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  1. Anti-infection
  2. RSV
  3. RSV604

RSV604 (A-60444) 是呼吸道合胞病毒 (RSV) 復(fù)制的抑制劑。RSV604 靶向核衣殼蛋白,Kd 值為 1.6 μM。RSV604 表現(xiàn)出針對 RSV A 和 B 亞型的眾多臨床分離株的亞微摩爾活性 (平均 EC50=0.8 μM)。

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RSV604 Chemical Structure

RSV604 Chemical Structure

CAS No. : 676128-63-5

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Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ¥660
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5 mg ¥600
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10 mg ¥990
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50 mg ¥3280
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Other Forms of RSV604:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

RSV604 (A-60444) is an inhibitor of respiratory syncytial virus (RSV) replication. RSV604 targets the nucleocapsid protein, with a Kd of 1.6 μM. RSV604 displays submicromolar activity against numerous clinical isolates of both the A and B subtypes of RSV (average EC50s=0.8 μM)[1][2].

IC50 & Target

Kd: 1.6 μM (nucleocapsid protein)[2]

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEp-2 EC50
> 20 μM
Compound: RSV604
Antiviral activity against RSV RSS with N protein I129L plus L139I mutant mutation in human Hep2 cells after 5 days by plaque reduction assay
Antiviral activity against RSV RSS with N protein I129L plus L139I mutant mutation in human Hep2 cells after 5 days by plaque reduction assay
[PMID: 17576833]
HEp-2 CC50
> 50 μM
Compound: RSV604
Cytotoxicity against RSV RSS infected human Hep2 cells after 6 days by XTT assay
Cytotoxicity against RSV RSS infected human Hep2 cells after 6 days by XTT assay
[PMID: 17576833]
HEp-2 EC50
> 50 μM
Compound: RSV604
Antiviral activity against Pneumonia virus of mice 15 infected human Hep2 cells after 5 days by plaque reduction assay
Antiviral activity against Pneumonia virus of mice 15 infected human Hep2 cells after 5 days by plaque reduction assay
[PMID: 17576833]
HEp-2 EC50
> 50 μM
Compound: RSV604
Antiviral activity against Parainfluenza virus type 1 infected human Hep2 cells after 5 days by plaque reduction assay
Antiviral activity against Parainfluenza virus type 1 infected human Hep2 cells after 5 days by plaque reduction assay
[PMID: 17576833]
HEp-2 EC50
> 50 μM
Compound: RSV604
Antiviral activity against Parainfluenza virus type 3 infected human Hep2 cells after 5 days by plaque reduction assay
Antiviral activity against Parainfluenza virus type 3 infected human Hep2 cells after 5 days by plaque reduction assay
[PMID: 17576833]
HEp-2 EC50
> 50 μM
Compound: RSV604
Antiviral activity against human Metapneumovirus infected human Hep2 cells after 5 days by plaque reduction assay
Antiviral activity against human Metapneumovirus infected human Hep2 cells after 5 days by plaque reduction assay
[PMID: 17576833]
HEp-2 EC50
0.3 μM
Compound: RSV604
Antiviral activity against bovine RSV snook infected human Hep2 cells after 5 days by plaque reduction assay
Antiviral activity against bovine RSV snook infected human Hep2 cells after 5 days by plaque reduction assay
[PMID: 17576833]
HEp-2 EC50
0.5 μM
Compound: RSV604
Antiviral activity against RSV A2 infected human Hep2 cells after 5 days by plaque reduction assay
Antiviral activity against RSV A2 infected human Hep2 cells after 5 days by plaque reduction assay
[PMID: 17576833]
HEp-2 EC50
0.6 μM
Compound: RSV604
Antiviral activity against RSV B infected human Hep2 cells after 5 days by plaque reduction assay
Antiviral activity against RSV B infected human Hep2 cells after 5 days by plaque reduction assay
[PMID: 17576833]
HEp-2 EC50
0.6 μM
Compound: RSV604
Antiviral activity against DMSO-passaged wild type RSV RSS infected human Hep2 cells by plaque reduction assay
Antiviral activity against DMSO-passaged wild type RSV RSS infected human Hep2 cells by plaque reduction assay
[PMID: 17576833]
HEp-2 IC50
0.7 μM
Compound: 17b, RSV-604
Antiviral activity against RSV RSS in Hep2 cells by plaque assay
Antiviral activity against RSV RSS in Hep2 cells by plaque assay
[PMID: 17341059]
HEp-2 EC50
0.8 μM
Compound: RSV604
Antiviral activity against RSV Long infected human Hep2 cells after 5 days by plaque reduction assay
Antiviral activity against RSV Long infected human Hep2 cells after 5 days by plaque reduction assay
