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  2. Anti-infection
  3. HBV
  4. Morphothiadin

Morphothiadin  (Synonyms: 莫非賽定; GLS4)

目錄號: HY-108917 純度: 99.84%
COA 產(chǎn)品使用指南

Morphothiadin 是野生型和阿德福韋耐藥 HBV 復(fù)制的有效抑制劑，其 IC50 值為 12 nM。

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Morphothiadin Chemical Structure

Morphothiadin Chemical Structure

CAS No. : 1092970-12-1

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥3960
In-stock
1 mg ￥1200
In-stock
5 mg ￥3600
In-stock
10 mg ￥5700
In-stock
50 mg   詢價  
100 mg   詢價  

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Customer Review

  • 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

Morphothiadin is a potent inhibitor on the replication of both wild-type and adefovir-resistant HBV with an IC50 of 12 nM.

IC50 & Target

IC50: 12 nM (HBV)[1]
細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
CCRF-CEM CC50
68.7 μM
Compound: GLS4
Cytotoxicity against human CEM cells assessed as reduction in cell viability by MTT assay
Cytotoxicity against human CEM cells assessed as reduction in cell viability by MTT assay
[PMID: 33421915]
CCRF-CEM CC50
69 μM
Compound: GLS4
Cytotoxicity against human CEM cells assessed as growth inhibition by CellTiter 96 non-radioactive cell proliferation colorimetric assay
Cytotoxicity against human CEM cells assessed as growth inhibition by CellTiter 96 non-radioactive cell proliferation colorimetric assay
[PMID: 28094179]
HEK293 IC50
0.86 μM
Compound: GLS4; GLS4JHS
Inhibition of human ERG expressed in HEK293 cells at -80 mV holding potential by manual-patch-clamp electrophysiology assay
Inhibition of human ERG expressed in HEK293 cells at -80 mV holding potential by manual-patch-clamp electrophysiology assay
[PMID: 29381358]
HepG2 CC50
> 100 μM
Compound: GLS4
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by MTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by MTT assay
[PMID: 33421915]
HepG2 CC50
> 100 μM
Compound: GLS4
Cytotoxicity against human HepG2 cells assessed as growth inhibition by CellTiter 96 non-radioactive cell proliferation colorimetric assay
Cytotoxicity against human HepG2 cells assessed as growth inhibition by CellTiter 96 non-radioactive cell proliferation colorimetric assay
[PMID: 28094179]
HepG2 IC50
0.012 μM
Compound: 5; GLS4
Inhibition of HBV DNA replication in HepG2 cells by southern blot analysis
Inhibition of HBV DNA replication in HepG2 cells by southern blot analysis
10.1039/C4MD00521J
HepG2 2.2.15 CC50
> 45 μM
Compound: 8n
Cytotoxicity in human HepG2.215 cells assessed as reduction in cell viability after 5 days by CCK8 assay
Cytotoxicity in human HepG2.215 cells assessed as reduction in cell viability after 5 days by CCK8 assay
[PMID: 28082068]
HepG2 2.2.15 EC50
0.0066 μM
Compound: GLS4
Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as reduction in viral DNA levels incubated for 6 days by PCR analysis
Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as reduction in viral DNA levels incubated for 6 days by PCR analysis
[PMID: 32421339]
PBMC CC50
28 μM
Compound: GLS4
Cytotoxicity against human PBMC assessed as growth inhibition by CellTiter 96 non-radioactive cell proliferation colorimetric assay
Cytotoxicity against human PBMC assessed as growth inhibition by CellTiter 96 non-radioactive cell proliferation colorimetric assay
[PMID: 28094179]
PBMC CC50
28.4 μM
Compound: GLS4
Cytotoxicity against human PBMC cells assessed as reduction in cell viability by MTT assay
Cytotoxicity against human PBMC cells assessed as reduction in cell viability by MTT assay
[PMID: 33421915]
Vero CC50
17.7 μM
Compound: GLS4
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability by MTT assay
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability by MTT assay
[PMID: 33421915]
Vero CC50
18 μM
Compound: GLS4
Cytotoxicity against African green monkey Vero cells assessed as growth inhibition by CellTiter 96 non-radioactive cell proliferation colorimetric assay
Cytotoxicity against African green monkey Vero cells assessed as growth inhibition by CellTiter 96 non-radioactive cell proliferation colorimetric assay
[PMID: 28094179]
體外研究
(In Vitro)

莫爾福噻啶是一種強(qiáng)效的抑制劑，對野生型和阿德福韋耐藥的乙型肝炎病毒（HBV）復(fù)制均有抑制作用，其半數(shù)抑制濃度（IC50）為12 nM。莫爾福噻啶（GLS4）在高達(dá)25 μM的濃度下未顯示出毒性。對于原代肝細(xì)胞，莫爾福噻啶的半數(shù)細(xì)胞毒性濃度（CC50）為115 μM（P<0.001）。在HepAD38細(xì)胞中，莫爾福噻啶的90%細(xì)胞毒性濃度（CC90）為190 μM（P<0.01）。莫爾福噻啶在25 nM至100 nM的濃度范圍內(nèi)強(qiáng)烈抑制HepAD38細(xì)胞上清液中的病毒積累（P<0.02）。結(jié)果顯示，用莫爾福噻啶處理的細(xì)胞中核心蛋白含量呈濃度依賴性減少[2]。

