Daclatasvir (BMS-790052)

別名: EBP883 中文名稱：達(dá)卡他韋

目錄號(hào)：S1482 Purity: 99.70%

Daclatasvir (BMS-790052, EBP883) 是一種高度選擇性的HCV NS5A抑制劑，EC50為9-50 pM，在細(xì)胞培養(yǎng)中，作用于多種HCV復(fù)制基因型和JFH-1基因型2a的感染性病毒。Phase 3。

Daclatasvir (BMS-790052) Chemical Structure

CAS: 1009119-64-5

規(guī)格	價(jià)格	庫(kù)存
5mg	1373.65	現(xiàn)貨
50mg	7941.93	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次：純度： 99.70%

99.70

Daclatasvir (BMS-790052)相關(guān)產(chǎn)品

相關(guān)產(chǎn)品	Lomibuvir (VX-222) Danoprevir Asunaprevir PSI-6206 (GS-331007)	點(diǎn)擊展開
相關(guān)化合物庫(kù)	FDA藥物庫(kù) 天然產(chǎn)物庫(kù) 已知活性藥物庫(kù)-I 蛋白酶抑制劑庫(kù) 泛素化化合物庫(kù)	點(diǎn)擊展開

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	給藥濃度	孵育時(shí)間	活性描述	文獻(xiàn)信息
GS4.3	Antiviral assay	0.15 uM	6 days	Antiviral activity against HCV infected in human GS4.3 cells assessed as inhibition of NS3/4A levels at 0.15 uM treated with fresh media containing compound every 2 days measured after 6 days by Western blot method	29232582
GS4.3	Antiviral assay	0.15 uM	6 days	Antiviral activity against HCV infected in human GS4.3 cells assessed as inhibition of viral core protein levels at 0.15 uM treated with fresh media containing compound every 2 days measured after 6 days by Western blot method	29232582
Huh7.5.1	Antiviral assay	100 pM to 1 uM		Antiviral activity against HCV genotype 1b NK/R2AN infected in human Huh7.5.1 cells expressing NS5A L31V mutant assessed as reduction in virus replication at 100 pM to 1 uM by luciferase reporter gene assay	26134551
Huh7.5.1	Antiviral assay	100 pM to 1 uM		Antiviral activity against HCV genotype 1b NK/R2AN infected in human Huh7.5.1 cells expressing NS5A Y93H mutant assessed as reduction in virus replication at 100 pM to 1 uM by luciferase reporter gene assay	26134551
Huh-luc/neo-ET replicon	Antiviral assay		48 hrs	Antiviral activity against Hepatitis C virus genotype 1b harboring NS5A L28V mutant gene in Huh-luc/neo-ET replicon cells after 48 hrs by transient replicon mutant-based luciferase assay, EC50=0.000004μM	24568313
Huh7	Antiviral assay		3 days	Antiviral activity against HCV genotype 1b infected in human Huh7 cells after 3 days by cell-based replicon assay, EC50=0.000003μM	25148100
human CEM cells	Cytotoxicity assay		3 days	Cytotoxicity against human CEM cells after 3 days, CC50=9.6 μM	25154714
HuH-Lcu-Neo	Function assay		48 hrs	Inhibition of NS5A in HCV genotype 1b infected in HuH-Lcu-Neo cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter gene assay, EC50=0.0000081μM	32202782
Huh-5.2	Antiviral assay		4 days	Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh-5.2 cells assessed as decrease in HCV replicon RNA replication after 4 days by luciferase assay, EC50=0.000009μM	24900811
HuH7	Antiviral assay		3 days	Antiviral activity against HCV genotype 1b Con1 infected in human HuH7 cells assessed as inhibition of viral RNA replication after 3 days by renilla luciferase reporter gene assay, EC50=0.000009μM	24320933
HuH7	Antiviral assay		72 hrs	Antiviral activity against HCV1b infected in human HuH7 cells assessed as inhibition of viral replication after 72 hrs by FRET assay, EC50=0.000009μM	24521299
Huh7.5/J6/JFH1/EMCVIRES/hRlucNeo	Function assay		72 hrs	Inhibition of NS5A in HCV genotype 2a infected in human Huh7.5/J6/JFH1/EMCVIRES/hRlucNeo cells assessed as inhibition of replicon levels incubated for 72 hrs by luciferase reporter gene assay, IC50=0.000009μM	31710479
HuH7 replicon	Function assay		2 days	Inhibition of NS5A in HCV genotype 1b infected in human HuH7 replicon cells assessed as reduction in subgenomic viral RNA replication treated for 2 days followed by compound washout and subsequent compound dosing measured after 1 day by SEAP reporter gene, EC50=0.000009μM	30772607
Huh-luc/neo-ET replicon	Antiviral assay		48 hrs	Antiviral activity against Hepatitis C virus genotype 1b in Huh-luc/neo-ET replicon cells after 48 hrs by replicon-based luciferase assay, EC50=0.00001μM	24568313
HuH7.5/Con1/SG-Neo(I)-hRluc2aUb	Function assay		72 hrs	Inhibition of NS5A in HCV genotype 1b infected in human HuH7.5/Con1/SG-Neo(I)-hRluc2aUb cells assessed as inhibition of replicon levels incubated for 72 hrs by luciferase reporter gene assay, IC50=0.000023μM	31710479
HuH-Lcu-Neo	Function assay		48 hrs	Inhibition of NS5A in HCV genotype 1a infected in HuH-Lcu-Neo cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter gene assay, EC50=0.0000324μM	32202782
Huh-luc/neo-ET replicon	Antiviral assay		48 hrs	Antiviral activity against Hepatitis C virus genotype 1a in Huh-luc/neo-ET replicon cells after 48 hrs by replicon-based luciferase assay, EC50=0.0000398μM	24568313
W11.8	Antiviral assay		4 days	Antiviral activity against Hepatitis C virus genotype 1a infected in W11.8 cells assessed as decrease in NS5A expression in replicon cell after 4 days by luminescence based ELISA, EC50=0.00005μM	24900811
HuH7	Antiviral assay		3 days	Antiviral activity against HCV genotype 1a H77 infected in human HuH7 cells assessed as inhibition of viral RNA replication after 3 days by renilla luciferase reporter gene assay, EC50=0.00005μM	24320933
HuH7	Antiviral assay		72 hrs	Antiviral activity against HCV1a infected in human HuH7 cells assessed as inhibition of viral replication after 72 hrs by FRET assay, EC50=0.00005μM	24521299
HuH-Lcu-Neo	Function assay		48 hrs	Inhibition of NS5A in patient-derived HCV genotype 3a infected in HuH-Lcu-Neo cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter gene assay, EC50=0.0001145μM	32202782
Huh-luc/neo-ET replicon	Antiviral assay		48 hrs	Antiviral activity against Hepatitis C virus genotype 1b harboring NS5A L31V mutant gene in Huh-luc/neo-ET replicon cells after 48 hrs by transient replicon mutant-based luciferase assay, EC50=0.0001259μM	24568313
Huh-luc/neo-ET replicon	Antiviral assay		48 hrs	Antiviral activity against Hepatitis C virus genotype 1b harboring NS5A Y93H mutant gene in Huh-luc/neo-ET replicon cells after 48 hrs by transient replicon mutant-based luciferase assay, EC50=0.0003162μM	24568313
HuH7	Antiviral assay		72 hrs	Antiviral activity against HCV1a infected in human HuH7 cells assessed as inhibition of viral replication after 72 hrs by FRET assay, EC90=0.00038μM	24521299
HuH-Lcu-Neo	Function assay		48 hrs	Inhibition of NS5A in HCV genotype 3a con infected in HuH-Lcu-Neo cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter gene assay, EC50=0.0004115μM	32202782
HuH-Lcu-Neo	Function assay		48 hrs	Inhibition of NS5A in patient-derived HCV genotype 2a infected in HuH-Lcu-Neo cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter gene assay, EC50=0.0494μM	32202782
HuH-Lcu-Neo	Function assay		48 hrs	Inhibition of NS5A in HCV genotype 2a con infected in HuH-Lcu-Neo cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter gene assay, EC50=0.05285μM	32202782
CEM	Cytotoxicity assay		3 days	Cytotoxicity against human CEM cells after 3 days, CC50=9.6μM	22507961
Vero	Cytotoxicity assay		3 days	Cytotoxicity against african green monkey Vero cells after 3 days, CC50=21μM	22507961
HuH7	Antiviral assay		3 days	Antiviral activity against HCV genotype 1b infected in human HuH7 cells at >= 10 times antiviral EC50 after 3 days by luciferase reporter assay	28430437
HuH7	Antiviral assay		3 days	Antiviral activity against HCV genotype 1b infected in human HuH7 cells co-treated with asunaprevir after 3 days by luciferase reporter assay	28430437
