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  1. Anti-infection
  2. HBV
  3. AB-423

AB-423 是一種 HBV 衣殼組裝抑制劑,在細(xì)胞中,能夠抑制 HBV 復(fù)制,EC50/EC90 值分別為 0.08-0.27 μM/0.33-1.32 μM。

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AB-423 Chemical Structure

AB-423 Chemical Structure

CAS No. : 1572510-80-5

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Customer Review

Other Forms of AB-423:

  • 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

AB-423 is an inhibitor of HBV capsid assembly, and potent inhibits HBV replication with EC50/EC90 of 0.08-0.27 μM/0.33-1.32 μM in cells.

IC50 & Target

HBV capsid[1]

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
HepG2 2.2.15 EC50
0.28 μM
Compound: AB-423
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]
體外研究
(In Vitro)

AB-423 is an inhibitor of HBV capsid assembly. AB-423 shows inhibitory effect on rcDNA production in AML12-HBV10 and HepDE19 cells with EC50s of ~0.260 μM. AB-423 also suppresses cccDNA formation-dependent HBeAg production in the HepBHAe82 assay with an EC50 of 0.267 μM and inhibits HBV DNA levels in culture supernatants of HepG 2.2.15 cells with an EC50 of 0.134 μM. However, AB-423 has no cytotoxicity in any of the three cell lines[1].

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

體內(nèi)研究
(In Vivo)

AB-423 (30 and 100 mg/kg, p.o. bid) blocks HBV replication in a mouse model of HBV. AB-423 (100 mg/kg, p.o. bid) with entecavir (ETV, 100 ng/mg, qd, p.o.) or 0.1 mg/kg dose of ARB-1467 potently inhibits serum HBV DNA in an HDI model of HBV in immunodeficient NOD-SCID mice[1].

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

分子量

386.39

Formula

C17H17F3N2O3S

CAS 號(hào)
性狀

固體

顏色

White to off-white

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)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 (258.81 mM; 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)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.5881 mL 12.9403 mL 25.8806 mL
5 mM 0.5176 mL 2.5881 mL 5.1761 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, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?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(dòng)物實(shí)驗(yàn):

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)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(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)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(chǔ)備液可以根據(jù)儲(chǔ)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(qǐng)依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.47 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(chǔ)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(qǐng)依序添加每種溶劑: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.47 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,此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中,混合均勻。

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
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的動(dòng)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(gòu)。 Tween 80,均可在 MCE 網(wǎng)站選購(gòu)。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)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(chǔ)備液濃度超過該產(chǎn)品的實(shí)測(cè)溶解度,以下方案僅供參考,如有需要,請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)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(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)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: 99.31%

參考文獻(xiàn)
Cell Assay
[1]

To test the compound combinations, HepBHAe82 (50,000 cells/well) are plated in 96-well tissue-culture treated microtiter plates in DMEM/F12 medium supplemented with 10% fetal bovine serum, 1% penicillin-streptomycin and tetracycline (1 μg/mL), and incubated in a humidified incubator at 37°C and 5% CO2 overnight. On the next day, the cells are switched to fresh medium and treated with inhibitor A and inhibitor B, at concentration range in the vicinity of their respective EC50 values. The inhibitors are either diluted in 100% DMSO (ETV, TDF and AB-423) or growth medium (ARB-1467 and ARB-1740) and the final DMSO concentration in the assay is ≤0.5%. The two inhibitors are tested both singly as well as in combinations determine their effects on inhibition of rcDNA production. The final DMSO concentration in the assay is 0.5%. The plates are incubated for 9 days in a humidified incubator at 37°C and 5% CO2. Following a 9 day-incubation, medium is removed, and cells are subjected to RNA extraction to measure the cccDNA-dependent precore mRNA level[1].

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

Animal Administration
[1]

Mice[1]
Prior to start of treatment, 10 micrograms of the plasmid pHBV1.3 is administered to NOD.CB17-Prkdcscid/J mice via hydrodynamic injection (HDI; rapid high volume injection into the tail vein; n = 6 to 8 animals per group). This plasmid carries a 1.3-fold overlength copy of a HBV genotype D genome which, when expressed, generates hepatitis B viral particles and other HBV products. AB-423 is administered via oral gavage at 30 or 100 mg/kg twice-daily for 7 consecutive days, starting on Day 0. Entecavir (ETV) at 100 ng/kg once-daily for 7 consecutive days, starting on Day 0. ARB-1467 is administered as a single intravenous bolus tail vein injection at 0.1 mg/kg on Day 0. Blood is collected on Days 0 (pre-dose), 4 and 7 for HBV biomarker analysis. Serum HBV DNA concentration in mice is measured from total extracted DNA using a quantitative PCR assay using primer/probe sequences[1].

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

參考文獻(xiàn)

AB-423 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, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?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 2.5881 mL 12.9403 mL 25.8806 mL 64.7015 mL
5 mM 0.5176 mL 2.5881 mL 5.1761 mL 12.9403 mL
10 mM 0.2588 mL 1.2940 mL 2.5881 mL 6.4701 mL
15 mM 0.1725 mL 0.8627 mL 1.7254 mL 4.3134 mL
20 mM 0.1294 mL 0.6470 mL 1.2940 mL 3.2351 mL
25 mM 0.1035 mL 0.5176 mL 1.0352 mL 2.5881 mL
30 mM 0.0863 mL 0.4313 mL 0.8627 mL 2.1567 mL
40 mM 0.0647 mL 0.3235 mL 0.6470 mL 1.6175 mL
50 mM 0.0518 mL 0.2588 mL 0.5176 mL 1.2940 mL
60 mM 0.0431 mL 0.2157 mL 0.4313 mL 1.0784 mL
80 mM 0.0324 mL 0.1618 mL 0.3235 mL 0.8088 mL
100 mM 0.0259 mL 0.1294 mL 0.2588 mL 0.6470 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:
AB-423
目錄號(hào):
HY-112142
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