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VX-148 is a novel, non-competitive IMPDH inhibitor with a K(i) value of 6 nM for IMPDH Type II enzyme. It is slightly more effective than mycophenolic acid and VX-497 in inhibiting the proliferation of primary human lymphocytes (IC(50) approximately 80 nM). The presence of exogenous guanosine can mitigate VX-148's inhibitory activity. Notably, VX-148 does not impede the proliferation of non-lymphocyte types such as fibroblasts, indicating selective inhibition of IMPDH activity. The compound exhibits oral bioavailability in rats and mice; oral administration of VX-148 inhibits the primary antibody response in mice in a dose-dependent manner, with an ED(50) of 38 mg/kg b.i.d. Additionally, in mice, VX-148 at a dosage of 100 mg/kg b.i.d. significantly prolongs skin graft survival time.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
10 mg | Inquiry | 10-14 weeks | |
50 mg | Inquiry | 10-14 weeks |
Description | VX-148 is a novel, non-competitive IMPDH inhibitor with a K(i) value of 6 nM for IMPDH Type II enzyme. It is slightly more effective than mycophenolic acid and VX-497 in inhibiting the proliferation of primary human lymphocytes (IC(50) approximately 80 nM). The presence of exogenous guanosine can mitigate VX-148's inhibitory activity. Notably, VX-148 does not impede the proliferation of non-lymphocyte types such as fibroblasts, indicating selective inhibition of IMPDH activity. The compound exhibits oral bioavailability in rats and mice; oral administration of VX-148 inhibits the primary antibody response in mice in a dose-dependent manner, with an ED(50) of 38 mg/kg b.i.d. Additionally, in mice, VX-148 at a dosage of 100 mg/kg b.i.d. significantly prolongs skin graft survival time. |
Alias | VX148, VX-148, VX 148 |
Molecular Weight | 435.48 |
Formula | C23H25N5O4 |
Cas No. | 297730-05-3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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