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Postion:Product Catalog >Biochemical Engineering>Inhibitors>Proteases>HCV Protease Inhibitors>Daclatasvir
Daclatasvir
  • Daclatasvir
  • Daclatasvir

Daclatasvir NEW

Price $35 $0.9
Package 1kg 1000kg
Min. Order: 1kg
Supply Ability: g-kg-tons, free sample is available
Update Time: 2024-03-23

Product Details

Product Name: Daclatasvir CAS No.: 1009119-64-5
Min. Order: 1kg Purity: 99%
Supply Ability: g-kg-tons, free sample is available Release date: 2024/03/23
Lead time: In stock, ready for shipment Packaging: bag/bottle/drum/IBC
Delivery: By express, by air, by sea Origin: Manufacturer, advantage product
COA, MSDS: Available, contact us for details Name: Mia

1. Materials information

Names

Namedaclatasvir
SynonymMore Synonyms

 Daclatasvir (BMS-790052) Biological Activity

DescriptionDaclatasvir is a potent HCV NS5A protein inhibitor, with mean EC50 values of 50 and 9 pM against genotype 1a and 1b replicons, respectively.
Related Catalog
Signaling Pathways >> Metabolic Enzyme/Protease >> HCV Protease
Signaling Pathways >> Anti-infection >> HCV
Research Areas >> Infection
Target

EC50: 9±4 pM (HCV replicon genotype 1b, in Con1 cells), 50 ± 13 pM (HCV replicon genotype 1a, in H77 cells)[1]

In VitroDaclatasvir (BMS-790052) is a small molecule inhibitor of the HCV NS5A protein that exhibits picomolar half-maximum effective concentrations (EC50) towards replicons expressing a broad range of HCV genotypes and the JFH-1 genotype 2a infectious virus in cell culture. Daclatasvir is a potent inhibitor of the JFH-1 genotype 2a infectious virus that replicates in cell culture (EC50=28 pM), an assay considered to be a more biologically relevant in vitro cell culture system. In addition, Daclatasvir displays similar potency in Huh-7, HeLa and HEK293T cells, demonstrating that the function(s) of NS5A inhibited by Daclatasvir is (are) highly conserved in different cellular environments[1].
In VivoIn a randomized, double-blind, placebo-controlled, single ascending-dose study, Daclatasvir (BMS-790052) is administered at six dose levels to healthy, non-HCV-infected subjects over a range of 1 to 200 mg as an oral solution. Daclatasvir is safe and well tolerated up to 200 mg with no clinically relevant adverse effects. After oral administration, Daclatasvir is readily absorbed, with dose-proportional exposures over the studied dose range, and all subjects have drug concentrations greater than the protein-binding-adjusted EC90 for genotypes 1a and 1b, as measured in the replicon assay, at and beyond 24 h post-dose. (The protein binding-adjusted EC90 figures are derived from an analysis of the effect of the addition of human serum on antiviral activity in replicons. In the presence of 40% human serum, the EC90 for Daclatasvir is 383 pM (0.28 ng/mL) for the genotype 1a replicon and 49 pM (0.04 ng/mL) for the genotyope 1b replicon)[1]. Mice in each group that developed persistent HCV infection are divided into two treatment groups. One group receive 4 weeks of Asunaprevir/Daclatasvir treatment and the other group received 4 weeks of Ledipasvir/GS-558093 treatment. Asunaprevir/Daclatasvir therapy and Ledipasvir/GS-558093 therapy rapidly decease serum HCV RNA levels to below the sensitivity, and they are not detected after completion of the therapy except for two mice in the Ledipasvir/GS-558093 group[2].
Cell AssayHCV genotype 1a and 1b replicon cells are maintained in media containing Daclatasvir at a concentration of 5- to 20-fold above EC50 and 0.5 mg/mL G418. Replicon cells similarly treated with DMSO are maintained as controls. After approximately 4-5 weeks when cell growth is similar to DMSO-treated control cells, selected cells are expanded for resistance testing and analysis by PCR with reverse transcription[1].
Animal AdminMice[2] Humanized liver chimeric mice, whose chimeric rate of the liver is estimated as over 40 %, are injected intravenously with 100 µL of HCV-positive human serum samples. After inoculation, their blood is collected from an external jugular vein every 1-4 weeks. The HCV RNA levels are measured by the COBAS TaqMan HCV test in 100-fold diluted serum with a lower measurement range of 3.2 log IU/mL serum. After serum levels of HCV RNA reach plateau levels, mice are administered orally once a day for 4 weeks with one of the following: 40 mg/kg of Asunaprevir plus 30 mg/kg of Daclatasvir, 15 mg/kg of Ledipasvir plus 50 mg/kg of GS-558093 and 50 mg/kg of GS-558093 plus 400 mg/kg of Telaprevir.
References

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

[2]. Kai Y, et al. Emergence of hepatitis C virus NS5A L31V plus Y93H variant upon treatment failure of daclatasvir and asunaprevir is relatively resistant to ledipasvir and NS5B polymerase nucleotide inhibitor GS-558093 in human hepatocyte chimeric mice. J Ga

[3]. Zhang X, et al. Discovery and evolution of aloperine derivatives as a new family of HCV inhibitors with novel mechanism. Eur J Med Chem. 2018 Jan 1;143:1053-1065.

 Chemical & Physical Properties

Density1.3±0.1 g/cm3
Boiling Point1071.2±65.0 °C at 760 mmHg
Molecular FormulaC40H50N8O6
Molecular Weight738.875
Flash Point601.7±34.3 °C
Exact Mass738.385315
PSA174.64000
LogP5.44
Vapour Pressure0.0±0.3 mmHg at 25°C
Index of Refraction1.595

 Safety Information

Hazard CodesXi
Safety Phrases24/25

2. Packaging of materials

  • For powders: normal is 25kgs/Drum or bag, or larger/smaller package as request.

  • For liquids: normal 25kgs/drum, 180-300kgs/bucket, or IBC, determined by the nature of the product. 

                             Or smaller package 1kg/bottle, 10kgs/bottle as request. 


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3. Shipping & Delivery

  • By Express

Provide door to door service

Suitable for goods under 50kg

Delivery: 3-7 days

Cost: low cost

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  • By Air

Provide airport to airport service

Suitable for goods over 50kg

Delivery: 3-14 days

Cost: high cost

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  • By Sea

Provide seaport to seaport service

Suitable for goods over 100kg

Delivery: 2-45 days

Cost: low cost

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4. Contact information

For more details, pls contact us freely.

Email address: mia@fdachem.com

Mob: 86 18336764634

WhatsApp/Skype/Wechat/LINE: 86 18336764634










Company Profile Introduction

Henan Fengda Chemical Co., Ltd. is located in the High-tech Development Zone of Henan Province. Specializing in the production and sales of various fine chemical products required for industrial production, including chemical raw materials, organic raw materials, petrochemicals, chemical reagents, solvents, catalysts, and additives, etc.

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  • Since: 2023-02-10
  • Address: Room 01, 2288 E05, Building 14, East Henan University, Science and Technology Park, 279 Xisanhuan Ro
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