Rapacuronium bromide Org 9487|cas:156137-99-4|西域试剂

Rapacuronium bromide Org 9487,98.0%

产品编号：Bellancom-16423| CAS NO：156137-99-4| 分子式：C₃₇H₆₁BrN₂O₄| 分子量：677.80

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-16423	￥3500.00	杭州北京（现货）
Bellancom-16423	￥5500.00	杭州北京（现货）
Bellancom-16423	￥11000.00	杭州北京（现货）
Bellancom-16423	￥16000.00	杭州北京（现货）
Bellancom-16423	￥26000.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

Rapacuronium bromide Org 9487

产品介绍

Rapacuronium bromide (Org 9487) 是一种非去极化神经肌肉阻滞剂，是毒蕈碱乙酰胆碱受体 (mAChR) 的变构调节剂。

生物活性

Rapacuronium bromide (Org 9487), a non-depolarizing neuromuscular blocker, is an allosteric modulator of muscarinic acetylcholine receptor (mAChR).

体外研究

Rapacuronium binds to all muscarinic receptor subtypes at physiologically relevant concentrations and displays micromolar affinity and slight selectivity towards M₂ receptor. Rapacuronium exhibits complex effects on the kinetics of ACh binding and subsequent receptor activation estimated from stimulation of [³⁵S]GTPγS binding. Rapacuronium alone concentration dependently lowers [³⁵S]GTPγS binding to membranes with a maximal effect of approximately 25% at odd-numbered subtypes and 15% at even-numbered subtypes, with EC₅₀ ranging from 28 μM at M₂ receptors to 76 μM at M₃ receptors. While the EC₅₀ values of Rapacuronium in inhibiting [³⁵S]GTPγS binding at individual subtypes correlated with affinities measured in binding experiments with [³H]ACh (R² = 0.76) they are lower (4- to 12-fold) at all subtypes. Measurements of ACh-stimulated [³⁵S]GTPγS binding in the presence of 0.1, 1 and 10 μM Rapacuronium shows differential effects of Rapacuronium on receptor activation by an orthosteric agonist at individual receptor subtypes. At even-numbered subtypes 1 μM and 10 μM Rapacuronium significantly increases ACh EC₅₀, with lowering of E_MAX at 10 μM Rapacuronium. At this subtype 0.1 and 1 μM Rapacuronium causes a significant 2-fold decrease in ACh EC₅₀ and approximately 60% and 35% increase in E_MAX, respectively. Rapacuronium at 10 μM increases ACh EC₅₀ by about 3-fold without a significant change in E_MAX. Rapacuronium (0.1 - 10 μM) has no effect on ACh efficacy at the M₁ and M₅ subtypes but decreases the EC₅₀ of ACh in stimulating [³⁵S]GTPγS binding by 1.5- and 4-fold, respectively, at concentrations of 0.1 and 1 μM. However, this effect is not evident at 10 μM Rapacuronium.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

Time course of the neuromuscular effects of Rapacuronium following the administration of the 2×ED₉₀ doses to rats and guinea-pigs with ED₉₀ of 5953±199 and 187±16 µg/kg in rat and guinea pig, respectively.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 125 mg/mL (184.42 mM)

* "≥" 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	1.4754 mL	7.3768 mL	14.7536 mL
5 mM	0.2951 mL	1.4754 mL	2.9507 mL
10 mM	0.1475 mL	0.7377 mL	1.4754 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 (sealed storage, away from moisture)。-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: ≥ 2.08 mg/mL (3.07 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.07 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (3.07 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.07 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.07 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.07 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。