Ledipasvir D-tartrate

SKU: orb1709272

Description

Ledipasvir D-tartrate

Research Area

Infectious Disease & Virology, Pharmacology & Drug Discovery, Protein Biochemistry

Key Properties

• CAS Number: 1502654-87-6
• MW: 1039.104
• Formula: C₅₃H₆₀F₂N₈O₁₂
• SMILES: O[C@@H]([C@H](O)C(O)=O)C(O)=O.[H][C@]12CC[C@]([H])(C1)N([C@@H]2c1nc2ccc(cc2[nH]1)-c1ccc2-c3ccc(cc3C(F)(F)c2c1)-c1cnc([nH]1)[C@@H]1CC2(CC2)CN1C(=O)[C@@H](NC(=O)OC)C(C)C)C(=O)[C@@H](NC(=O)OC)C(C)C
• Target: Others
• Solubility: DMSO:20 mg/mL (19.25 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (1.92 mM)

Bioactivity

• Target IC50:
  GT1b:4 pM|GT1a:34 pM (EC50)
• In Vivo:
  Method: Pharmacokinetic parameters of Ledipasvir D-tartrate, including plasma half-life, systemic clearance (CL), and steady-state volume of distribution (Vss), were measured in rats and dogs to evaluate its in vivo pharmacokinetic properties. Result: Ledipasvir D-tartrate exhibited favorable plasma half-lives in rats (1.83 ± 0.22 hours) and dogs (2.63 ± 0.18 hours), low systemic clearance, and moderate Vss values greater than total body water volume. The drug demonstrated good bioavailability and long half-lives in various primates, with predicted low clearance in humans.
  Read more...
• In Vitro:
  Method: Ledipasvir D-tartrate antiviral activity against HCV genotypes 1a and 1b and protein-adjusted EC50 values were determined using replicon systems. Protein binding and inhibitory effects on the JFH/3a-NS5A replicon were also evaluated. Result: Ledipasvir D-tartrate exhibited EC50 values of 31 pM and 4 pM against genotypes 1a and 1b, respectively, with protein-adjusted EC50 values of 210 pM and 27 pM. It showed high protein binding. The EC50 against the JFH/3a-NS5A replicon was 141 nM.
  Read more...

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GS-5885 D-tartrate

Compound Identifiers

PubChem CID

78357794