| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
GRP-60367 hydrochloride specifically targets the rabies virus (RABV) G protein. The G protein is the viral glycoprotein responsible for receptor binding and membrane fusion during viral entry. By inhibiting the G protein, GRP-60367 hydrochloride blocks viral entry into host cells, preventing infection. This mechanism is distinct from other antiviral approaches and represents a first-in-class strategy for RABV inhibition. The compound shows nanomolar potency against certain RABV strains.
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| ln Vitro |
In dose-response experiments, GRP-60367 (0.1 nM-1000 μM) demonstrates the scaffold's strong and specific anti-RABV action, with EC50 values ranging from 2 to 52 nM on several host cell lines[1].
In vitro, GRP-60367 hydrochloride demonstrates potent inhibition of rabies virus entry with nanomolar potency against certain RABV strains. It specifically targets the RABV G protein, blocking viral entry into host cells. The compound has been validated for potency in antiviral assays. It exhibits potent inhibition of viral replication, making it a valuable tool for studying viral life cycles. The compound's first-in-class mechanism provides a unique approach for studying RABV entry and developing antiviral strategies. |
| ln Vivo |
In vivo data for GRP-60367 hydrochloride is limited in publicly available sources. As a first-in-class RABV entry inhibitor with potent in vitro activity, the compound is expected to have potential applications in animal models of rabies virus infection. By blocking viral entry, it could prevent or treat RABV infections. However, specific published in vivo efficacy studies are not widely reported for this compound. The compound is primarily used as a research tool for studying RABV entry mechanisms.
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| Enzyme Assay |
The in vitro RABV entry inhibition assay for GRP-60367 hydrochloride involves infecting susceptible cells with rabies virus in the presence of varying concentrations of the compound. Viral entry is measured by detecting viral replication or reporter gene expression after infection. The compound's specificity for the RABV G protein is confirmed by showing that it does not inhibit entry of other viruses. IC50 values are calculated from dose-response curves. The assay may use pseudotyped viruses for enhanced safety and throughput.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: BEAS-2B, 293T, or Hep-2 cell lines Tested Concentrations: 0.1 nM, 1 nM, 10 nM, 100 nM, 1 μM, 10 μM, 100 μM, 1000 μM Incubation Duration: 48 hrs (hours) Experimental Results: EC50s of 2 nM, 3 nM, and 52 nM for RABV-ΔG-nanoLuc virus in BEAS-2B, 293T, or Hep-2 cell lines, respectively. Cellular assays for GRP-60367 hydrochloride are conducted in cell lines susceptible to rabies virus infection. Cells are treated with varying concentrations of the compound prior to or during viral infection. Viral replication is measured by quantifying viral RNA, protein, or infectious progeny. Cell viability is assessed to confirm that inhibition is due to antiviral activity rather than cytotoxicity. The compound's effects on viral entry are confirmed by measuring the internalization of viral particles using fluorescence or electron microscopy. |
| Animal Protocol |
In vivo studies for GRP-60367 hydrochloride would typically involve animal models of rabies virus infection, such as mice challenged with lethal doses of RABV. The compound would be administered via various routes (e.g., intraperitoneal, oral, or local) at doses determined by pharmacokinetic studies. Efficacy would be assessed by measuring survival rates, viral loads in tissues, and clinical signs of infection. However, specific published in vivo protocols for GRP-60367 hydrochloride are not available in the current literature.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for GRP-60367 hydrochloride is not extensively reported in publicly available sources. The compound has a molecular weight of 389.92 g/mol and a purity of ≥95%. As a small molecule entry inhibitor, it is expected to have moderate oral bioavailability. Detailed PK parameters such as half-life, clearance, and volume of distribution are not available in the current literature for this research compound. The compound is typically stored at -20°C for long-term stability.
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| Toxicity/Toxicokinetics |
Toxicity data for GRP-60367 hydrochloride is limited in publicly available sources. As with all research compounds, GRP-60367 hydrochloride is intended for research use only and not for human therapeutic applications. Standard in vitro cytotoxicity assays and in vivo tolerability studies would be required for a complete toxicity assessment. No specific toxicity data has been reported for this compound in the available literature.
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| References | |
| Additional Infomation |
GRP-60367 hydrochloride is a first-in-class small-molecule rabies virus (RABV) entry inhibitor that specifically targets the RABV G protein. It shows nanomolar potency against certain RABV strains and represents a novel approach for studying and potentially treating rabies virus infections. The compound's unique mechanism of action makes it a valuable tool for antiviral research and mechanism-of-action studies. It is available as a high-purity research chemical for in vitro and in vivo studies.
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| Exact Mass |
389.187
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| CAS # |
2803211-60-9
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| Related CAS # |
GRP-60367;1309241-34-6
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| PubChem CID |
155291570
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| Appearance |
Off-white to light yellow solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
27
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| Complexity |
431
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC(=C(C=C1)C)OCCNC2CCN(CC2)C(=O)C3=CC=NC=C3.Cl
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| InChi Key |
OOJFZGBROIVYNL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H27N3O2.ClH/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;1H
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| Chemical Name |
[4-[2-(2,5-dimethylphenoxy)ethylamino]piperidin-1-yl]-pyridin-4-ylmethanone;hydrochloride
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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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| Solubility (In Vitro) |
DMSO : 250 mg/mL (641.16 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.33 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.33 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.33 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
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.
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