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Chemical Structure| 1256388-51-8 Chemical Structure| 1256388-51-8

Structure of Ledipasvir
CAS No.: 1256388-51-8

Chemical Structure| 1256388-51-8

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Ledipasvir (GS-5885) is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicons, respectively. It is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.62 μM.

Synonyms: GS-5885

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Product Details of Ledipasvir

CAS No. :1256388-51-8
Formula : C49H54F2N8O6
M.W : 889.00
SMILES Code : O=C(OC)N[C@H](C(N([C@H](C1=NC=C(C2=CC(C(F)(F)C3=C4C=CC(C5=CC=C6N=C([C@H]7N(C([C@@H](NC(OC)=O)C(C)C)=O)[C@]8([H])CC[C@@]7([H])C8)NC6=C5)=C3)=C4C=C2)N1)C9)CC%109CC%10)=O)C(C)C
Synonyms :
GS-5885
MDL No. :MFCD25976756
InChI Key :VRTWBAAJJOHBQU-KMWAZVGDSA-N
Pubchem ID :67505836

Safety of Ledipasvir

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • HCV Protease

In Vitro:

Cell Line
Concentration Treated Time Description References
143B cells 10 µM Ledipasvir did not significantly inhibit arginine uptake in 143B cells PMC11752724
Huh-7.5.1 cells 3 µM 8 hours To evaluate the inhibitory effect of LDV on HCV translation, results showed that LDV significantly suppressed viral translation after 8 hours. PMC4432190

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Human hepatocyte chimeric mice Oral 50 mg/kg once daily for 16 days To evaluate the effect of Ledipasvir monotherapy on HCV-infected mice, the results showed that HCV RNA levels decreased after treatment but did not reach undetectable levels, and the Y93H mutation was newly generated after treatment. PMC5278351

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.12mL

0.22mL

0.11mL

5.62mL

1.12mL

0.56mL

11.25mL

2.25mL

1.12mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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