BMS-790052 dihydrochloride|1009119-65-6|(盐酸达拉他韦; BMS-790052 dihydrochloride; EBP 883 dihydrochloride)-陌孚医药/Medlife

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BMS-790052 dihydrochloride (Synonyms: 盐酸达拉他韦; BMS-790052 dihydrochloride; EBP 883 dihydrochloride)

目录号: PC15623 纯度: ≥98%

CAS No. :1009119-65-6

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中文名称	BMS-790052 dihydrochloride
中文别名	达卡他韦二盐酸盐;1-苯基-3-三氟甲基-1H-吡唑-4-甲醛;BMS790052,达卡他韦二盐酸盐;Daclatasvir丁二盐酸盐;N,N'-[[1,1'-联苯]-4,4'-二基双[1H-咪唑-5,2-二基-(2S)-2,1-吡咯烷二基[(1S)-1-(1-甲基乙基)-2-氧代-2,1-乙烷二基]]]二氨基甲酸二甲酯二盐酸盐;N,N’-[[1,1’-联苯]-4,4’-二基双[1H-咪唑-5,2-二基-(2S)-2,1-吡咯烷二基[(1S)-1-(1-甲基乙基)-2-氧代-2,1-乙烷二基]]]二氨基甲酸二甲酯二盐酸盐;达卡他韦;达卡他韦(二盐酸盐);达卡拉韦;达卡他韦盐;盐酸达拉他韦;盐酸达卡他韦;达卡他韦双盐酸盐;达卡他韦,达卡他韦二盐酸盐;吡咯烷二基[(1S)-1-(1-甲基乙基)-2-氧代-2,1-乙烷二基]]]二氨基甲酸二甲酯二盐酸盐
英文名称	BMS-790052 dihydrochloride
英文别名	BMS790052;Daclatasvir dihydrochloride;BMS790052 HCl;Daclatasvir (BMS-790052);methyl N-[(2S)-1-[(2S)-2-[5-[4-[4-[2-[(2S)-1-[(2S)-2-(methoxycarbonylamino)-3-methylbutanoyl]pyrrolidin-2-yl]-1H-imidazol-5-yl]phenyl]phenyl]-1H-imidazol-2-yl]pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl;N,N'-[[1,1'-Biphenyl]-4,4'-diylbis[1H-imidazole-5,2-diyl-(2S)-2,1-pyrrolidinediyl[(1S)-1-(1-methylethyl)-2-oxo-2,1-ethanediyl]]]biscarbamic acid dimethyl ester hydrochloride;BMS-790052 2HCl;BMS790052 dihydrochloride;BMS-790052 dihydrochloride;CS-0270;Daclatasvir;Daclatasvir dihydrochloride (USAN);Daclatasvir hydrochloride (JAN);methyl N-[(2S)-1-[(2S)-2-[5-[4-[4-[2-[(2S)-1-[(2S)-2-(methoxycarbonylamino)-3-methylbutanoyl]pyrrolidin-2-yl]-1H-imidazol-5-yl]phenyl]phenyl]-1H-imidazol-2-yl]pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]carbamate,dihydrochloride;Daclatasvir HCL;Daclatasvir API;DACLATASVIR(2HCl);daclatasvir hydrochloride;Dclatasvir dihydrochloride;Daclatavir Dihydrochloride;Daklinza;EBP 883;BMS 790052;C40H50N8O6;LI2427F9CI;methyl N-[(1S)-1-[(2S)-2-[5-[4-[4-[2-[(2S)-1-[(2S)-2-(methoxycarbonylamino)-3-methyl-butanoyl]pyrrolidin-2-yl]-1H-imidazol-5-yl]phenyl]phenyl]-1H-imidazol-2-yl]pyrrolidine-1-carbonyl]-2-methyl-propyl]carbamate;Daclatasvir (USAN);Daclatasvir BMS 790052;MLS006011140;EBP883;SCHE;Daclatasvir 2HCl;BMS790052.2HCl
Cas No.	1009119-65-6
分子式	C₄₀H₅₀N₈O₆
分子量	738.88
包装储存	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

Daclatasvir dihydrochloride (BMS-790052 dihydrochloride) is a potent and orally active HCV NS5A protein inhibitor with EC₅₀s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir dihydrochloride is also an organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC₅₀s of 1.5 μM and 3.27 μM, respectively.

性状

Solid

IC50 & Target[1][2]

EC50: 50 pM (HCV replicon genotype 1a), 9?pM (HCV replicon genotype 1b), 71 pM (HCV replicon genotype 2a), 146 pM (HCV replicon genotype 3a), 12 pM (HCV replicon genotype 4a) and 33 pM (HCV replicon genotype 5a)
Kd: 8 nM (NS5A33-202) and 210 nM (NS5A26-202)
IC50: 1.5 μM (OATP1B) and 3.27 μM (OATP1B3)

体外研究(In Vitro)

Daclatasvir (BMS-790052) demonstrates potent inhibitory activity towards all genotypes tested, with EC₅₀ values ranging from 9 pM to 146?pM. Daclatasvir inhibits HCV replicon genotype 1a, 1b, 2a, 3a, 4a and 5a with EC₅₀ values of 50 pM, 9?pM, 71 pM, 146 pM, 12 pM and 33 pM, respectively. Daclatasvir is a potent inhibitor of the JFH-1 genotype 2a infectious virus that replicates in cell culture (EC₅₀=28 pM). Daclatasvir (BMS-790052) binds tightly to NS5A33-202 and NS5A26-202 with K_ds of 8 nM and 210 nM, respectively.

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

体内研究(In Vivo)

Daclatasvir (BMS-790052; 30?mg/kg; oral administration; daily; for 27 days) treatment reduces serum HCV RNA titers very rapidly by ~1.5 log₁₀ at day 3.

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

Animal Model:	NOD/SCID male mice (5 weeks of age, 18-20?g) bearing HCV RNA-transfected cells
Dosage:	30?mg/kg
Administration:	Oral administration; daily; for 27 days
Result:	Reduced serum HCV RNA titers very rapidly by ~1.5 log₁₀ at day 3.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Min Gao, et al. Chemical genetics strategy identifies an HCV NS5A inhibitor with a potent clinical effect. Nature. 2010 May 6;465(7294):96-100. [Information]

[2]. David B Ascher, et al. Potent hepatitis C inhibitors bind directly to NS5A and reduce its affinity for RNA. Sci Rep. 2014 Apr 23;4:4765. [Information]

[3]. Tomomi Furihata, et al. Different interaction profiles of direct-acting anti-hepatitis C virus agents with human organic anion transporting polypeptides. Antimicrob Agents Chemother. 2014 Aug;58(8):4555-64. [Information]

[4]. Seung-Hoon Lee, et al. HA1077 displays synergistic activity with daclatasvir against hepatitis C virus and suppresses the emergence of NS5A resistance-associated substitutions in mice. Sci Rep. 2018 Aug 20;8(1):12469. [Information]

溶解度数据

体外研究:

DMSO : ≥ 56 mg/mL (68.98 mM)

H₂O : 50 mg/mL (61.59 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.2318 mL	6.1592 mL	12.3183 mL
5 mM	0.2464 mL	1.2318 mL	2.4637 mL
10 mM	0.1232 mL	0.6159 mL	1.2318 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 1 mg/mL (1.23 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (1.23 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1 mg/mL (1.23 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (1.23 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 1 mg/mL (1.23 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (1.23 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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