[PMID: 17576833]
HEp-2 EC50
0.8 μM
Compound: RSV604
Antiviral activity against RSV A isolates infected human Hep2 cells after 5 days by plaque reduction assay
Antiviral activity against RSV A isolates infected human Hep2 cells after 5 days by plaque reduction assay
[PMID: 17576833]
HEp-2 EC50
0.8 μM
Compound: RSV604
Antiviral activity against RSV B isolates infected human Hep2 cells after 5 days by plaque reduction assay
Antiviral activity against RSV B isolates infected human Hep2 cells after 5 days by plaque reduction assay
[PMID: 17576833]
HEp-2 EC50
0.86 μM
Compound: RSV604
Antiviral activity against RSV RSS infected human Hep2 cells assessed as inhibition of virus-induced cell death after 6 days by XTT assay
Antiviral activity against RSV RSS infected human Hep2 cells assessed as inhibition of virus-induced cell death after 6 days by XTT assay
[PMID: 17576833]
HEp-2 IC50
0.9 μM
Compound: 17b, RSV-604
Antiviral activity against RSV RSS in Hep2 cells by XTT assay
Antiviral activity against RSV RSS in Hep2 cells by XTT assay
[PMID: 17341059]
HEp-2 EC50
0.9 μM
Compound: RSV604
Antiviral activity against RSV RSS infected human Hep2 cells after 5 days by plaque reduction assay
Antiviral activity against RSV RSS infected human Hep2 cells after 5 days by plaque reduction assay
[PMID: 17576833]
HEp-2 EC50
1.14 μM
Compound: RSV604
Antiviral activity against RSV RSS M2 mutant infected human Hep2 cells after 5 days by plaque reduction assay
Antiviral activity against RSV RSS M2 mutant infected human Hep2 cells after 5 days by plaque reduction assay
[PMID: 17576833]
HEp-2 IC50
1.4 μM
Compound: 17b, RSV-604
Antiviral activity against RSV RSS in Hep2 cells by ELISA
Antiviral activity against RSV RSS in Hep2 cells by ELISA
[PMID: 17341059]
HEp-2 EC50
1.4 μM
Compound: RSV604
Antiviral activity against 0.02 MOI RSV RSS infected human Hep2 cells assessed as inhibition of virus-induced cell death after 6 days by XTT assay
Antiviral activity against 0.02 MOI RSV RSS infected human Hep2 cells assessed as inhibition of virus-induced cell death after 6 days by XTT assay
[PMID: 17576833]
HEp-2 EC50
1.7 μM
Compound: RSV604
Antiviral activity against RSV RSS infected human Hep2 cells assessed as reduction of viral antigen synthesis after 3 days by ELISA
Antiviral activity against RSV RSS infected human Hep2 cells assessed as reduction of viral antigen synthesis after 3 days by ELISA
[PMID: 17576833]
HEp-2 EC50
2.55 μM
Compound: RSV604
Antiviral activity against 1.5 MOI RSV RSS infected human Hep2 cells assessed as inhibition of virus-induced cell death after 6 days by XTT assay
Antiviral activity against 1.5 MOI RSV RSS infected human Hep2 cells assessed as inhibition of virus-induced cell death after 6 days by XTT assay
[PMID: 17576833]
HEp-2 EC50
2.7 μM
Compound: RSV604
Antiviral activity against plaque picked A-33903-resistant RSV RSS from passage 2 in human Hep2 cells by plaque reduction assay
Antiviral activity against plaque picked A-33903-resistant RSV RSS from passage 2 in human Hep2 cells by plaque reduction assay
[PMID: 17576833]
HEp-2 EC50
30.4 μM
Compound: RSV604
Antiviral activity against plaque picked RSV604-resistant RSV RSS from passage 2 in human Hep2 cells by plaque reduction assay
Antiviral activity against plaque picked RSV604-resistant RSV RSS from passage 2 in human Hep2 cells by plaque reduction assay
[PMID: 17576833]
HEp-2 EC50
4.78 μM
Compound: RSV604
Antiviral activity against RSV RSS with N protein N105D mutation in human Hep2 cells after 5 days by plaque reduction assay
Antiviral activity against RSV RSS with N protein N105D mutation in human Hep2 cells after 5 days by plaque reduction assay
[PMID: 17576833]
HEp-2 EC50
6.03 μM
Compound: RSV604
Antiviral activity against RSV RSS with N protein I120L mutation in human Hep2 cells after 5 days by plaque reduction assay
Antiviral activity against RSV RSS with N protein I120L mutation in human Hep2 cells after 5 days by plaque reduction assay
[PMID: 17576833]
HEp-2 EC50
6.7 μM
Compound: RSV604
Antiviral activity against RSV RSS with N protein L139I mutation in human Hep2 cells after 5 days by plaque reduction assay
Antiviral activity against RSV RSS with N protein L139I mutation in human Hep2 cells after 5 days by plaque reduction assay
[PMID: 17576833]
體外研究
(In Vitro)

