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GC376

Cat. No. M6204
GC376 Structure
Size Price Availability
1mg USD 160 Custom Synthesis
5mg USD 450 Custom Synthesis
10mg USD 660 Custom Synthesis
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

In vitro: GC376 covalently binds to Cys 139, Cys 147, and Cys 144 of NV 3CLpro, PV 3Cpro, and TGEV 3CLpro, respectively. GC376 is significantly effective against caliciviruses (NV and MNV-1), coronaviruses (TGEV, FIPV, MHV, 229E, and BCV), and picornaviruses (HRVs 18, 51, and 68, EV71, and PTV), with nanomolar or low micromolar IC50s, except for FCV and HAV. Interestingly, FCV is less sensitive to GC376, with IC50 of 35 μM. GC376 shows no or weak effectiveness against the replication of HAV in cells. Proteases from NV, MD145 or MNV-1 are inhibited by GC376 with a similar potency. The IC50 values of GC376 against 3CLpro from NV, MD145, and MNV-1 are comparable among tested viruses. GC376 effectively inhibits the replication of NPI52-resistant viruses in cell culture as wild-type viruses, indicating that the mutation does not confer cross-resistance to GC376.

In vivo: GC376 exhibits favorable bioavailability and safety in cats. GC376 is rapidly absorbed after s.c. administration and the peak plasma level is reached within 2 hr after injection. The mean plasma drug concentrations remains above the 50% effective concentration (EC50) value of the aldehyde form of GC376 (8 ng/mL) for 18 hrs post injection. Virus infected cats shows improvement in attitude and resolution of fever. The profound absolute lymphopenia observed in all cats prior to antiviral treatment also returns to normal before the next blood testing one week later.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 507.53
Formula C21H30N3NaO8S
CAS Number 1416992-39-6
Purity >99%
Solubility 10 mM in DMSO
Storage at -20°C
References

Efficacy of a 3C-like protease inhibitor in treating various forms of acquired feline infectious peritonitis.
Pedersen NC, et al. J Feline Med Surg. 2017 Sep 1;1098612X17729626. PMID: 28901812.

Broad-spectrum antivirals against 3C or 3C-like proteases of picornaviruses, noroviruses, and coronaviruses.
Kim Y, et al. J Virol. 2012 Nov;86(21):11754-62. PMID: 22915796.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GC376 supplier, inhibitors

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