[CAS NO. 198821-22-6] Merimepodib
PRODUCTS SPECIFICATIONS [198821-22-6]
DESCRIPTION [198821-22-6]
Overview
| MDL | MFCD09837807 |
|---|---|
| Molecular Weight | 452.46 |
| Molecular Formula | C23H24N4O6 |
| SMILES | O=C(O[C@@H]1COCC1)NCC2=CC=CC(NC(NC3=CC=C(C4=CN=CO4)C(OC)=C3)=O)=C2 |
2 Publications Citing Use of MCE
Summary
Merimepodib (VX-497) is a noncompetitive and oral inhibitor of inosine monophosphate dehydrogenase ( IMPDH ) with broad spectrum antiviral activities.
In Vitro
VX-497 has antiproliferative effect on lymphoid and keratinocyte cells. The antiproliferative effect of VX-497 in cells is reversed within 48 h of its removal [1] . VX-497 has intermediate antiviral activity against a second group of viruses, which includes HSV-1, parainfluenza-3 virus, BVDV, VEEV, and dengue virus, with IC 50 s ranging from 6 to 19 μM. VX-497 is 100-fold more potent, with an IC 50 of 380 nM and a corresponding CC 50 of 5.2 μM, for a therapeutic index of 14. The antiviral activity of VX-497 in HepG2.2.2.15 cells is reversed threefold by the addition of guanosine [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Oral administration of VX-497 inhibits the primary IgM antibody response in a dose-dependent manner, with an ED 50 value of appr 30-35 mg/kg in mice. Single daily dosing of VX-497 is observed to be as effective as twice-daily dosing in this model of immune activation [1] . GVHD developed in the vehicle-treated allografted F1 mice and treatment with VX-497 improved all manifestations of the disease significantly. The 2.9-fold increase in spleen weight in allografted animals is reduced to a 1.6-fold increase in the VX-497-treated mice. Serum IFN-gamma levels are increased 54-fold in the vehicle group while there is a 7.4-fold increase in VX-497-treated animals [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT04410354 | ViralClear Pharmaceuticals, Inc. |
COVID-19
|
June 16, 2020 | Phase 2 |
| NCT00088504 | Vertex Pharmaceuticals Incorporated |
Hepatitis C|Hepatitis
|
July 2004 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 31 mg/mL ( 68.51 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.2101 mL | 11.0507 mL | 22.1014 mL |
| 5 mM | 0.4420 mL | 2.2101 mL | 4.4203 mL |
| 10 mM | 0.2210 mL | 1.1051 mL | 2.2101 mL |
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1.
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2.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.53 mM); Clear solution
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3.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.53 mM); Clear solution
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4.
Add each solvent one by one: 5% DMSO >> 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.53 mM); Clear solution
References
- [1] Jain J, et al. VX-497: a novel, selective IMPDH inhibitor and immunosuppressive agent. J Pharm Sci. 2001 May;90(5):625-37.
- [2] Markland W, et al. Broad-spectrum antiviral activity of the IMP dehydrogenase inhibitor VX-497: a comparison with ribavirin and demonstration of antiviral additivity with alpha interferon. Antimicrob Agents Chemother. 2000 Apr;44(4):859-66.
- [3] Decker CJ, et al. The novel IMPDH inhibitor VX-497 prolongs skin graft survival and improves graft versus host disease in mice. Drugs Exp Clin Res. 2001;27(3):89-95.
Synonyms