RSV604 (5 天) 抑制四種實(shí)驗(yàn)室 RSV 菌株 (RSS、Long、A2 和 B) 的生長,在噬菌斑減少試驗(yàn)中,EC50 范圍為 0.5 至 0.9 μM[1]。
RSV604 (6 天) 抑制 RSV 誘導(dǎo)的 HEp-2 細(xì)胞死亡,EC50 為 0.86 μM[1]。
RSV604 (3 天) 減少 RSV 感染的 HEp-2 細(xì)胞中的病毒抗原合成,EC50 為 1.7 μM[1]。
RSV604 (1-20 μM;7 天) 以劑量依賴性方式抑制人氣道上皮 (HAE) 細(xì)胞中的 RSV 感染,沒有明顯的細(xì)胞毒性、基底外側(cè)液體滲漏到頂端表面或改變纖毛擺動頻率[1]

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

Clinical Trial
分子量

388.39

Formula

C22H17FN4O2

CAS 號
性狀

固體

顏色

White to off-white

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 100 mg/mL (257.47 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.5747 mL 12.8737 mL 25.7473 mL
5 mM 0.5149 mL 2.5747 mL 5.1495 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲存時(shí),請?jiān)?年內(nèi)使用, -20°C儲存時(shí),請?jiān)?年內(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

動物實(shí)驗(yàn):

請根據(jù)您的 實(shí)驗(yàn)動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用;
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.44 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.44 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中,混合均勻。

    2 g SBE-β-CD(磺丁基醚 β-環(huán)糊精)粉末定容于 10 mL 的生理鹽水中,完全溶解至澄清透明。
動物溶解方案計(jì)算器
請輸入動物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

由于實(shí)驗(yàn)過程有損耗,建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的動物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括:DMSO, ,均可在 MCE 網(wǎng)站選購。 ,Tween 80,均可在 MCE 網(wǎng)站選購。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。
您所需的儲備液濃度超過該產(chǎn)品的實(shí)測溶解度,以下方案僅供參考,如有需要,請與 MCE 中國技術(shù)支持聯(lián)系。
動物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液,加入 μL  μL ,混合均勻至澄清,再加 μL Tween 80,混合均勻至澄清,再加 μL 生理鹽水
連續(xù)給藥周期超過半月以上,請謹(jǐn)慎選擇該方案。
請確保第一步儲備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.92%

參考文獻(xiàn)

RSV604 相關(guān)分類

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲存時(shí),請?jiān)?年內(nèi)使用, -20°C儲存時(shí),請?jiān)?年內(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 2.5747 mL 12.8737 mL 25.7473 mL 64.3683 mL
5 mM 0.5149 mL 2.5747 mL 5.1495 mL 12.8737 mL
10 mM 0.2575 mL 1.2874 mL 2.5747 mL 6.4368 mL
15 mM 0.1716 mL 0.8582 mL 1.7165 mL 4.2912 mL
20 mM 0.1287 mL 0.6437 mL 1.2874 mL 3.2184 mL
25 mM 0.1030 mL 0.5149 mL 1.0299 mL 2.5747 mL
30 mM 0.0858 mL 0.4291 mL 0.8582 mL 2.1456 mL
40 mM 0.0644 mL 0.3218 mL 0.6437 mL 1.6092 mL
50 mM 0.0515 mL 0.2575 mL 0.5149 mL 1.2874 mL
60 mM 0.0429 mL 0.2146 mL 0.4291 mL 1.0728 mL
80 mM 0.0322 mL 0.1609 mL 0.3218 mL 0.8046 mL
100 mM 0.0257 mL 0.1287 mL 0.2575 mL 0.6437 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:
RSV604
目錄號:
HY-12993
需求量: