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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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GRP 60367 is a novel,potent and selective rabies virus (RABV) entry inhibitor with nanomolar potency against some RABV strains. 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.
ln Vitro |
Certain RABV strains are prevented from entering by GRP-60367. In dose-response tests on various host cell lines, GRP-60367 showed scaffold-specific and strong anti-RABV action, with an EC50 ranging from 2 to 52 nM [1].
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References |
[1]. Venice Du Pont, et al. Identification and Characterization of a Small-Molecule Rabies Virus Entry Inhibitor. J Virol. 2020 Jun 16;94(13):e00321-20.
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Molecular Formula |
C21H27N3O2
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Molecular Weight |
353.457985162735
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Exact Mass |
353.21
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Elemental Analysis |
C, 71.36; H, 7.70; N, 11.89; O, 9.05
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CAS # |
1309241-34-6
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Related CAS # |
GRP-60367 hydrochloride;2803211-60-9
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Appearance |
Solid powder
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SMILES |
O=C(N1CCC(NCCOC2=CC(C)=CC=C2C)CC1)C3=CC=NC=C3
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InChi Key |
WNJMKSOJWRDLLM-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C21H27N3O2/c1-16-3-4-17(2)20(15-16)26-14-11-23-19-7-12-24(13-8-19)21(25)18-5-9-22-10-6-18/h3-6,9-10,15,19,23H,7-8,11-14H2,1-2H3
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Chemical Name |
(4-((2-(2,5-dimethylphenoxy)ethyl)amino)piperidin-1-yl)(pyridin-4-yl)methanone
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Synonyms |
GRP-60367; GRP 60367; GRP60367;
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.8292 mL | 14.1459 mL | 28.2917 mL | |
5 mM | 0.5658 mL | 2.8292 mL | 5.6583 mL | |
10 mM | 0.2829 mL | 1.4146 mL | 2.8292 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.