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Daclatasvir

CAS No.
1009119-64-5
Chemical Name:
Daclatasvir
Synonyms
EBP 883;CS-1933;Daklinza;daclatavir;aclatasvir;Dacaltasvir;Daclatasvir;Dhaka He Wei;Daclatasvir-d16;Daclatasvir/EBP883
CBNumber:
CB52515028
Molecular Formula:
C40H50N8O6
Molecular Weight:
738.88
MDL Number:
MFCD17129086
MOL File:
1009119-64-5.mol
Last updated:2024-01-17 18:41:23

Daclatasvir Properties

Melting point >155oC (dec.)
Boiling point 1071.2±65.0 °C(Predicted)
Density 1.249
storage temp. Refrigerator
solubility Aqueous Acid (Slightly), Chloroform (Sparingly), DMSO (Sparingly), Methanol (Sparingly)
form Solid
pka 10.92±0.46(Predicted)
color White to Dark Yellow
FDA UNII LI2427F9CI
NCI Drug Dictionary daclatasvir
ATC code J05AP07

Pharmacokinetic data

Protein binding 99%
Excreted unchanged in urine 6.6%
Volume of distribution 47 Litres
Biological half-life 12-15 / -

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H302
Precautionary statements  P264-P270-P301+P312-P330-P501
Safety Statements  24/25
HS Code  29332900
NFPA 704
0
2 0

Daclatasvir price More Price(30)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 23730 Daclatasvir ≥95% 1009119-64-5 5mg $33 2024-03-01 Buy
Cayman Chemical 23730 Daclatasvir ≥95% 1009119-64-5 10mg $53 2024-03-01 Buy
Cayman Chemical 23730 Daclatasvir ≥95% 1009119-64-5 100mg $262 2024-03-01 Buy
Cayman Chemical 23730 Daclatasvir ≥95% 1009119-64-5 50mg $196 2024-03-01 Buy
Cayman Chemical 23730 Daclatasvir ≥95% 1009119-64-5 25mg $180 2021-12-16 Buy
Product number Packaging Price Buy
23730 5mg $33 Buy
23730 10mg $53 Buy
23730 100mg $262 Buy
23730 50mg $196 Buy
23730 25mg $180 Buy

Daclatasvir Chemical Properties,Uses,Production

Anti-hepatitis C virus drugs

Daclatasvir (Daklinza) has obtained "priority review" status, combined with sorafenib for the treatment of genotype III adult patients with chronic hepatitis C. Daklinza has been the first drug that has been proved of being effective in the treatment of genotype III hepatitis C virus infection without the co-administration with interferon or ribavirin. Interferon and ribavirin are two drugs approved by FDA for the treatment of hepatitis C virus infection. Hepatitis C is a viral disease that can cause inflammation of the liver, resulting in decreased liver function or liver failure. Most patients infected with hepatitis C have no symptoms until liver damage becomes apparent, which may take several years. Globally, genotype III hepatitis C is the second most common genotype of hepatitis C after genotype 1 hepatitis C and is considered to be one of the most refractory genotype diseases. Daklinza is a pan-genotype NS5A replication complex inhibitor, with efficacy of inhibition of RNA replication and viral assembly, dual antiviral effect. For in vitro studies, Daklinza has been demonstrated to have anti-viral effect against genotype 1~6 hepatitis C virus. Daklinza is accompanied by a warning that the combination of amiodarone, Daklinza and Sofosbuvir may cause severe reduced heart rate. Daklinza is an oral tablet with the recommended dose of 60 mg for 1 times/d, in conjunction with Sofosbuvir for a total of 12 weeks.
【Research and development company】 Bristol-Myers Squibb.
【Patent Literature】 WO 2008021927A2 (August 9, 2007).
【Time of marketing】 July 24, 2015 listed in the United States, trade name Daklinza.
【Indications】 Used in combination with Sofosbuvir for the treatment of genotype 3 chronic hepatitis C (HCV) infection.
【Mechanism of action】 HCV nonstructural protein 5A (NS5A) inhibitors. Adverse reactions: headaches and fatigue.
【Formulation and specifications】 Tablets, 30 and 60mg.
  the structure of Daklinza
Figure 1 the structure of Daklinza
The above information is edited by the Dongfang of Chemicalbook. (2016-03-03)

