Ledipasvir D-tartrate

SKU: orb1709272

Description

Research Area

Infectious Disease & Virology, Protein Biochemistry

Images & Validation

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Key Properties

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CAS Number	1502654-87-6
MW	1039.09
Purity	99.83%
Formula	C₅₃H₆₀F₂N₈O₁₂
SMILES	[C@H]([C@@H](C(O)=O)O)(C(O)=O)O.C([C@@H](NC(OC)=O)[C@@H](C)C)(=O)N1CC2(C[C@H]1C=3NC(=CN3)C=4C=C5C(=CC4)C=6C(C5(F)F)=CC(=CC6)C=7C=C8C(=CC7)N=C(N8)[C@H]9N(C([C@@H](NC(OC)=O)C(C)C)=O)[C@]%10(C[C@@]9(CC%10)[H])[H])CC2
Target	HCV Protease
Solubility	DMSO:20 mg/mL (19.25 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (1.92 mM)

Bioactivity

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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

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Storage	store at low temperature \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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GS-5885 D-tartrate

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Compound Identifiers

PubChem CID

78357794 ↗

Key Properties

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No computed properties available.

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