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  2. Metabolic Enzyme/Protease Anti-infection
  3. HIV Integrase HIV
  4. Dolutegravir sodium

Dolutegravir sodium  (Synonyms: 度魯特韋鈉鹽; S/GSK1349572 sodium)

目錄號(hào): HY-13238A 純度: 99.97%
COA 產(chǎn)品使用指南 技術(shù)支持

Dolutegravir sodium (S/GSK1349572 sodium) 是一種高效、口服的 HIV 整合酶鏈轉(zhuǎn)移抑制劑，在 HIV-1 整合酶催化的鏈轉(zhuǎn)移中的 IC50 值為 2.7 nM，Dolutegravir sodium (S/GSK1349572 sodium) 抑制 HIV-1 病毒在外周血單個(gè)核細(xì)胞中的復(fù)制，IC50 為 0.51 nM。Dolutegravir sodium (S/GSK1349572 sodium) 對(duì) Y143R，N155H 和 G140S/Q148H 突變體也保持高效 (EC50=3.6-5.8 nM)。

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Dolutegravir sodium Chemical Structure

Dolutegravir sodium Chemical Structure

CAS No. : 1051375-19-9

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Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ￥990
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1 mg ￥473
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5 mg ￥1020
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10 mg ￥1625
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25 mg ￥3413
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50 mg ￥4960
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Customer Review

Other Forms of Dolutegravir sodium:

    Dolutegravir sodium purchased from MCE. Usage Cited in: Antivir Ther. 2017;22(8):645-657.  [Abstract]

    Dolutegravir (DTG) and MVC+DTG significantly increase the SIRT1 level by respectively, 9% and 18%.

    Dolutegravir sodium purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2016 Jul 21;39(2):639-650.  [Abstract]

    Arithmetic means±SEM (n=19) of erythrocyte annexin-V-binding following incubation for 48 hours to Ringer solution without (white bar) or with (black bars) Dolutegravir (4.77-19.08 μM). For comparison, the effect of the solvent DMSO is shown (grey bar).

    查看 HIV 亞型特異性產(chǎn)品:

    • 生物活性

    • 實(shí)驗(yàn)參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Dolutegravir sodium (S/GSK1349572 sodium) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir sodium (S/GSK1349572 sodium) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir sodium (S/GSK1349572 sodium) retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM)[1][2].

    IC50 & Target

    HIV-1

     