Market status

Daklinza is an inhibitor of hepatitis C virus (HCV) NS5A that is useful in the treatment of genotype 3 chronic hepatitis C infection.
On July 24, 2015, the FDA approved the chronic hepatitis C drug (Bristol-Myers Squibb) for marketing.
The FDA approval process of Daklinza (Bristol-Myers Squibb) has undergone twists and turns. It has been once rejected by the FDA, but finally approved in mid – 2015. The FDA approved the combination of Daklinza and Sofosbuvir for the treatment of hepatitis C gene type 3 patients.
In fact, as early as before the FDA approval, Daklinza had been approved for marketing in Japan, the European Union and South Korea and other countries. In 2014, Japanese health sector approved the application of Daklinza and asunaprevir (Sunvepra) for the treatment of genotype 1 infection. The European Union also approved Daclatasvir to be used in combination with other drugs in the treatment of HCV genotypes 1, 2, 3 and 4 in 2014. Daclatasvir is the first NS5A complex inhibitor approved by European Union (EU). When used in combination with other drugs, compared with the treatment combination of interferon and ribavirin which takes 48 weeks, it has a shorter duration of treatment (12 weeks or 24 weeks).
Daclathavir monotherapy is not recommended, the current mainstream protocol is combination therapy of dacastavir+ sofosbuvir, which is characterized by good efficacy, higher SVR, small side effects and further shortened treatment cycle than other options.
  Daclatasvir tablets from United States Bristol-Myers Squibb Company
Figure 2 Daclatasvir tablets from United States Bristol-Myers Squibb Company

Biological activity

Daclatasvir (BMS-790052) is a highly selective HCV NS5A inhibitor with an EC50 of 9-50 pM. It acts on the infectious virus of various HCV replication genotypes and JFH-1 genotype 2a in cell cultures. Phase III;

In vitro study

BMS-790052 is one of the most potent HCV replication inhibitors reported so far with EC50 values of 50 and 9 pM on HCV genotype 1a and 1b replicons, respectively. BMS-790052 treatment index (CC50/EC50) is 105 or more. It has no effect on the 10 RNA and DNA viruses in group I with EC50 being greater than 10 μM. BMS-790052 is only effective in the treatment of HCV. BMS-790052 acts on the Huh7 cells containing the HCV genotype 1b replicon and BMS-790052 inhibits transient and stable HCV chromosome replication with an EC50 of 1-15 pM. BMS-790052 (100 pM or 1 nM) changes the subcellular localization and biochemical structure of NS5A. BMS-790052 can inhibit the heterozygous replicon containing HCV genotype-4 NS5A gene with an EC50 of 7-13 pM. The NS5A residue 30 in the heterozygous replicon is an important site for selection of resistance to BMS-790052.

Feature

BMS-790052 is a first-class, highly selective hepatitis C virus (HCV) NS5A inhibitor with an EC50 range at picomolar.

Uses

Daclatasvir, inhibits the HCV protein NS5A, and thus can be used as a drug candidate for the treatment of hepatitis C (HCV).

Definition

ChEBI: A member of the class of biphenyls that is a potent inhibitor of nonstructural protein 5A and is used (as its hydrochloride salt) for treatment of hepatitis C.

Clinical Use

Inhibitor of nonstructural protein 5A (NS5A):
Treatment of chronic hepatitis C infection in combination with other medication

Drug interactions

Potentially hazardous interactions with other drugs
Aldesleukin: avoid concomitant use.
Antipsychotics: avoid with clozapine, increased risk of agranulocytosis.

Metabolism

Dacarbazine (DTIC) is assumed to be inactive
Dacarbazine is extensively metabolised in the liver Dacarbazine is extensively metabolised in the liver by the cytochrome P450 isoenzymes CYP1A2 and CYP2E1 (and possibly in the tissues by CYP1A1) to its active metabolite 5-(3-methyl-triazen-1-yl)- imidazole-4-carboxamide (MTIC), which spontaneously decomposes to the major metabolite 5-amino-imidazole- 4-carboxamide (AIC). About half of a dose is excreted in the urine by tubular secretion; 50% as unchanged DTIC and approximately 50% as AIC.

Daclatasvir Preparation Products And Raw materials

Raw materials

Preparation Products

Global( 236)Suppliers
Supplier Tel Email Country ProdList Advantage
Shanghai Daken Advanced Materials Co.,Ltd
+86-371-66670886 info@dakenam.com China 14770 58
Henan Tianfu Chemical Co.,Ltd.
+86-0371-55170693 +86-19937530512 info@tianfuchem.com China 21703 55
Shanghai Yingrui Biopharma Co., Ltd.
+86-21-33585366 - 03@ sales03@shyrchem.com CHINA 738 60
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795 ivan@atkchemical.com China 32480 60
career henan chemical co
+86-0371-86658258 sales@coreychem.com China 29919 58
Biochempartner
0086-13720134139 candy@biochempartner.com CHINA 967 58
Hubei Jusheng Technology Co.,Ltd.
18871490254 linda@hubeijusheng.com CHINA 28180 58
Beijing Yibai Biotechnology Co., Ltd
0086-182-6772-3597 sales04@yibaibiotech.com CHINA 419 58
Chongqing Chemdad Co., Ltd
+86-023-61398051 +8613650506873 sales@chemdad.com China 39916 58
Shanghai Yingrui Biopharma Co.,Ltd
21-33585366 export01@shyrchem.com CHINA 1320 58

