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RS-127445 hydrochloride

产品编号 T7519 CAS 199864-86-3

别名: 4-(4-氟-1-萘基)-6-(1-甲基乙基)-2-嘧啶胺盐酸盐, RS 127445, MT 500

RS-127445 hydrochloride (MT 500) 是一种可口服的，高亲和力选择性5-HT2B 受体拮抗剂，pKi 为 9.5，比作用于其他受体和离子通道的选择性高 1000 倍。

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RS-127445 hydrochloride Chemical Structure

RS-127445 hydrochloride, CAS 199864-86-3

规格	价格/CNY	货期
1 mg	￥ 166	现货
5 mg	￥ 428	现货
10 mg	￥ 686	现货
25 mg	￥ 1,414	现货
50 mg	￥ 2,544	现货
100 mg	￥ 3,817	现货
1 mL * 10 mM (in DMSO)	￥ 471	现货

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其他形式的 RS-127445 hydrochloride:

RS-127445
现货

选择批次

纯度: 98%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	RS-127445 hydrochloride (MT 500) is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist(pKi : 9.5).
靶点活性	5-HT2B:9.5(pKi)
体外活性	RS 127445 potently displaced [3H]-5-HT from human recombinant 5-HT2B receptors expressed in CHO-K1 cells.?The affinity (pKi value) of RS-127445 for the 5-HT2B receptor was 9.5±0.1 (n=9).?RS-127445 was selective for the 5-HT2B receptor, having approximately 1000 fold lower affinity for the human?recombinant 5-HT2A, 5-HT2C, 5-HT5, 5-HT6 and 5-HT7 receptors, a 5-HT1A receptor in rat brain membranes, a 5-HT1B/D receptor in bovine caudate, and a monoamine uptake site in rabbit platelets[1]
体内活性	RS 127445 (5 mg kg^?1) was administered to rats by oral, intraperitoneal and intravenous routes.?Peak plasma concentrations were rapidly achieved with the highest concentrations being found at the first time-point measured following intravenous and intraperitonael administration (0.08 h) and by 0.25 h following dosing by the oral route of administration.?RS-127445 was cleared from plasma with an estimated terminal elimination half-life of approximately 1.7 h. The bioavailability of RS-127445, when administered by the oral and intraperitoneal routes was approximately 14 and 62% of that obtained by intravenous administration .?To test?whether plasma levels were proportional to the dose administered, RS-127445 was given by the intraperitoneal route at doses of 1, 3 and 10 mg kg^?1.?Increasing the dose of RS-127445 resulted in proportional increases in its concentration in the plasma[1]
动物实验	Rats were euthanized.?Right and left external jugular veins were dissected, cleaned of connective tissues and cut into ring segments approximately 5 mm long.?Tungsten hooks (0.125 mm diameter) were inserted through the lumen of the vein and connected to tension transducers.?Tissues were kept in 10 ml organ baths containing Kreb's solution supplemented with cocaine (30 μm), corticosterone (30 μm), ketanserin (0.3 μm) and indomethacin (3 μm) at 37°C at a resting tension of 0.5 g.?Prior to the initiation of any studies, monamine oxidases were inactivated by a 30 min pre exposure of the tissue to pargyline (0.1 mm).?The veins were then exposed to 0.1 μm U46619 (9,11-dideoxy-9 α, 11 aα-methano-epoxy-PGF2α;?a thromboxane A2 mimetic) until a stable contraction was attained.?Acetylcholine (0.1 μm) was used to verify the integrity of the endothelium and to determine the maximum amount of nitric?oxide-dependent relaxation that was achievable.?After washout of the acetylcholine and recontraction with U46619, cumulative concentration-response curves to (±)-α-methyl-5-HT were constructed.?When maximum relaxation was reached, the baths were rinsed, and the tissues were maintained undisturbed for 2 h. Antagonists (RS 127445)were then added to the bath and allowed to equilibrate with the tissue for at least 1 h before a second concentration-response curve to (±)-α-methyl-5-HT was generated[1].

别名	4-(4-氟-1-萘基)-6-(1-甲基乙基)-2-嘧啶胺盐酸盐, RS 127445, MT 500
分子量	317.79
分子式	C17H17ClFN3
CAS No.	199864-86-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 31 mg/mL (97.55 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.1467 mL	15.7337 mL	31.4673 mL	78.6683 mL
	5 mM	0.6293 mL	3.1467 mL	6.2935 mL	15.7337 mL
	10 mM	0.3147 mL	1.5734 mL	3.1467 mL	7.8668 mL
	20 mM	0.1573 mL	0.7867 mL	1.5734 mL	3.9334 mL
	50 mM	0.0629 mL	0.3147 mL	0.6293 mL	1.5734 mL

计算器

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稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

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配液浓度

参考文献

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]. 1999, 127(5):1075-1082. 2. Devroye, Céline, Haddjeri N , Cathala A , et al. Opposite control of mesocortical and mesoaccumbal dopamine pathways by serotonin 2B, receptor blockade: Involvement of medial prefrontal cortex serotonin 1A, receptors[J]. Neuropharmacology, 2017, 119:91-99.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

RS-127445 hydrochloride 199864-86-3 GPCR/G Protein Neuroscience 5-HT Receptor Inhibitor 4-(4-氟-1-萘基)-6-(1-甲基乙基)-2-嘧啶胺盐酸盐 RS127445 Hydrochloride inhibit RS127445 RS-127445 RS127445 hydrochloride MT500 Serotonin Receptor RS-127445 Hydrochloride RS 127445 MT 500 RS 127445 hydrochloride RS 127445 Hydrochloride MT-500 5-hydroxytryptamine Receptor inhibitor

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RS-127445 hydrochloride

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

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剂量换算

体内实验配液计算器

技术支持

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