JNJ-47965567 是一种中央渗透性、高亲和力、选择性 P2X7 拮抗剂，对人和大鼠 P2X7 的 pKis 分别为 7.9 和 8.7。
| Cas No. | 1428327-31-4 |
| Canonical SMILES | O=C(C1=CC=CN=C1SC2=CC=CC=C2)NCC3(CCOCC3)N(CC4)CCN4C5=CC=CC=C5 |
| 分子式 | C28H32N4O2S |
| 分子量 | 488.6 |
| 溶解度 | DMF: 30 mg/mL,DMSO: 30 mg/mL,DMSO:PBS(pH 7.2) (1:3): 0.25 mg/mL,Ethanol: 12.5 mg/mL |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | JNJ-47965567 is a selective antagonist of the purinergic receptor P2X subtype 7 (P2X7), a ligand-gated ion channel. Activation of P2X receptors by BzATP induces calcium flux, which is reduced by JNJ-47965567 in 1321N1 cells transfected with recombinant P2X7 human, macaque, dog, rat, or mouse protein with pIC50s of 8.3, 8.6, 8.5, 7.2, or 7.5, respectively. JNJ-47965567 suppresses neonatal hypoxia-induced seizures in mice and has some anticonvulsant properties in rats. It also reduces spontaneous seizures in epileptic mice even after treatment is stopped. |
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