计算溶液所需的质量、体积或浓度。
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
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-18038683 is a 5-Hydroxytryptamine Type 7 ( 5-HT 7 ) receptor antagonist, with pK i s of 8.19, 8.20 for rat and human 5-HT 7 in HEK293 cells, respectively.
In Vitro
JNJ-18038683 displaced, with high affinity, specific [ 3 H]5-CT binding sites from rat and human 5-HT 7 receptor express in HEK293 cells (pK i =8.19±0.02 and 8.20±0.01, respectively). Similar values are obtained on the native 5-HT 7 in membranes from rat thalamus (pK i =8.50±0.20). Hill slope values are close to unity, suggesting one-site competitive binding. Antagonist potency of JNJ-18038683 is determined by the measurement of adenylate cyclase activity in HEK293 cells expressing the human or rat 5-HT 7 receptor. 5-HT stimulates adenylyl cyclase activity in rat and human 5-HT 7 /HEK293 cells with a pEC 50 of 8.09 and 8.12, respectively. JNJ-18038683 produces a concentration-dependent decrease of 5-HT (100 nM)-stimulated adenylyl cyclase. The pK B values determined for JNJ-18038683 are in good agreement with the corresponding K i values determined from [ 3 H]5-CT binding studies. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
JNJ-18038683 dose-dependently suppresses REM sleep mainly during the first 4 h after the treatment. The duration of REM sleep is significantly decreased from the dose of 1 mg/kg onward (P<0.05) during the first 4 h after oral administration. Concomitantly, the REM sleep latency tends to be prolonged in a dose-related manner with a significant increase in REM latency occurring only at the highest dose tested (10 mg/kg; P<0.05). These alterations in REM sleep seem to be state-specific. A separate study is conducted to determine whether repeated administration of JNJ-18038683 for 7 days would result in an adaptation of the EEG sleep response in particular on REM sleep in rats during the course of the treatment and after its discontinuation. JNJ-18038683 is administered for 7 consecutive days (1 mg/kg s.c. per day) at 2 h into the light phase. On the first day of treatment, JNJ-18038683 produces a significant decrease in the time spent in REM sleep during the first 8 h after the injection and a prolongation of the REM sleep latency. The REM sleep latency is increased during the 7-day repeated treatment and is normalized on the first recovery day after cessation of treatment. The significant decrease in REM sleep time is maintained during the 7-day repeated treatment, with a rebound occurring on the first recovery day after treatment discontinuation. The NREM sleep latency and the total NREM sleep time are not affected during the entire treatment . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:Rat 5-HT 7 Receptor 8.19 (pKi, in HEK293 cells ) Human 5-HT 7 Receptor 8.20 (pKi, in HEK293 cells )
规格
规格或纯度
10mM in DMSO
英文名称
JNJ-18038683
生化机理
JNJ-18038683 是一种 5- 羟色胺 7 型（5-HT 7）受体拮抗剂，在 HEK293 细胞中对大鼠和人类 5-HT 7 的 pK i 分别为 8.19 和 8.20。
储存条件
干燥,-80℃储存
运输条件
特低温运输
作用类型
拮抗剂
作用机制
羟色胺 7（5-HT7）受体拮抗剂
名称和识别符
分子类型
小分子
Isomeric SMILES
C1CNCCC2=C1C(=NN2CC3=CC=CC=C3)C4=CC=C(C=C4)Cl.C(C(=O)O)C(CC(=O)O)(C(=O)O)O
关联CAS
PubChem CID
MeSH Entry Terms
3-(4-chlorophenyl)-1,4,5,6,7,8-hexahydro-1-(phenylmethyl)pyrazolo(3,4-d)azepine 2-hydroxy-1,2,3-propanetricarboxylate;JNJ-18038683
分子量
529.97
技术文档
高级数据
安全和危险性（GHS）
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
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 851376-05-1，分子式为 C26H28ClN3O7，分子量为 529.97 g/mol。
本产品应如何储存？
请于?80 °C、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。
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