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.
|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|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|CAS Number||1309241-34-6 (free base)|
|Solubility||DMSO ≥ 100 mg/mL|
Cinobufotalin is a cardiotonic steroid, or butadienolide, derived from the skin secretions of toads. SREBP1 is a novel inhibitor that inhibits the proliferation of hepatocellular carcinoma by targeting adipogenesis.
A 438079 is A potent, selective P2X7 receptor antagonist with A pIC50 of 6.9.
|A 438079 hydrochloride
A 438079 Hydrochloride is A potent, selective P2X7 receptor antagonist with A pIC50 of 6.9.
Abatacept is a CTLA-4 agonist that binds to antigen presenting cells CD80 and CD86, blocks costimulatory signals and inhibits T cell activation, and is used in the study of rheumatoid arthritis and juvenile rheumatoid arthritis.
(-)-Taxifolin is a low activity isomer of Taxifolin. Taxifolin has important anti-tyrosinase activity. Taxifolin effectively inhibited collagenase with IC50 of 193.3 μM. Taxifolin is an important natural compound with anti-fibrosis effects. Taxifolin is a free radical scavenger with antioxidant capacity.
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