计算溶液所需的质量、体积或浓度。
| 活性类型 | Relation | Activity value | Units | Action Type | 期刊 | PubMed Id | doi | Assay Aladdin ID |
|---|
为什么选择此级别
提供 ≥98% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-20°C储存。超低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
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 (Pyr 1 ) apelin-13. BMS-986224 has the potential for the research of heart failure
In Vitro
BMS-986224 fully inhibits forskolin-mediated cAMP production, with an EC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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 . MCE 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.
Form:Solid
IC50& Target:Kd: 0.3 nM (APJ receptor)
规格
规格或纯度
≥98%
英文名称
BMS-986224
生化机理
BMS-986224 是一种强效、选择性和口服活性 APJ 受体激动剂（K d = 0.3 nM）。BMS-986224 与 (Pyr 1 ) apelin-13 具有相似的受体结合和信号传导特性。BMS-986224 具有研究心力衰竭的潜力。
储存条件
-20°C储存
运输条件
超低温运输
纯度
≥98%
名称和识别符
分子类型
小分子
Isomeric SMILES
CCOCC1=C(C(=C(C(=O)N1)C2=NN=C(O2)CC3=NC=C(C=C3)Cl)O)C4=C(C=CC=C4OC)OC
PubChem CID
分子量
498.92
技术文档
高级数据
关联靶点（其它种属）
Aplnr
Apelin receptor (201 活性数据)
Rattus norvegicus (775804 活性数据)
作用机制
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
化学和物理性质
溶解性
DMSO : 20.83 mg/mL (41.75 mM; ultrasonic and warming and heat to 60°C)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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危险品化学品经营许可证（带存储）