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GRP-60367 hydrochloride

Cat. No. M10646
GRP-60367 hydrochloride Structure
Synonym:

GRP-60367 HCl; GRP60367

Size Price Availability
10mg USD 150  USD150 4-7 Days
25mg USD 300  USD300 4-7 Days
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

GRP-60367 hydrochloride is a first-in-class potent and selective inhibitor of rabies virus (RABV) entry that specifically targets the RABV G protein. GRP-60367 inhibits entry of a subset of RABV strains. Resistance profiling of the chemotype revealed hot spots in conserved hydrophobic positions of the RABV G protein fusion loop that were confirmed in transient cell-to-cell fusion assays. Transfer of RABV G genes with signature resistance mutations into a recombinant VSV backbone resulted in the recovery of replication-competent virions with low susceptibility to the inhibitor.

Protocol
Cell Experiment
Cell lines Mouse neuronal N2a cells
Preparation method Virus yield reduction assays. Mouse neuronal N2a cells (1.5 × 104 cells/well) were seeded in a 96-well plate format and incubated for 24 h. GRP-60367 was added in 3-fold serial dilutions, followed by infection of 6,000 focus-forming units (FFU) (MOI, 0.2 FFU/cell) of virus. Control wells without compound were infected in parallel with the same amount of inoculum. After 60 min, the inoculum was removed and replaced with 100 μl fresh DMEM with (treated) or without (controls) compound. Culture supernatants were collected after 48 h incubation at 34°C, and progeny virus titers were determined on N2a cells.
Concentrations 100 nM, 1 uM, 10 uM, 100 uM, 1000 uM
Incubation time 48 h
Animal Experiment
Animal models
Formulation
Dosages
Administration
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 389.92
Formula C21H27N3O2.HCl
CAS Number 1309241-34-6 (free base)
Purity >99%
Solubility DMSO ≥ 100 mg/mL
Storage at -20°C
References

[1] Venice Du Pont, et al. J Virol . Identification and Characterization of a Small-Molecule Rabies Virus Entry Inhibitor

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GRP-60367 hydrochloride, GRP-60367 HCl; GRP60367 supplier, inhibitors

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