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  2. Anti-infection
  3. HCV HBV
  4. Inarigivir soproxil

Inarigivir soproxil  (Synonyms: SB9200; GS-9992)

目錄號: HY-109035 純度: 99.87%
COA 產(chǎn)品使用指南 技術(shù)支持

Inarigivir soproxil (SB9200) 是一種先天免疫激動劑，對耐藥 HCV 變異體具有有效的抗病毒活性，在基因型 1 HCV 復(fù)制子系統(tǒng)的細(xì)胞中，對 HCV 1a/1b 的 EC50 分別為 2.2 和 1.0 μM。Inarigivir soproxil 是 SB 9000 的口服生物可利用前體。Inarigivir soproxil 對 RNA 病毒具有廣譜抗病毒活性，包括 HCV、諾如病毒、呼吸道合胞病毒以及流感和 HBV。

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Inarigivir soproxil Chemical Structure

Inarigivir soproxil Chemical Structure

CAS No. : 942123-43-5

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規(guī)格 價(jià)格 是否有貨 數(shù)量
1 mg ￥1500
In-stock
5 mg ￥3200
In-stock
10 mg ￥4800
In-stock
25 mg 現(xiàn)貨 詢價(jià)
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Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻(xiàn)

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Inarigivir soproxil (SB9200) is an agonist of innate immunity and shows potent antiviral activity against resistant HCV variants, with EC50s of 2.2 and 1.0 μM for HCV 1a/1b in cells of genotype 1 HCV replicon systems. Inarigivir soproxil, an orally bioavailable proagent of SB 9000, has broad-spectrum antiviral activity against RNA viruses including HCV, norovirus, respiratory syncytial virus and influenza and HBV[1][2].

IC50 & Target

EC50: 2.2/1.0 μM (HCV 1a/1b)[1].
細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
HepG2 2.2.15 EC50
2.1 μM
Compound: 3
Antiviral activity against 3TC-resistant HBV with polymerase L180M mutation infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization
Antiviral activity against 3TC-resistant HBV with polymerase L180M mutation infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization
[PMID: 20117930]
HepG2 2.2.15 EC50
2.4 μM
Compound: 3
Antiviral activity against 3TC-resistant HBV with polymerase M204V mutation infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization
Antiviral activity against 3TC-resistant HBV with polymerase M204V mutation infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization
[PMID: 20117930]
HepG2 2.2.15 EC50
2.5 μM
Compound: 3
Antiviral activity against wild type HBV infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization
Antiviral activity against wild type HBV infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization
[PMID: 20117930]
HepG2 2.2.15 EC50
2.8 μM
Compound: 3
Antiviral activity against ADV-resistant HBV N236T mutation infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization
Antiviral activity against ADV-resistant HBV N236T mutation infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization
[PMID: 20117930]
HepG2 2.2.15 EC50
3 μM
Compound: 3
Antiviral activity against 3TC-resistant HBV with polymerase M204I mutation infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization
Antiviral activity against 3TC-resistant HBV with polymerase M204I mutation infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization
[PMID: 20117930]
HepG2 2.2.15 EC50
3.1 μM
Compound: 3
Antiviral activity against 3TC-resistant HBV with polymerase LMMV mutation infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization
Antiviral activity against 3TC-resistant HBV with polymerase LMMV mutation infected in HepG2.2.15 cells assessed as nucleic acid and protein levels dosed daily for 9 days and measured 24 hrs after last treatment by Southern blot hybridization
[PMID: 20117930]
HFF CC50
> 1000 μM
Compound: 3
Cytotoxicity against human HFF cells after 24 hrs by MTT assay
Cytotoxicity against human HFF cells after 24 hrs by MTT assay
[PMID: 20117930]
Vero CC50
> 1000 μM
Compound: 3
Cytotoxicity against african green monkey Vero cells after 24 hrs by MTT assay
Cytotoxicity against african green monkey Vero cells after 24 hrs by MTT assay
[PMID: 20117930]
體外研究
(In Vitro)