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    IM-9 CC50
    4.8 μM
    Compound: S/GSK-1349572
    Cytotoxicity against human IM9 cells after 2 days by Cell titer Glo luminescent assay
    Cytotoxicity against human IM9 cells after 2 days by Cell titer Glo luminescent assay
    		[PMID: 21115794]
    MOLT-4 CC50
    15 μM
    Compound: S/GSK-1349572
    Cytotoxicity against human MOLT4 cells after 2 days by Cell titer Glo luminescent assay
    Cytotoxicity against human MOLT4 cells after 2 days by Cell titer Glo luminescent assay
    		[PMID: 21115794]
    MT2 EC50
    0.26 nM
    Compound: S/GSK-1349572
    Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect measured after 2 to 3 days by PCR
    Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect measured after 2 to 3 days by PCR
    		[PMID: 21115794]
    MT2 EC50
    0.26 nM
    Compound: S/GSK-1349572
    Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 14 passages measured after 2 to 3 days by PCR
    Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 14 passages measured after 2 to 3 days by PCR
    		[PMID: 21115794]
    MT2 EC50
    0.26 nM
    Compound: S/GSK-1349572
    Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 28 passages measured after 2 to 3 days by PCR
    Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 28 passages measured after 2 to 3 days by PCR
    		[PMID: 21115794]
    MT2 EC50
    0.26 nM
    Compound: S/GSK-1349572
    Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 42 passages measured after 2 to 3 days by PCR
    Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 42 passages measured after 2 to 3 days by PCR
    		[PMID: 21115794]
    MT2 EC50
    1.3 nM
    Compound: S/GSK-1349572
    Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 56 passages measured after 2 to 3 days by PCR
    Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 56 passages measured after 2 to 3 days by PCR
    		[PMID: 21115794]
    MT2 EC50
    1.3 nM
    Compound: S/GSK-1349572
    Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase S153Y/L101I/T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 70 passages measured after 2 to 3 day
    Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase S153Y/L101I/T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 70 passages measured after 2 to 3 day
    		[PMID: 21115794]
    MT2 EC50
    1.3 nM
    Compound: S/GSK-1349572
    Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase S153Y/L101I/T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 84 passages measured after 2 to 3 day
    Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase S153Y/L101I/T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 84 passages measured after 2 to 3 day
    		[PMID: 21115794]
    MT2 EC50
    1.3 nM
    Compound: S/GSK-1349572
    Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase S153Y/L101I/T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 98 passages measured after 2 to 3 day
    Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase S153Y/L101I/T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 98 passages measured after 2 to 3 day
    		[PMID: 21115794]
    MT2 EC50
    1.3 nM
    Compound: S/GSK-1349572
    Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase S153Y/L101I/T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 112 passages measured after 2 to 3 da
    Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase S153Y/L101I/T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 112 passages measured after 2 to 3 da
    		[PMID: 21115794]
    MT4 EC50
    0.36 nM
    Compound: S/GSK-1349572
    Antiviral activity against PI-resistant Human immunodeficiency virus 1 NL432 harboring nucleotide reverse transcriptase L24I/M46I/L63P/A71V/G73S/V82Tmutant infected in human MT4 cells after 2 to 3 days by reverse transcriptase activity
    Antiviral activity against PI-resistant Human immunodeficiency virus 1 NL432 harboring nucleotide reverse transcriptase L24I/M46I/L63P/A71V/G73S/V82Tmutant infected in human MT4 cells after 2 to 3 days by reverse transcriptase activity
    		[PMID: 21115794]
    MT4 EC50
    0.71 nM
    Compound: S/GSK-1349572
    Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as viral viability after 4 to 5 days by Cell titer Glo luminescent assay
    Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as viral viability after 4 to 5 days by Cell titer Glo luminescent assay
    		[PMID: 21115794]
    MT4 CC50
    14 μM
    Compound: S/GSK-1349572
    Cytotoxicity against human MT4 cells after 2 days by Cell titer Glo luminescent assay
    Cytotoxicity against human MT4 cells after 2 days by Cell titer Glo luminescent assay
    		[PMID: 21115794]
    PBMC CC50
    189 μM
    Compound: S/GSK-1349572
    Cytotoxicity against PHA-stimulated human PBMC after 2 days by Cell titer Glo luminescent assay
    Cytotoxicity against PHA-stimulated human PBMC after 2 days by Cell titer Glo luminescent assay
    		[PMID: 21115794]
    PBMC CC50
    52 μM
    Compound: S/GSK-1349572
    Cytotoxicity against unstimulated human PBMC after 2 days by Cell titer Glo luminescent assay
    Cytotoxicity against unstimulated human PBMC after 2 days by Cell titer Glo luminescent assay
    		[PMID: 21115794]
    U-937 CC50
    7 μM
    Compound: S/GSK-1349572
    Cytotoxicity against human U937 cells after 2 days by Cell titer Glo luminescent assay
    Cytotoxicity against human U937 cells after 2 days by Cell titer Glo luminescent assay
    		[PMID: 21115794]
    體外研究
    (In Vitro)

