BAY-7081 是一种有效的、选择性的、具有口服活性的可溶性氰吡啶基PDE9A抑制剂，其IC50为 15 nM。
| 生物活性 | BAY-7081 is a potent, selective, orally active and soluble cyanopyridone-basedPDE9Ainhibitor with anIC50of 15 nM[1]. |
| IC50& Target[1] | |
体内研究
(In Vivo) | BAY-7081 (0.3 or 1.0 mg/kg; i.v. or p.o.) 表现出良好的体内药代动力学特性[1]。
| Animal Model: | Wistar rats and dogs[1] | | Dosage: | 0.3 or 1.0 mg/kg | | Administration: | Intravenous injection or oral (Pharmacokinetic Analysis) | | Result: | PK Profile of PDE9A Inhibitor BAY-7081 in Selected Speciesa[1]
| species | CLbb[L h–1 kg–1] | VSSc[L kg–1] | MRTd[h] | Fe[%] | | Rat | 2.4 | 4.5 | 1.9 | 61 | | Dog | 0.9 | 3.0 | 4.0 | 80 |
aValues were derived by intravenous (dose 0.3 mg/kg) and oral (dose 1.0 mg/kg) administration of solutions in either plasma 99% + DMSO 1% (rat iv) or EtOH/PEG400/H2O (dog iv, rat and dog po) vehicles.
bBlood clearance.
cVolume of distribution at steady state.
dMean residence time after iv application.
eOral bioavailability. |
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| 分子量 | |
| Formula | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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