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

莫爾福噻啶（Morphothiadin, GLS4）從0到24小時的血藥濃度-時間曲線下面積（AUC0-24）為556 h·ng/mL。靜脈給予10 mg/kg莫爾福噻啶后，其總血漿清除率和表觀分布容積分別為4.2升/小時/千克和7.38升/千克。莫爾福噻啶的生物利用度為25.5%。研究發(fā)現(xiàn)，每日給予3.75 mg/kg莫爾福噻啶處理的小鼠病毒滴度增加了83.5倍，而每日給予7.5 mg/kg的小鼠病毒滴度增加了28.3倍，但對于使用更高劑量莫爾福噻啶處理的小鼠，病毒滴度僅增加了3至6倍。通常情況下，莫爾福噻啶劑量與病毒滴度呈負(fù)相關(guān)關(guān)系，其中每日給予3.75 mg/kg莫爾福噻啶的小鼠表現(xiàn)出最大的反彈（540倍），而每日給予60 mg/kg莫爾福噻啶的小鼠則表現(xiàn)出最小的反彈（23倍）（P<0.001）。大于7.5 mg/kg/天的莫爾福噻啶劑量在整個治療期間顯著抑制了病毒復(fù)制周期，而大于15 mg/kg/天的劑量則在治療結(jié)束后長達(dá)兩周內(nèi)持續(xù)抑制病毒[2]。

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

509.39

Formula

C21H22BrFN4O3S
CAS 號
性狀

固體

顏色

Light yellow to yellow

中文名稱

莫非賽定
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 : 62.5 mg/mL (122.70 mM; 超聲助溶 (<60°C); 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 1.9631 mL 9.8157 mL 19.6313 mL
5 mM 0.3926 mL 1.9631 mL 3.9263 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，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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: ≥ 3 mg/mL (5.89 mM); 澄清溶液

    此方案可獲得 ≥ 3 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 30.0 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% Corn Oil

    Solubility: ≥ 3 mg/mL (5.89 mM); 澄清溶液

    此方案可獲得 ≥ 3 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 30.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中，混合均勻。

動物溶解方案計算器
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: 99.84%

參考文獻(xiàn)
Cell Assay
[2]

HepAD38 cells are grown to about 80% confluence in 0.3 μg/mL of tetracycline (TET). After the removal of TET, the cells are treated with different doses of Morphothiadin (GLS4), or no drug. Cell viability is monitored by 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay[2].

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

ICR mice are used to evaluate the pharmacokinetic (PK) properties of Morphothiadin (GLS4). Following oral administration of 10 mg/kg (of body weight) of Morphothiadin to male mice, the concentration of Morphothiadin in plasma is determined using liquid chromatography-tandem mass spectrometry (LC/MS/MS). For toxicity studies, ICR mice are given Morphothiadin by gavage over a 4-week period and then kept off drug for another 2 weeks. Groups consisting of 20 male plus 20 female mice are administered a vehicle (1% methyl-2-hydroxyethyl cellulose), 35.7, 118.9, or 356.6 mg/kg per day in a volume corresponding to 20 mL/kg. Ten mice per dose group are euthanized 2 weeks after the end of drug treatment. Body weight, food consumption, serum albumin levels, and adverse effects are determined[2].

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

Morphothiadin 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，請在2年內(nèi)使用， -20°C儲存時，請在1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 1.9631 mL 9.8157 mL 19.6313 mL 49.0783 mL
5 mM 0.3926 mL 1.9631 mL 3.9263 mL 9.8157 mL
10 mM 0.1963 mL 0.9816 mL 1.9631 mL 4.9078 mL
15 mM 0.1309 mL 0.6544 mL 1.3088 mL 3.2719 mL
20 mM 0.0982 mL 0.4908 mL 0.9816 mL 2.4539 mL
25 mM 0.0785 mL 0.3926 mL 0.7853 mL 1.9631 mL
30 mM 0.0654 mL 0.3272 mL 0.6544 mL 1.6359 mL
40 mM 0.0491 mL 0.2454 mL 0.4908 mL 1.2270 mL
50 mM 0.0393 mL 0.1963 mL 0.3926 mL 0.9816 mL
60 mM 0.0327 mL 0.1636 mL 0.3272 mL 0.8180 mL
80 mM 0.0245 mL 0.1227 mL 0.2454 mL 0.6135 mL
100 mM 0.0196 mL 0.0982 mL 0.1963 mL 0.4908 mL
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產(chǎn)品名稱：
Morphothiadin
目錄號：
HY-108917
需求量：