雷米普利, 血管紧张素转换酶抑制剂

ACE 选择性抑制剂｜调节剂

1篇引用文献

COA

级别和纯度:

Moligand™

10mM in DMSO

CAS编号: 87333-19-5
分子式: C₂₃H₃₂N₂O₅
分子量: 416.51
EC号: 642-904-3

有货

库存信息

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货号 (SKU)	包装规格	是否现货	价格	数量
R409196-1ml	1ml	现货

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Compound libraries (12333)

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基本描述

英文别名	(2S,3aS,6aS)-1-[(2S)-2-[[(1S)-1-(ethoxycarbonyl)-3-phenylpropyl]amino]-1-oxopropyl]octahydro-cyclopenta[b]pyrrole-2-carboxylic acid
规格或纯度	Moligand™, 10mM in DMSO
英文名称	Ramipril
生化机理	雷米普利是一种血管紧张素转换酶（ACE）抑制剂，IC50 为 5 nM。
储存温度	-80℃储存
运输条件	超低温冰袋运输
作用类型	抑制剂
作用机制	血管紧张素转换酶抑制剂
产品介绍	Ramipril 是血管紧张素转换酶(ACE)抑制剂，IC50为5 nM。An inhibitor of the angiotensin- coverting enzyme (ACE). Information Ramipril is anangiotensin-converting enzyme (ACE)inhibitor withIC50of 5 nM. In vitro Ramipril is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 5 nM. Ramipril enhances the activity of ACE-associated CK2 and the phosphorylation of ACE Ser¹²⁷⁰ in cultured endothelial cells, but is unable to activate JNK or stimulate the nuclear accumulation of c-Jun in endothelial cells expressing a S1270A ACE mutant or in ACE-deficient cells. Prolonged Ramipril treatment increases ACE expression in primary cultures of human endothelial cells and in vivo (mouse lung), which can be prevented by pretreatment with the JNK inhibitor SP600125. Ramipril displays little enhanced effect on the rate of in vitro endothelial apoptosis induced by the serum deprivation method. In vivo Chronic in vivo administration of Ramipril to rats at a dosage that has similar hypotensive effects in vitro HUVECs significantly reduces the rate of LPS-induced apoptosis compared to the other ACE inhibitors, which contrasts with the apoptosis effect in vitro. Ramipril inhibits systolic blood pressure (SBP) with IC50 of 1.97 mg/kg in spontaneously hypertensive rats (SHR). When in combination with AT1-receptor blockade by candesartan-cilexetil increases SBP reduction synergistically rather than additively. Administration of Ramipril to spontaneously hypertensive rats (SHR) produces significant inhibition of aorta ACE and lung ACE with IC50 ~5 mg/kg, but shows little effect for brain ACE ex vivo. Ramipril prevents beta cell dysfunction in osteoprotegerin treated mice through decreasing islet monocyte/macrophage infiltration, fibrosis and apoptosis involving decreasing RAS, growth factor genes and inflammatory molecules expressions. Cell Data cell lines： Concentrations：~1 μM Incubation Time：24 hours Powder Purity:≥99%

产品属性

ALogP	1.4

关联靶点（人）

ACE Tclin 血管紧张素转换酶(Angiotensin-converting enzyme) (2 活性数据)

点击查看靶蛋白信息： ACE

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

名称和识别符

EC号	642-904-3
分子类型	小分子
Isomeric SMILES	CCOC(=O)[C@H](CCC1=CC=CC=C1)N[C@@H](C)C(=O)N2[C@H]3CCC[C@H]3C[C@H]2C(=O)O
关联CAS	87333-19-5
PubChem CID	5362129
NSC Number	758933
MeSH Entry Terms	Acovil;Altace;Carasel;Delix;HOE 498;HOE-498;HOE498;Ramace;Ramipril;Triatec;Tritace;Vesdil;Zabien
分子量	416.51

化学和物理性质

溶解性	Solubility (25°C) In vitro DMSO: 30 mg/mL (197.17 mM); Ethanol: -1 mg/mL
比旋光度	40° (C=1,0.1 NHCl in EtOH)
熔点	109 °C

安全和危险性（GHS）

WGK Germany	2
RTECS	GY5879600
Merck Index	8103
个人防护装备	Eyeshields， Gloves， type N95 (US)， type P1 (EN143) respirator filter

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引用文献

1. Liu K, Zhao X, Qi X, Hou DL, Li HB, Gu YH, Xu QL.. (2021) Design, synthesis, and biological evaluation of a novel dual peroxisome proliferator-activated receptor alpha/delta agonist for the treatment of diabetic kidney disease through anti-inflammatory mechanisms.. Eur J Med Chem, 218 (113388-113388). [PMID:33784603] [10.1016/j.ejmech.2021.113388]