KVA-D-88 is an inhibitor of phosphodiesterase 4B (PDE4B). It is selective for PDE4B over a panel of 20 PDE isoforms and a panel of 39 CNS receptors at 10 µM but does inhibit the activity of PDE4C1, PDE3B, the serotonin receptor subtype 5-HT2C, and sigma-2 (σ2) receptors by greater than 50%. KVA-D-88 decreases LPS- or Pam3Cys-induced production of TNF-α in mouse bone marrow-derived macrophages. It reduces cocaine self-administration and the progressive ratio breakpoint in mice when administered at a dose of 5 mg/kg.
MedKoo Cat#: 535102
Name: KVA-D-88
CAS#: 2410550-31-9
Chemical Formula: C17H11Cl2F2N3O
Exact Mass: 381.0247
Molecular Weight: 382.19
Elemental Analysis: C, 53.43; H, 2.90; Cl, 18.55; F, 9.94; N, 10.99; O, 4.19
| Solvent | mg/mL | mM | |
|---|---|---|---|
| Solubility | |||
| DMF | 30.0 | 78.49 | |
| DMSO | 30.0 | 78.49 | |
| DMSO:PBS (pH 7.2) (1:5) | 0.2 | 0.42 |
The following data is based on the product molecular weight 382.19 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.
| 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 |
