Free shipping on all orders over $ 500

GS-5885

Cat. No. M2553
GS-5885 Structure
Synonym:

Ledipasvir

Size Price Availability Quantity
10mM*1mL USD 297  USD330 In stock
5mg USD 126  USD140 In stock
10mg USD 216  USD240 In stock
50mg USD 810  USD900 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

GS-5885 is an inhibitor of the hepatitis C virus (HCV) NS5A protein and exhibits potent suppression of genotype 1 HCV replicons. GS-5885 was well tolerated and resulted in median maximal reductions in HCV RNA ranging from 2.3 log(10) IU/ml (1 mg QD) to 3.3 log(10) IU/ml (10 mg QD in genotype 1b and 30 mg QD). E(max) modeling indicated GS-5885 30 mg was associated with>95% of maximal antiviral response to HCV genotype 1a. HCV RNA reductions were generally more sustained among patients with genotype 1b vs. 1a. Three of 60 patients had a reduced response and harbored NS5A-resistant virus at baseline. NS5A sequencing identified residues 30 and 31 in genotype 1a, and 93 in genotype 1b as the predominant sites of mutation following GS-5885 dosing. Ledipasvir (formerly GS-5885) is currently in Phase III clinical trials.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 889.0
Formula C49H54F2N8O6
CAS Number 1256388-51-8
Purity >98%
Solubility DMSO
Storage at -20°C
References

Natural prevalence of NS5A polymorphisms in subjects infected with hepatitis C virus genotype 3 and their effects on the antiviral activity of NS5A inhibitors.
Hernandez D, et al. J Clin Virol. 2013 May;57(1):13-8. PMID: 23384816.

A phase 1, randomized, placebo-controlled, 3-day, dose-ranging study of GS-5885, an NS5A inhibitor, in patients with genotype 1 hepatitis C.
Lawitz EJ, et al. J Hepatol. 2012 Jul;57(1):24-31. PMID: 22314425.

Related HCV Protease Products
Merimepodib

Merimepodib, also known as VX-497, is an orally bioavailable IMPDH inhibitor with broad spectrum antiviral activities.

Inarigivir soproxil

Inarigivir soproxil, also known as SB 9200, is a novel agonist of innate immunity, which shows potent antiviral activity against resistant HCV variants.

Ombitasvir

Ombitasvir is a potent inhibitor of the hepatitis C virus protein NS5A, with EC50s of 0.82 to 19.3 pM against HCV genotypes 1 to 5 and 366 pM against genotype 6a.

Paritaprevir

Paritaprevir (ABT-450) is a potent non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50 values of 1 and 0.21 nM for HCV 1a and 1b, respectively.

BLT-1

Block lipid transport-1 (BLT-1) is a specific inhibitor of the SR-BI (Scavenger receptor, class B, type I) mediated lipid transfer.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GS-5885, Ledipasvir supplier, HCV Protease, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.