HuH7	Antiviral assay			Antiviral activity against HCV genotype 1b infected in human HuH7 cells assessed as reduction in viral RNA replication, EC50=0.000004μM	26099532
HuH7	Antiviral assay			Antiviral activity against HCV1b infected in human HuH7 cells assessed as inhibition of viral replication by RT-PCR analysis, EC50=0.0000066μM	22507961
HuH7	Antiviral assay			Antiviral activity against HCV genotype 1b Con1 infected in human HuH7 cells assessed as inhibition of viral replication, EC50=0.000009μM	26077493
HuH7	Antiviral assay			Antiviral activity against HCV 1b infected in human HuH7 cells by in vitro replicon assay, EC50=0.00001μM	23466233
HuH7	Function assay			Inhibition of NS5A in HCV genotype-1b infected in human HuH7 cells by luciferase reporter gene assay, EC50=0.000023μM	25453810
HuH7	Antiviral assay			Antiviral activity against HCV genotype 1b JFH-1 infected in human HuH7 cells assessed as inhibition of viral replication, EC50=0.000028μM	26077493
HuH7	Antiviral assay			Antiviral activity against HCV 1b infected in human HuH7 cells by in vitro replicon assay, EC90=0.00003μM	23466233
HuH7	Antiviral assay			Antiviral activity against HCV genotype 1b expressing NS5A L31V mutant infected in human HuH7 cells assessed as reduction in viral RNA replication, EC50=0.000035μM	26099532
HuH7	Antiviral assay			Antiviral activity against wild type HCV genotype 1b infected in human HuH7 cells assessed as reduction in viral RNA replication, EC50=0.000048μM	26099532
HuH7	Antiviral assay			Antiviral activity against HCV genotype 5a infected in human HuH7 cells by luciferase reporter gene assay, EC50=0.000051μM	25453811
HuH7	Antiviral assay			Antiviral activity against HCV genotype 1b infected in human HuH7 cells by luciferase reporter gene assay, EC50=0.000073μM	25453811
HuH7	Function assay			Inhibition of NS5A in HCV genotype-1a infected in human HuH7 cells by luciferase reporter gene assay, EC50=0.00014μM	25453810
HuH7	Antiviral assay			Antiviral activity against HCV genotype 1a infected in human HuH7 cells by luciferase reporter gene assay, EC50=0.00014μM	25453811
HuH7	Antiviral assay			Antiviral activity against HCV genotype 1b expressing NS5A Y93H mutant infected in human HuH7 cells assessed as reduction in viral RNA replication, EC50=0.00018μM	26099532
HuH7	Antiviral assay			Antiviral activity against HCV genotype 4a infected in human HuH7 cells by luciferase reporter gene assay, EC50=0.00041μM	25453811
HuH7	Antiviral assay			Antiviral activity against HCV genotype 6a infected in human HuH7 cells by luciferase reporter gene assay, EC50=0.00045μM	25453811
HuH7	Antiviral assay			Antiviral activity against HCV genotype 3a infected in human HuH7 cells by luciferase reporter gene assay, EC50=0.00067μM	25453811
HuH7	Antiviral assay			Antiviral activity against HCV genotype 2a infected in human HuH7 cells by luciferase reporter gene assay, EC50=0.00067μM	25453811
CEM	Cytotoxicity assay			Cytotoxicity against human CEM cells, CC50=9.6μM	22704887
Vero	Cytotoxicity assay			Cytotoxicity against african green monkey Vero cells, CC50=9.6μM	23466233
CEM	Cytotoxicity assay			Cytotoxicity against human CEM cells, CC50=10μM	26099532
PBMC	Cytotoxicity assay			Cytotoxicity against human PBMC cells, CC50=19μM	22704887
Vero	Cytotoxicity assay			Cytotoxicity against african green monkey Vero cells, CC50=21μM	22704887
CEM	Cytotoxicity assay			Cytotoxicity against human CEM cells, CC50=21μM	23466233
Vero	Cytotoxicity assay			Cytotoxicity against african green monkey Vero cells, CC50=21μM	26099532
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