    Dolutegravir (S/GSK1349572) 針對(duì) PBMC 中 HIV-1 的 EC50 為 0.51 nM，在 MT-4 細(xì)胞中為 0.71 nM，在 PHIV 測(cè)定中為 2.2 nM，其使用假型自滅活病毒。Dolutegravir 在增殖的 IM-9、U-937、MT-4 和 Molt-4 細(xì)胞中的 50% 細(xì)胞毒性濃度 (CC50) 分別為 4.8、7.0、14 和 15 μM。在未刺激和刺激的 PBMC 中，CC50 分別為 189 μM 和 52 μM?；诙嗵胬f對(duì) PBMC 中 HIV-1 的 EC50 (即 0.51 nM)，這轉(zhuǎn)化為基于細(xì)胞的治療指數(shù)至少為9,400[1]。

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

    單次靜脈內(nèi) (IV) 給藥 Dolutegravir 后，血漿清除率在大鼠 (0.23 mL/min/kg) 和猴子 (2.12 mL/min/kg) 中較低。在大鼠和猴體內(nèi)的半衰期相似，約為 6 小時(shí)，穩(wěn)態(tài)分布容積 (VSS) 較低?？诜?，Dolutegravir 被快速吸收，當(dāng)作為溶液給予禁食的雄性大鼠和一只猴子時(shí)具有高口服生物利用度 (分別為 75.6 和 87.0%)。Dolutegravir 暴露 (Cmax 和 AUC) 隨著劑量的增加而增加，在對(duì)非禁食大鼠和非禁食猴子口服給藥高達(dá) 250 mg/kg 和高達(dá) 50 mg/kg 的懸浮液后，盡管增加小于比例[2]。

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

    441.36

    Formula

    C20H18F2N3NaO5
    CAS 號(hào)
    性狀

    固體

    顏色

    Off-white to yellow

    中文名稱

    度魯特韋鈉鹽
    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 : 2 mg/mL (4.53 mM; 超聲助溶 (<60°C); 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)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.2657 mL 11.3286 mL 22.6572 mL
    5 mM --- --- ---
    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

    只
    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

    純度: 99.97%

    參考文獻(xiàn)
    Cell Assay
    [1]

    In vitro growth inhibition (cytotoxicity) studies are conducted with S/GSK1349572 (0.16, 0.8, 4, and 20 nM) in proliferating human leukemic and lymphomic cell lines (IM-9, U-937, MT-4, and Molt-4) as well as in stimulated and unstimulated human PBMCs. ATP levels are quantified by using the CellTiter-Glo luciferase reagent to measure the ability of a compound to inhibit cell growth as an indicator of the compound's potential for cytotoxicity[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    For rat and monkey PK studies, Dolutegravir is administered as the free acid or the sodium salt. All doses are presented in terms of the free acid. Dolutegravir is administered by intravenous (IV) short-term (within 2 min) bolus (1 mg/kg) to three male rats and two male monkeys. For single oral administration, Dolutegravir as a solution (5 mg/kg) is administered to three fasted male rats and two fasted male monkeys. Dolutegravir is administered as single oral doses of 5, 50, 100, and 250 mg/kg to non-fasted male rats (n=2/dose level) and 3, 10, and 50 mg/kg to non-fasted female monkeys. For intravenous administration, blood samples are collected from rats (0.2 mL via jugular vein cannula) and monkeys (approximately 0.2 or 0.5 mL via saphenous vein in a hindlimb) into Na2EDTA-treated syringes at 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, and 24 h. For oral administration, samples are collected at 0.25 (rats only), 0.5, 1, 2, 4, 6 [rats (solution and suspension) and monkey (solution only)], 8, and 24 h. Following collection, the blood is immediately put on wet ice and then centrifuged within an hour at 1740 g for 10 min at 4°C to obtain plasma. All samples are stored at approximately -20°C or colder prior to analysis by using a method based on protein precipitation and LC-MS/MS analysis.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    參考文獻(xiàn)

    Dolutegravir sodium 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 2.2657 mL 11.3286 mL 22.6572 mL 56.6431 mL
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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：
    Dolutegravir sodium
    目錄號(hào)：
    HY-13238A
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