View Lastest Price from Daclatasvir manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Daclatasvir pictures 2024-01-17 Daclatasvir
1009119-64-5
US $0.00-0.00 / kg 1kg 99%,single impurity<0.1 1 ton Nanjing Fred Technology Co., Ltd
Daclatasvir pictures 2023-11-27 Daclatasvir
1009119-64-5
US $0.00 / g 100g 99% 500kg Wuhan Senwayer Century Chemical Co.,Ltd
dimethyl (2S,2'S)-1,1'-((2S,2'S)-2,2'-(4,4'-(biphenyl-4,4'-diyl)bis(1H-imidazole-4,2-diyl))bis(pyrrolidine-2,1-diyl))bis(3-methyl-1-oxobutane-2,1-diyl)dicarbamate pictures 2023-02-09 dimethyl (2S,2'S)-1,1'-((2S,2'S)-2,2'-(4,4'-(biphenyl-4,4'-diyl)bis(1H-imidazole-4,2-diyl))bis(pyrrolidine-2,1-diyl))bis(3-methyl-1-oxobutane-2,1-diyl)dicarbamate
1009119-64-5
US $30.00 / kg 1kg 99% 100 tons Hebei Duling International Trade Co. LTD
  • Daclatasvir pictures
  • Daclatasvir
    1009119-64-5
  • US $0.00-0.00 / kg
  • 99%,single impurity<0.1
  • Nanjing Fred Technology Co., Ltd
  • Daclatasvir pictures
  • Daclatasvir
    1009119-64-5
  • US $0.00 / g
  • 99%
  • Wuhan Senwayer Century Chemical Co.,Ltd

Daclatasvir Spectrum

diMethyl (2S,2'S)-1,1'-((2S,2'S)-2,2'-(4,4'-(biphenyl-4,4'-diyl) Daclatasvir EBP 883 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 C,C'-dimethyl ester dimethyl (2S,2'S)-1,1'-((2S,2'S)-2,2'-(4,4'-(biphenyl-4,4'-diyl)bis(1H-imidazole-4,2-diyl))bis(pyrrolidine-2,1-diyl))bis(3-methyl-1-oxobutane-2,1-diyl)dicarbamate Daclatasvir/EBP883 daclatavir DiMethyl (2S, 2'S)-1, 1'-((2S, 2'S)-2, 2'-(4, 4'-(biphenyl-4, 4'-diyl)bis(1H-iMidazole-4, 2-diyl))bis(pyrrolidine-2, 1-diyl))bis(3-Methyl-1-oxobutane-2, 1-diyl)dicarbaMate (Related Reference) Carbamic acid, 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]]]bis-, C,C'-dimethyl ester 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 C,C'-dimethyl ester Daclatasvir BMS 790052 Dacaltasvir Daklinza Daclatasvir-d16 Dhaka He Wei BMS-790052(Daclatasvir) Daclatasvir, >=98% Dimethyl ((2S,2'S)-((2S,2'S)-2,2'-(5,5'-([1,1'-biphenyl]-4,4'-diyl)bis(1H-imidazole-5,2-diyl)) BMS-790052;EBP 883;BMS 790052 CS-1933 Daclatasvir, 99%, Highly selective HCV NS5A inhibitors dimethyl (2S,2'S)-1,1'-((2S,2'S)-2,2'-(4,4'-(biphenyl-4,4'-d dimethyl(2S,2'S)-1,1'-((2S,2'S)-2,2'-(4,4'-(biphenyl-4,4'-diyl)bis(1H-imidazolChemicalbooke-4,2-diyl))bis(pyrrolidine-2,1-diyl))bis(3-methyl-1-oxobutane-2,1-diyl)dicarbamate Daclatasvir 13C2D6Q: What is Daclatasvir 13C2D6 Q: What is the CAS Number of Daclatasvir 13C2D6 Q: What is the storage condition of Daclatasvir 13C2D6 Q: What are the applications of Daclatasvir 13C2D6 DaclatasvirQ: What is Daclatasvir Q: What is the CAS Number of Daclatasvir Q: What is the storage condition of Daclatasvir C40H50N8O6 Daclatasvir (BMS-790052) 1009119-64-5 Methyl ((S)-1-((S)-2-(5-(4'-(2-((S)-1-((methoxycarbonyl)-L-valyl)pyrrolidin-2-yl)-1H-imidazol-5-yl)-[1,1'-biphenyl]-4-yl)-1H-imidazol-2-yl)pyrrolidin-1-yl)-3-methyl-1-oxobutan-2-yl)carbamate aclatasvir 1009119-64-5 1009119-94-5 C40H50N8O6 C41H52N8O6 API Inhibitors