BMS-986224|cas:2055200-88-7|西域试剂

BMS-986224,98.82%

产品编号：Bellancom-139485| CAS NO：2055200-88-7| 分子式：C₂₄H₂₃ClN₄O₆| 分子量：498.92

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-139485		￥6500.00	杭州北京（现货）
Bellancom-139485		￥9800.00	杭州北京（现货）

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BMS-986224

产品介绍

BMS-986224 是一种有效选择性和具有口服活性的 APJ 受体激动剂 (K_d = 0.3 nM)，表现出与 (Pyr¹) apelin-13 相似的受体结合和信号传导谱。BMS-986224 具有研究心力衰竭的潜力。

生物活性

BMS-986224 is a potent, selective and orally active APJ receptor agonist (K_d = 0.3 nM). BMS-986224 exhibits similar receptor binding and signaling profile to (Pyr¹) apelin-13. BMS-986224 has the potential for the research of heart failure.

体外研究

BMS-986224 fully inhibits forskolin-mediated cAMP production, with an EC₅₀ for human APJ of 0.02 nM. BMS-986224 (0-100 nM) fully stimulates β-arrestin recruitment, ERK phosphorylation, and APJ internalization in Chinese hamster ovary-K1 or HEK293 ZF cells.
BMS-986224 is a potent and selective APJ receptor agonist that exhibits a similar signaling profile to (Pyr1) apelin-13.

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

体内研究

BMS-986224 (0.192 mg/kg or 3 mg/kg; SC infusion; daily;) in the RHR model increased stroke volume and cardiac output to levels seen in healthy animals but without preventing cardiac hypertrophy and fibrosis, effects differentiated from enalapril.

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

Animal Model:	Male Sprague-Dawley rats (renal hypertensive rat model)
Dosage:	0.192 mg/kg or 3 mg/kg
Administration:	SC infusion; daily; Initiated 3 days before surgery and continued for 7 days after surgery
Result:	The achieved steady-state plasma concentrations during 10-day infusion were 102 and 2686 nmol/L at low dose and HD, respectively. At the low dose, BMS-986224 increased SV and CO without affecting other measured parameters, including the measured diastolic parameters, cardiac fibrosis, and heart weight in RHR.

体内研究

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

Animal Model:	Male Sprague-Dawley rats (renal hypertensive rat model)
Dosage:	0.192 mg/kg or 3 mg/kg
Administration:	SC infusion; daily; Initiated 3 days before surgery and continued for 7 days after surgery
Result:	The achieved steady-state plasma concentrations during 10-day infusion were 102 and 2686 nmol/L at low dose and HD, respectively. At the low dose, BMS-986224 increased SV and CO without affecting other measured parameters, including the measured diastolic parameters, cardiac fibrosis, and heart weight in RHR.

性状

Solid

溶解性数据

In Vitro:

DMSO : 20.83 mg/mL (41.75 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0043 mL	10.0216 mL	20.0433 mL
5 mM	0.4009 mL	2.0043 mL	4.0087 mL
10 mM	0.2004 mL	1.0022 mL	2.0043 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: ≥ 2.08 mg/mL (4.17 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.17 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% corn oil
Solubility: ≥ 2.08 mg/mL (4.17 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.17 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。