计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
避光,干燥,-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
JNJ-55308942 is a high-affinity, selective, brain-penetrant P2X7 functional antagonist (hP2X7: IC 50 =10 nM, K i =7.1 nM; rP2X7: IC 50 =15 nM, K i =2.9 nM). JNJ-55308942 is orally bioavailable, binds to brain P2X7 and blocks IL-1β release from adult rodent brain.
In Vitro
JNJ-55308942 shows pK i s of 8.1and 8.5 for recombinant human and rat P2X7 channels, respectively. In human blood and in mouse blood and microglia, JNJ-55308942 attenuates IL-1β release in a potent and concentration-dependent manner. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
JNJ-55308942 (30 mg/kg; p.o.) attenuates LPS-induced microglial activation in mice. In a model of Bacillus Calmette-Guerin (BCG)-induced depression, JNJ-55308942 dosed orally (30 mg/kg), reversed the BCG-induced deficits of sucrose preference and social interaction. After oral dosing, the compound exhibited both dose and concentration-dependent occupancy of rat brain P2X7 with an ED 50 of 0.07 mg/kg. The P2X7 antagonist (3 mg/kg, oral) blocked Bz-ATP-induced brain IL-1β release in conscious rats, demonstrating functional effects of target engagement in the brain. JNJ-55308942 (5 mg/kg; p.o.) shows the F, V ss , CL, C max and AUC 24h values are 81%, 1.7 L/kg, 3.7 mL min/kg, 1747 ng/mL, and 17549 (ng/mL) h, respectively . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Sixteen male C57/BL6J miceDosage: 30 mg/kg Administration: P.o. (after an i.p. injection of LPS (0.8 mg/kg, i.p.)) Result: Significantly attenuated the effect of LPS on FSC, CD45 surface expression and CD11b surface expression. Animal Model: Rat Dosage: P.o. (Pharmacokinetic Analysis) Administration: 5 mg/kg Result: The F, V ss , CL, C max and AUC 24h were 81%, 1.7 L/kg, 3.7 mL min/kg, 1747 ng/mL, and 17549 (ng/mL) h, respectively.
规格
规格或纯度
10mM in DMSO
英文名称
JNJ-55308942
生化机理
JNJ-55308942 是一种高亲和性、选择性、脑穿透性 P2X7 功能拮抗剂（hP2X7：IC 50 =10 nM，K i =7.1 nM；rP2X7：IC 50 =15 nM，K i =2.9 nM）。JNJ-55308942 具有口服生物可利用性，能与脑 P2X7 结合，并能阻断成鼠 IL-1β 的释放。
储存条件
避光,干燥,-80℃储存
运输条件
特低温运输
作用类型
拮抗剂
名称和识别符
分子类型
小分子
Isomeric SMILES
C[C@H]1CC2=C(CN1C(=O)C3=C(C(=NC=C3)C(F)(F)F)F)N=NN2C4=NC=C(C=N4)F
PubChem CID
MeSH Entry Terms
(S)-(3-fluoro-2-(trifluoromethyl)pyridin-4-yl)(1-(5-fluoropyrimidin-2-yl)-6-methyl-1,4,6,7-tetrahydro-5H-(1,2,3)triazolo(4,5-c)pyridin-5-yl)methanone;JNJ-55308942
分子量
425.32
技术文档
高级数据
关联靶点（人）
P2RX7
Tchem
P2X嘌呤受体 7(P2X purinoceptor 7)
(3 活性数据)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
常见问题
本产品应如何储存？
请于?80 °C、避光、干燥条件下保存。请与干燥剂一同密封保存，本品对湿气敏感。
本产品如何运输？
本产品采用干冰配冷袋冷冻运输。收货后请立即拆包，并按上述储存条件保存；处理干冰时请戴隔热手套并保持通风。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 2166558-11-6，分子式为 C17H12F5N7O，分子量为 425.32 g/mol。
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