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
-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
SB269970 HCl是SB-269970的盐酸盐形式，是一种5-HT7受体拮抗剂，pKi为8.3，比作用于其他受体选择性高50倍以上。A selective and potent SR-7 antagonist.
Information
SB269970 HCl is a hydrochloride salt form of SB-269970, which is a5-HT7receptor antagonist withpKiof 8.3, exhibits >50-fold selectivity against other receptors.
In vitro
SB-269970 inhibits 5-CT-stimulated adenylyl cyclase activity in guinea-pig hippocampal membranes. SB-269970 (0.03 μM, 0.1 μM, 0.3 μM and 1 μM) produces a concentration-related rightward-shift of the 5-CT concentration-response curve with no significant alteration in the maximal response to 5-CT. SB-269970 (1 μM) has any effect on 5-HT efflux when superfused alone.
In vivo
SB-269970 (10 mg/kg and 30 mg/kg) significantly reduces the effects of amphetamine by 25 and 27%, respectively, and blocks the effects of ketamine by 38% (10 mg/kg) and 30% (30 mg/kg). SB-269970 significantly reduces amphetamine-induced hyperactivity in wild-type mice and is without effects in 5-HT7 knockout mice. Systemic administration of SB-269970 (30 mg/kg) significantly reverses amphetamine disruption of PPI and did not enhance PPI by itself compared to control. SB-269970 significantly reverses the deficits induced by MK-801, but not by scopolamine. SB-269970 normalizes MK-801-induced glutamate but not dopamine release in the cortex. SB-269970 (in one medium dose of 0.5 or 1 mg/kg) exerts a specific antianxiety-like effect in the Vogel drinking test in rats, in the elevated plus-maze test in rats and in the four-plate test in mice. Moreover, SB-269970 (in one medium dose of 5 or 10 mg/kg) reveals antidepressant-like activity in the forced swimming and the tail suspension tests in mice. SB-269970 at doses of 0.3, 1 and 3 μg exhibits an anticonflict effect which is weaker than that of diazepam (40 μg), whereas SB-269970 at doses of 3 and 10 μg had marked anti-immobility action comparable to that of imipramine (0.1 μg).
Cell Data
cell lines：HUAEC, HT-29, HT1080, A431, MDA-435, MDA-231, H526, DLD-1, 9L and MV4-11 cells
Concentrations：
Incubation Time：
Powder Purity:≥99%
规格
英文别名
Phenol, 3-[[(2R)-2-[2-(4-methyl-1-piperidinyl)ethyl]-1-pyrrolidinyl]sulfonyl]-, hydrochloride (1:1)
规格或纯度
10mM in DMSO
英文名称
SB269970 HCl
生化机理
SB269970 HCl 是 SB-269970 的盐酸盐形式，它是一种 5-HT7 受体拮抗剂，pKi为 8.3，对其他受体的选择性大于 50 倍。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
分子类型
小分子
Isomeric SMILES
CC1CCN(CC1)CC[C@H]2CCCN2S(=O)(=O)C3=CC=CC(=C3)O.Cl
关联CAS
分子量
388.95
技术文档
高级数据
关联靶点（人）
HTR7
Tclin
5-羟色胺受体 7(5-hydroxytryptamine receptor 7)
(1 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro Water: 42 mg/mL (199.37 mM); DMSO: Insoluble; Ethanol: Insoluble;
比旋光度
[α]/D 75 to 90°, c = 1.0 in DMSO
熔点
199.1 - 202.4 °C
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
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