino)benzonitr
Cas No.	244767-67-7
分子式	C₂₀H₁₉N₅
分子量	329.40
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

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.

性状

Solid

体外研究(In Vitro)

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

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.
has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

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

ClinicalTrial

参考文献

[1]. 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.
[2]. Bríd Devlin, et al. Development of dapivirine vaginal ring for HIV prevention. Antiviral Res. 2013 Dec;100 Suppl:S3-8.
[3]. Yven Van Herrewege, et al. In

溶解度数据	In Vitro: DMSO : ≥ 47 mg/mL (142.68 mM)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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