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RS 127445 HCl
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
RS 127445 HCl图片
CAS NO:199864-87-4
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议

产品介绍

化学性质

Physical AppearanceA solid
StorageStore at -20°C
M.Wt317.79
Cas No.199864-87-4
FormulaC17H17ClFN3
SynonymsRS-127445; MT 500; RS127445
Solubility≥31.8 mg/mL in DMSO; insoluble in H2O; ≥33.15 mg/mL in EtOH
Chemical Name4-(4-fluoronaphthalen-1-yl)-6-isopropylpyrimidin-2-amine hydrochloride
Canonical SMILESFC1=CC=C(C2=CC(C(C)C)=NC(N)=N2)C3=CC=CC=C31.Cl
运输条件蓝冰运输或根据您的需求运输。
一般建议为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

RS-127445 is a selective, high affinity 5-HT2B receptor antagonist.

The 5-HT2B receptor is a G-protein coupled receptor. 5-HT2B receptors are widely expressed in peripheral tissues of various species. 5-HT2B receptor expresses throughout the gastrointestinal tract including smooth muscle of the stomach fundus, oesophagus, colon and small intestine. The receptor has also been found in the placenta, uterus, lung and prostate. 5-HT2B receptors are present in many vascular beds and have been localized to both vascular smooth muscle and vascular endothelial cells [1].

RS-127445 (2-amino-4-(4-fluoronaphth-1-yl)-6-isopropylpyrimidine) showed nanomolar affinity for the 5-HT2B receptor with the pKi of 9.5 ± 0.1. In cells expressing human recombinant 5-HT2B receptors, RS-127445 potently antagonized 5-HT-evoked formation of inositol phosphates (pKB = 9.5 ± 0.1) and 5-HT-evoked increases in intracellular calcium (pIC50 = 10.4 ± 0.1). RS-127445 blocked 5-HT-evoked contraction of rat isolated stomach fundus (pA2 = 9.5 ± 1.1) and (±)α-methyl-5-HT-mediated relaxation of the rat jugular vein (pA2 = 9.9 ± 0.3). In rats, RS-127445 was bioavailable via the oral or intraperitoneal routes.

Reference:
[1] Bonhaus D W, Flippin L A, Greenhouse R J, et al.  RS‐127445: a selective, high affinity, orally bioavailable 5‐HT2B receptor antagonist[J]. British journal of pharmacology, 1999, 127(5): 1075-1082.

生物活性

DescriptionRS 127445是高亲和力的5-HT2B受体拮抗剂，其pKi值为9.5。
靶点5-HT2B receptor     
IC509.5 (pKi)