MedKoo Cat#: 555848 | Name: GRP-60367
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

GRP-60367 is a 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.

Chemical Structure

GRP-60367
GRP-60367
CAS#1309241-34-6

Theoretical Analysis

MedKoo Cat#: 555848

Name: GRP-60367

CAS#: 1309241-34-6

Chemical Formula: C21H27N3O2

Exact Mass: 353.2103

Molecular Weight: 353.47

Elemental Analysis: C, 71.36; H, 7.70; N, 11.89; O, 9.05

Price and Availability

Size Price Availability Quantity
50mg USD 450.00 2 Weeks
100mg USD 750.00 2 Weeks
200mg USD 1,250.00 2 Weeks
500mg USD 1,950.00 2 Weeks
1g USD 2,950.00 2 Weeks
2g USD 5,250.00 2 Weeks
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Related CAS #
No Data
Synonym
GRP-60367; GRP 60367; GRP60367;
IUPAC/Chemical Name
(4-((2-(2,5-dimethylphenoxy)ethyl)amino)piperidin-1-yl)(pyridin-4-yl)methanone
InChi Key
WNJMKSOJWRDLLM-UHFFFAOYSA-N
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
SMILES Code
O=C(N1CCC(NCCOC2=CC(C)=CC=C2C)CC1)C3=CC=NC=C3
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Rabies virus (RABV) causes a severe and fatal neurological disease, but morbidity is vaccine preventable and treatable prior to the onset of clinical symptoms. However, immunoglobulin (IgG)-based rabies postexposure prophylaxis (PEP) is expensive, restricting access to life-saving treatment, especially for patients in low-income countries where the clinical need is greatest, and does not confer cross-protection against newly emerging phylogroup II lyssaviruses.
Product Data
Biological target:
GRP-60367 is a first-in-class small-molecule rabies virus (RABV) entry inhibitor with nanomolar potency against some RABV strains.
In vitro activity:
Sourced GRP-60367 confirmed specific and potent anti-RABV activity of the scaffold, returning in dose-response assays EC50s ranging from 2 to 52 nM on different host cell lines (Fig. 2B). Reference: J Virol. 2020 Jun 16;94(13):e00321-20. https://pubmed.ncbi.nlm.nih.gov/32321812/
In vivo activity:
TBD

Preparing Stock Solutions

The following data is based on the product molecular weight 353.47 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Du Pont V, Wirblich C, Yoon JJ, Cox RM, Schnell MJ, Plemper RK. Identification and Characterization of a Small-Molecule Rabies Virus Entry Inhibitor. J Virol. 2020 Jun 16;94(13):e00321-20. doi: 10.1128/JVI.00321-20. PMID: 32321812; PMCID: PMC7307179.
In vitro protocol:
1. Du Pont V, Wirblich C, Yoon JJ, Cox RM, Schnell MJ, Plemper RK. Identification and Characterization of a Small-Molecule Rabies Virus Entry Inhibitor. J Virol. 2020 Jun 16;94(13):e00321-20. doi: 10.1128/JVI.00321-20. PMID: 32321812; PMCID: PMC7307179.
In vivo protocol:
TBD
Du Pont V, Wirblich C, Yoon JJ, Cox RM, Schnell MJ, Plemper RK. Identification and Characterization of a Small-Molecule Rabies Virus Entry Inhibitor. J Virol. 2020 Jun 16;94(13):e00321-20. doi: 10.1128/JVI.00321-20. PMID: 32321812; PMCID: PMC7307179.