特性

BMS-790052是一流的高選擇性C型肝炎病毒(HCV) NS5A抑制劑， EC50為皮摩爾級(jí)。

靶點(diǎn)

HCV NS5A ^[1]

9 pM-50 pM(EC50)

體外研究(In Vitro)
體外研究活性	BMS-790052是到目前為止報(bào)道的最有效的HCV復(fù)制抑制劑之一,作用于HCV基因型1a和1b復(fù)制子時(shí)EC50分別為50和9?pM。 BMS-790052治療指數(shù)(CC50/EC50)為10⁵以上，對(duì)一組10種RNA和DNA病毒沒有作用效果, EC50大于10?μM, BMS-790052只針對(duì)HCV有效。^[1] BMS-790052作用于含HCV基因型1b復(fù)制子的Huh7細(xì)胞, BMS-790052抑制短暫和穩(wěn)定的HCV染色體復(fù)制, EC50為1-15 pM。BMS-790052 (100 pM或1 nM)改變NS5A的亞細(xì)胞定位和生化結(jié)構(gòu)。^[2] BMS-790052抑制含HCV基因型-4 NS5A基因的雜合復(fù)制子，EC50為7-13 pM。雜合復(fù)制子中的NS5A殘基30是BMS-790052選擇耐抗性的一個(gè)重要位點(diǎn)。^[3]
激酶實(shí)驗(yàn)	針對(duì)HCV NS5A抑制劑的FRET實(shí)驗(yàn)
激酶實(shí)驗(yàn)	肽段 (Ac-Asp-Glu-Asp [EDANS]-Glu-Glu-Abu-[COO] Ala-Ser-Lys [DABCYL]-NH2)含熒光供體{EDANS, 5-[(2-氨乙基)氨基]萘-1-磺酸} ，位于肽段一端；受體 {DABCYL, 4-[4-(二甲基氨基)苯偶氮]苯甲酸}，位于肽段另一端。通過在供體和受體之間分子能量共振轉(zhuǎn)移使肽段熒光淬滅，NS3蛋白酶使肽段斷裂，共振能量轉(zhuǎn)移淬滅使產(chǎn)物釋放，供體的熒光隨著底物被NS3蛋白酶降解的時(shí)間而增強(qiáng)。反應(yīng)所用試劑如下：5×熒光素酶細(xì)胞培養(yǎng)液用dH₂O稀釋到1×,NaCl (150 mM), FRET肽(20 μM)。HCV-Huh-7細(xì)胞按每孔1×10⁴個(gè)接種在96孔板上，粘附過夜。第二天, BMS-790052加到孔中，溫育72小時(shí)。用PBS沖洗板，每孔加入30 μL FRET肽實(shí)驗(yàn)試劑進(jìn)行FRET實(shí)驗(yàn)。使用Cytofluor 4000儀測(cè)定吸光值。隨后，40 μL熒光素酶底物加到每孔中，測(cè)定熒光值。
細(xì)胞實(shí)驗(yàn)	細(xì)胞系	HCV復(fù)制子細(xì)胞(Huh7)
	濃度	0.1 pM-50 μM, 溶于DMSO，最終DMSO濃度為0.5%
	孵育時(shí)間	72小時(shí)
	方法	細(xì)胞接種在96孔板上的200μL培養(yǎng)基中，12小時(shí)后，BMS-790052加到含HCV復(fù)制子的96孔板上。溫育72小時(shí)，測(cè)定復(fù)制活性和細(xì)胞毒性。使用CellTiter-Blue測(cè)定細(xì)胞毒性。隨后，移除培養(yǎng)基和染料，使板倒轉(zhuǎn)，殘留的液體用紙巾吸干，使用Renilla熒光素酶測(cè)定HCV 基因型1a細(xì)胞系的復(fù)制活性。1×Renilla熒光素酶溶解buffer (30 μL)加到每孔中，溫和震蕩15分鐘。加入Renilla熒光素酶底物(40 μL)，使用Top Count光度計(jì)測(cè)定信號(hào)。

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗(yàn)信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05992077	Recruiting	HCV Infection	ANRS Emerging Infectious Diseases	August 7 2023	Not Applicable
NCT04852614	Recruiting	Hepatitis C Virus Infection	Ain Shams University	December 1 2020	--
NCT04773756	Completed	Covid19	Alexandria University	November 1 2020	Phase 4
NCT03208322	Withdrawn	Hepatitis C	Bristol-Myers Squibb	November 30 2018	--

參考文獻(xiàn)
[1] Gao M, et al. Nature, 2010, 465(7294), 96-100. [2] Lee C, et al. Virology, 2011, 414(1), 10-18. [3] Wang C, et al. Antimicrob Agents Chemother, 2012, 56(3), 1588-1590. [4] O'Boyle DR 2nd, et al. Antimicrob Agents Chemother, 2005, 49(4), 1346-1353. + 展開

參考文獻(xiàn)

[1] Gao M, et al. Nature, 2010, 465(7294), 96-100.
[2] Lee C, et al. Virology, 2011, 414(1), 10-18.
[3] Wang C, et al. Antimicrob Agents Chemother, 2012, 56(3), 1588-1590.

[4] O'Boyle DR 2nd, et al. Antimicrob Agents Chemother, 2005, 49(4), 1346-1353.

+ 展開

化學(xué)信息&溶解度

分子量	738.88	分子式	C₄₀H₅₀N₈O₆
CAS號(hào)	1009119-64-5	SDF	Download Daclatasvir (BMS-790052) SDF
Smiles	CC(C)C(C(=O)N1CCCC1C2=NC=C(N2)C3=CC=C(C=C3)C4=CC=C(C=C4)C5=CN=C(N5)C6CCCN6C(=O)C(C(C)C)NC(=O)OC)NC(=O)OC
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1個(gè)月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 148 mg/mL ( (200.3 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Ethanol : 148 mg/mL (200.3 mM)

Water : Insoluble

DMSO : 148 mg/mL ( (200.3 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Ethanol : 148 mg/mL (200.3 mM)

Water : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

給藥劑量 mg/kg 動(dòng)物平均體重 g 每只動(dòng)物給藥體積 μL 動(dòng)物數(shù)量只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
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