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  1. Anti-infection Metabolic Enzyme/Protease
  2. SARS-CoV MMP
  3. Rilpivirine hydrochloride

Rilpivirine hydrochloride  (Synonyms: 鹽酸利匹韋林; TMC-278 hydrochloride; TMC278 hydrochloride; TMC 278 hydrochloride)

目錄號(hào): HY-10574A 純度: 99.81%
COA 產(chǎn)品使用指南 技術(shù)支持

Rilpivirine (R278474) hydrochloride 是一種有效和特異性的二芳基嘧啶 (DAPY) 非核苷逆轉(zhuǎn)錄酶抑制劑 (NNRTI)。Rilpivirine hydrochloride 對(duì)野生型 HIV (EC50=0.4 nM) 和突變體 (EC50=0.1-2.0 nM) 具有很高的抗病毒活性。Rilpivirine hydrochloride 對(duì) HIV 耐藥性的形成產(chǎn)生了高度的遺傳障礙。

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Rilpivirine hydrochloride Chemical Structure

Rilpivirine hydrochloride Chemical Structure

CAS No. : 700361-47-3

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10 mM * 1 mL in DMSO ¥660
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Customer Review

Other Forms of Rilpivirine hydrochloride:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Rilpivirine (R278474) hydrochloride is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine hydrochloride has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine hydrochloride has a high genetic barrier to resistance development of HIV[1][2].

IC50 & Target

IC50: 20±10 μM (MMP)[1] Ki: 1.5±0.27 nM (MMPs)[1]

體外研究
(In Vitro)

R278474 對(duì)野生型 HIV-1 具有活性 (EC50=0.4 nM) 和所有測(cè)試的單突變體和雙突變體 (EC50=0.1-2.0 nM)[1]。
R278474 (10-5000 nM; 30 d) 在 30 天內(nèi)未觀察到 1 μM 野生型 HIV-1 突破的跡象[1]。
R278474 在 50% 抑制濃度 (EC50) 小于 1 nM 時(shí)抑制 81% 的臨床分離株(約 1200 種重組臨床分離株),在 EC50 小于 10 nM 時(shí)則抑制 94%[1]
TMC278 對(duì)野生型 HIV-1 M 組分離株 (0.07-1.01 nM) 顯示亞納摩爾的 EC50[2]。

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

體內(nèi)研究
(In Vivo)

R278474 (10-160 mg/kg; p.o. for 1 month) does not produce abnormal effects in rat, apart from liver weight increase and species-specific thyroid hypertrophy, both at the higher dose levels[1].
R278474 (i.v.) exhibits elimination half-life ranges from 4.4 h in rat to 31 h in dog, and exposure (AUCinf) amounts to 3.1 μg h/mL (4 mg/kg) in rat, 8.7 μg h/mL (1.25 mg/kg) in dog, 1.4 μg h/mL (1.25 mg/ kg) in monkey, and 44 μg h/mL (1.25 mg/kg) in rabbit[1].
R278474 (p.o.) exhibits half-life ranges between 2.8 h in rat and 39 h in dog, and oral bioavailability of 32% and 31% in rat and dog[1].

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

Clinical Trial
分子量

402.88

Formula

C22H19ClN6

CAS 號(hào)
性狀

固體

顏色

White to off-white

中文名稱

鹽酸利匹韋林;鹽酸利吡韋林

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 125 mg/mL (310.27 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.4821 mL 12.4106 mL 24.8213 mL
5 mM 0.4964 mL 2.4821 mL 4.9643 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

由于實(shí)驗(yàn)過程有損耗,建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
參考文獻(xiàn)

Rilpivirine hydrochloride 相關(guān)分類

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4821 mL 12.4106 mL 24.8213 mL 62.0532 mL
5 mM 0.4964 mL 2.4821 mL 4.9643 mL 12.4106 mL
10 mM 0.2482 mL 1.2411 mL 2.4821 mL 6.2053 mL
15 mM 0.1655 mL 0.8274 mL 1.6548 mL 4.1369 mL
20 mM 0.1241 mL 0.6205 mL 1.2411 mL 3.1027 mL
25 mM 0.0993 mL 0.4964 mL 0.9929 mL 2.4821 mL
30 mM 0.0827 mL 0.4137 mL 0.8274 mL 2.0684 mL
40 mM 0.0621 mL 0.3103 mL 0.6205 mL 1.5513 mL
50 mM 0.0496 mL 0.2482 mL 0.4964 mL 1.2411 mL
60 mM 0.0414 mL 0.2068 mL 0.4137 mL 1.0342 mL
80 mM 0.0310 mL 0.1551 mL 0.3103 mL 0.7757 mL
100 mM 0.0248 mL 0.1241 mL 0.2482 mL 0.6205 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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產(chǎn)品名稱:
Rilpivirine hydrochloride
目錄號(hào):
HY-10574A
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