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McN5691
CAS No. 99254-95-2
McN5691 ( —— )
产品货号. M33013 CAS No. 99254-95-2
McN5691 是一种电压依赖性钙通道 (calcium channel) 阻滞剂。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 5MG | ￥4674 | 有现货 |
|
| 10MG | ￥6774 | 有现货 |
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| 25MG | ￥9858 | 有现货 |
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| 50MG | ￥12834 | 有现货 |
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| 500MG | 获取报价 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
生物学信息
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产品名称McN5691
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注意事项本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
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产品简述McN5691 是一种电压依赖性钙通道 (calcium channel) 阻滞剂。
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产品描述McN5691 is a voltage-sensitive calcium channel blocker.
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体外实验McN5691 (1 and 10 μM) prevents 60 mM KCl-induced contraction and calcium uptake and causes concentration-dependent relaxation (EC50=190 μM) of 30 mM KCl-contracted aortic rings. At or below 10 μM, McN5691 (McN-5691) has no effects on basal tone or calcium uptake (45Ca) in isolated rings of rabbit thoracic aorta. McN5691 causes complete high affinity inhibition (Kd=39.5 nM) of specific diltiazem binding to the benzothiazepine receptor on the voltage-sensitive calcium channel in skeletal muscle microsomal membranes. In contrast to diltiazem, McN5691 inhibits specific dihydropyridine receptor binding, but the effect is biphasic with high (Kd=4.7 nM) and low (Kd=919.8 nM) affinity components. McN5691 inhibits norepinephrine (NE)-induced contraction (10 μM) and calcium uptake (1 and 10 μM) and causes concentration-dependent relaxation (EC50=159 μM) of 1 μM NE-contracted rings of rabbit thoracic aorta.
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体内实验The excretion and metabolism of a 2-ethynylbenzenealkanamine analog, antihypertensive McN5691 (RWJ-26240), in beagle dogs is investigated. A total of 96.8% and 2.8% of the radioactive dose are excreted in feces and urine, respectively, during the 7 days after oral administration of 14C-McN5691. Of the radioactive dose, 96.8% and 2.8% is recovered in feces and urine, respectively, in the 7 days after oral administration of 14C-McN5691. More than 87% of the dose is excreted in feces during the 48 hours. McN5691 is extensively metabolized in dogs. Unchanged McN5691 is found in less than 0.1% and 19% of the dose in the 0-24 hour urine and 0-48 hour fecal extract, respectively, and 36% of the sample in the 4 hour plasma. In the McN5691 (McN-5691) study, vascular resistances tend to be higher in spontaneously hypertensive rat (SHR) than in Wistar-Kyoto (WKY) but the differences are statistically significant only in the cerebellum and the midbrain.
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同义词——
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通路GPCR/G Protein
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靶点Calcium Channel
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受体Calcium Channel
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研究领域——
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适应症——
化学信息
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CAS Number99254-95-2
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分子量457.6
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分子式C30H35NO3
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纯度>98% (HPLC)
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溶解度——
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SMILESC(#CC1=CC=C(OC)C=C1CCC(N(C)CCC2=CC=C(OC)C(OC)=C2)C)C=3C=CC=CC3
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化学全称——
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1. Flaim SF, et al. Structurally novel antihypertensive compound, McN-5691, is a calcium channel blocker in vascular smooth muscle. J Pharmacol Exp Ther. 1991 Jan;256(1):279-88.?
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