Inarigivir soproxil (SB 9200) is a first-in-class oral modulator of innate immunity that acts via the activation of the RIG-I and NOD2 pathways[1].
Inarigivir soproxil is an effective inhibitor of HCV replication in cell culture. The antiviral activity of Inarigivir soproxil against HCV was assessed using genotype 1 HCV replicon systems in duplicate experiments using 4 drug concentrations. Inarigivir soproxil inhibits HCV replication with EC50s of 2.2 and 1.0 μM, and EC90s of 8.0 and 6.0 μM for genotype 1A and 1B, respectively[1].
Inarigivir soproxil (SB 9200), an orally bioavailable dinucleotide, activates the viral sensor proteins, retinoic acid-inducible gene 1 (RIG-I) and nucleotide-binding oligomerization domain-containing protein 2 (NOD2) causing the induction of the interferon (IFN) signaling cascade for antiviral defense[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

The induction of host immune responses by pretreatment with Inarigivir soproxil (SB 9200) followed by Entecavir (ETV) resulted in antiviral efficacy that was superior to that obtained using the strategy of viral reduction with ETV followed by immunomodulation[2].
Sequential treatment of chronic WHV carrier woodchucks with Inarigivir soproxil (30 mg/kg)followed by ETV induced marked suppression of serum viremia and antigenemia and delayed recrudescence of viral replication compared to sequential treatment with ETV followed by Inarigivir soproxil[2].

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

Animal Model: Woodchucks chronically infected with woodchuck hepatitis virus (WHV)[2]
Dosage: 30 mg/kg
Administration: Orally treated once daily; group 1 received ETV for 4 weeks followed by Inarigivir soproxil for 12 weeks. Group 2 received Inarigivir soproxil for 12 weeks followed by ETV for 4 weeks
Result: Both groups demonstrated marked reductions in hepatic WHV nucleic acid levels which were more pronounced in Group 2.
Clinical Trial
分子量

703.62

Formula

C25H34N7O13PS
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

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 80 mg/mL (113.70 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)

H2O 中的溶解度 : 10 mg/mL (14.21 mM; 超聲助溶 (<60°C))

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 1.4212 mL 7.1061 mL 14.2122 mL
5 mM 0.2842 mL 1.4212 mL 2.8424 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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C儲存時(shí)，請?jiān)?個月內(nèi)使用，-20°C儲存時(shí)，請?jiān)?個月內(nèi)使用。

* 備注：如您選擇水作為儲備液，請稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

  • 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    90% Corn Oil

    Solubility: ≥ 5 mg/mL (7.11 mM); 澄清溶液

    此方案可獲得 ≥ 5 mg/mL（飽和度未知）的澄清溶液，此方案實(shí)驗(yàn)周期在半個月以上的動物實(shí)驗(yàn)酌情使用。

    以 1 mL 工作液為例，取 100 μL 50.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中，混合均勻。

  • 方案 二

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

    Solubility: ≥ 4 mg/mL (5.68 mM); 澄清溶液

    此方案可獲得 ≥ 4 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 40.0 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。
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

只
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）。

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

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: 99.87%

參考文獻(xiàn)

Inarigivir soproxil 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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C儲存時(shí)，請?jiān)?個月內(nèi)使用，-20°C儲存時(shí)，請?jiān)?個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 1.4212 mL 7.1061 mL 14.2122 mL 35.5305 mL
5 mM 0.2842 mL 1.4212 mL 2.8424 mL 7.1061 mL
10 mM 0.1421 mL 0.7106 mL 1.4212 mL 3.5531 mL
DMSO 15 mM 0.0947 mL 0.4737 mL 0.9475 mL 2.3687 mL
20 mM 0.0711 mL 0.3553 mL 0.7106 mL 1.7765 mL
25 mM 0.0568 mL 0.2842 mL 0.5685 mL 1.4212 mL
30 mM 0.0474 mL 0.2369 mL 0.4737 mL 1.1844 mL
40 mM 0.0355 mL 0.1777 mL 0.3553 mL 0.8883 mL
50 mM 0.0284 mL 0.1421 mL 0.2842 mL 0.7106 mL
60 mM 0.0237 mL 0.1184 mL 0.2369 mL 0.5922 mL
80 mM 0.0178 mL 0.0888 mL 0.1777 mL 0.4441 mL
100 mM 0.0142 mL 0.0711 mL 0.1421 mL 0.3553 mL

* 備注：如您選擇水作為儲備液，請稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

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  • 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：
Inarigivir soproxil
目錄號：
HY-109035
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