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| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
RS-127445, 5-HT 2A 受体拮抗剂；5-HT 2B 受体拮抗剂；5-HT 2C 受体拮抗剂
有货
为什么选择此级别
Moligand™ 级 ，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
Information
RS-127445 (MT500) is a selective5-HT2Breceptor antagonist withpKiof 9.5 andpIC50of 10.4, exhibits >1000-fold selectivity against other 5-HT receptors.
In vitro
RS-127445 is a novel high affinity, selective 5-HT2B receptor antagonist devoid of detectable intrinsic activity. RS-127445 is found to have nM affinity and 1000 fold selectivity for the 5-HT2B receptor. RS-127445 is thus among the highest affinity, most selective 5- HT2B receptor ligands. RS-127445 potently blocks the 5-HT evoked increase in inositol phosphate formation and blocks the 5-HT evoked increases in intracellular calcium concentrations with a potency 1000 times greater than that of yohimbine. [1]
In vivo
RS-127445 is readily absorbed with no obvious dose or route-dependent limitations and rapidly absorbed following both oral and intraperitoneal administration with peak plasma concentrations being achieved within 15 min of dosing. RS-127445 concentration in the plasma are proportional to the administered dose. RS-127445 administrated at dose of 5 mg/kg with approximately 60% of an intraperitoneal dose and 14% of the oral dose is bioavailable. RS-127445 concentration in the plasma is predicted to fully saturate accessible 5-HT2B receptors can be readily achieved and maintained in the rat. RS-127445 administered at 1 to 10 mg/kg with oral significantly inhibits visceral hypersensitivity up to 35 to 74% provoked by restraint stress. Oral RS-127445 produces a significant suppression of TNBS-induced visceral hypersensitivity (15 to 62% inhibition at 3 to 30 mg/ kg), although RS-127445 has no significant effect on the visceral nociceptive threshold of native rats. RS-127445 administrated orally with 1 to 30 mg/kg also dose -dependently reduce the restraint stress-induced defecation in native and TNBS-treated rats. [2]. RS-127445 inhibits colonic motility and defecation. [3]
Cell Data
cell lines：
Concentrations：10 μM
Incubation Time：20 min
Powder Purity:≥97%
规格
英文别名
MT500 | 4-(4-fluoronaphthalen-1-yl)-6-isopropylpyrimidin-2-amine
规格或纯度
Moligand™, 10mM in DMSO
英文名称
RS-127445
生化机理
RS-127445 (MT500) 是一种选择性 5-HT2B 受体拮抗剂，pKi为 9.5，pIC50 为 10.4，对其他 5-HT 受体的选择性大于 1000 倍。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
拮抗剂
作用机制
5-HT 2A 受体拮抗剂；5-HT 2B 受体拮抗剂；5-HT 2C 受体拮抗剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CC(C)C1=NC(=NC(=C1)C2=CC=C(C3=CC=CC=C32)F)N
关联CAS
PubChem CID
MeSH Entry Terms
2-amino-4-(4-fluoronaphth-1-yl)-6-isopropylpyrimidine;MT 500;MT-500;MT500 cpd;RS 127445;RS 27354;RS-127445;RS-27354;RS127445;RS27354
分子量
281.34
技术文档
高级数据
关联靶点（人）
HTR1B
Tclin
5-羟色胺受体 1B(5-hydroxytryptamine receptor 1B)
(0 活性数据)
HTR2A
Tclin
5-羟色胺受体 2A(5-hydroxytryptamine receptor 2A)
(1 活性数据)
HTR2C
Tclin
5-羟色胺受体 2C(5-hydroxytryptamine receptor 2C)
(1 活性数据)
HTR2B
Tclin
5-羟色胺受体 2B(5-hydroxytryptamine receptor 2B)
(0 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 36 mg/mL (197.61 mM); Water: 36 mg/mL (197.61 mM); Ethanol: Insoluble;
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:
通过匹配包装上的批号来查找并下载产品的 COA，每批产品都进行了严格的验证，您可放心使用！
| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
 G2416116 |
分析证书 | R407929 |
溶液计算器
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