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MRK-016 is a selective, orally bioavailable inverse agonist of GABAA α5 receptor, with an EC50 of 3 nM for GABAA α5, and Kis of 0.83, 0.85, 0.77?and 1.4?nM for human?GABAA?α1β3γ2, GABAA?α2β3γ2, GABAA?α3β3γ2, and GABAA?α5β3γ2, respectively; MRK-016 also readily penetrates the CNS.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 27.15 mL | 135.73 mL | 271.45 mL |
| 0.5 mM | 5.43 mL | 27.15 mL | 54.29 mL |
| 1 mM | 2.71 mL | 13.57 mL | 27.15 mL |
| 5 mM | 0.54 mL | 2.71 mL | 5.43 mL |
*The above data is based on the productmolecular weight 368.39. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 目录号 | A12046 |
|---|---|
| 作用机制 | Agonist (激动剂) |
| M. Wt | 368.39 |
| Formula | C17H20N8O2 |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
| CAS No. | 342652-67-9 |
| Synonyms | MRK 016, MRK016 |
| SMILES | CN1N=CN=C1COC2=NN3C(C4=NOC(C)=C4)=NN=CC3=C2C(C)(C)C |
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