RS-127445 hydrochloride - CAS:199864-86-3

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RS-127445 hydrochloride

目录号 : KM6164 CAS No. : 199864-86-3 纯度 : 98%

Data Sheet 产品使用指南

RS-127445 hydrochloride 是一种有效的，具有口服活性的，高亲和力选择性 5-HT_2B 受体拮抗剂，pK_i 为 9.5，比作用于其他受体和离子通道的选择性高 1000 倍。

规格	价格	是否有货
5mg		In-stock
10mg		In-stock
50mg		In-stock
100mg	询价	In-stock
200mg	询价	In-stock

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生物活性

RS-127445 hydrochloride is a selective, high affinity, orally bioavailable 5-HT_2B receptor antagonist with a pK_i of 9.5. RS-127445 hydrochloride shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites.

体外研究

RS-127445 is found to has nanomolar affinity for the 5-HT_2B receptor (pK_i=9.5±0.1) and 1,000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites. RS-127445 potently displaces [H]-5-HT from human recombinant 5-HT_2B receptors expressed in CHO-K1 cells. The affinity (pK_i value) of RS-127445 for the 5-HT_2B receptor is 9.5±0.1 (n=9). RS-127445 is selective for the 5-HT_2B receptor, having approximately 1000 fold lower affinity for the human recombinant 5-HT_2A, 5-HT_2C, 5-HT₅, 5-HT₆ and 5-HT₇ receptors, a 5-HT_1A receptor in rat brain membranes, a 5-HT_1B/D receptor in bovine caudate, and a monoamine uptake site in rabbit platelets. RS-127445 potently blocks the 5-HT (10 nM) evoked increases in intracellular calcium concentrations in the HEK-293 cells expressing the 5-HT_2B receptor (pIC₅₀ of 10.4±0.1). In cells expressing human recombinant 5-HT_2B receptors, RS-127445 potently antagonizes 5-HT-evoked formation of inositol phosphates (pK_B=9.5±0.1) and 5-HT-evoked increases in intracellular calcium (pIC₁₀=10.4±0.1). RS-127445 also blocks 5-HT-evoked contraction of rat isolated stomach fundus (pA_2B=9.5±1.1) and (±)α-methyl-5-HT-mediated relaxation of the rat jugular vein (pA₂=9.9±0.3).

体内研究

In rats, the fraction of RS-127445 that is bioavailable via the oral or intraperitoneal routes is 14 and 60% respectively. Intraperitoneal administration of RS-127445 (5 mg/kg) produced plasma concentrations predicted to fully saturate accessible 5-HT_2B receptors for at least 4 h.RS-127445 (5 mg/kg) is administered to rats by oral, intraperitoneal and intravenous routes. Peak plasma concentrations are 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 is 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 is approximately 14 and 62% of that obtained by intravenous administration. Approximately 60% of an intraperitoneal dose and 14% of the oral dose of RS-127445 (5 mg/kg) is bioavailable. RS-127445 (1-30 mg/kg), dose-dependently reduces faecal output, reaching significance at 10 and 30 mg/kg (n=6-11). In blood and brain, >98% of RS-127445 is protein-bound.

分子式

C₁₇H₁₆N₃F^.HCl

分子量

317.79

CAS号

199864-86-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 31 mg/mL (97.55 mM)

H₂O : 2.27 mg/mL (7.14 mM; ultrasonic and warming and heat to 60°C)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.1467 mL	15.7337 mL	31.4673 mL
5 mM	0.6293 mL	3.1467 mL	6.2935 mL
10 mM	0.3147 mL	1.5734 mL	3.1467 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (7.87 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.87 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (7.87 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.87 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (7.87 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.87 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。