2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. Calcium Channel
  4. McN5691

McN5691 是一种电压依赖性钙通道 (calcium channel) 阻滞剂。

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McN5691 Chemical Structure

McN5691 Chemical Structure

CAS No. : 99254-95-2

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McN5691 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

McN5691 is a voltage-sensitive calcium channel blocker.

IC50 & Target

Calcium Channel[1]
体外研究
(In Vitro)

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[1].

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

McN5691 相关抗体:
体内研究
(In Vivo)

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[2]. 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[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

457.60

Formula

C30H35NO3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献
Animal Administration
[2][3]

Dogs[2]
14C- McN5691 is administered by gavage to male and female beagle dogs (3 of each sex, weight 10.2-12.8 kg) as a single 6 mg/kg (as free base in corn oil) dose. Plasma samples are obtained for 24 hours after dosing. Urine and fecal samples are collected over a 7-day period. Each collected sample is assayed for total radioactivity and analyzed by TLC and HPLC.
Rats[3]
Studies are conducted in male SHR and control normotensive Wistar-Kyoto (WKY) rats. All animals are housed in constant temperature and environment facilities and given standard lab chow and water ad libitum. Four separate studies are conducted using conscious, age-matched animals:(a) SHR receiving McN5691 as a hydrochloride salt (McN5691) (n=8, body weight=361±7 g); (b) SHR receiving vehicle (VH) (n= 8, body weight=381±5g); (C) WKY receiving McN5691(n=9, body weight=355±7 g); and (d) WKY receiving VH (n=6, body weight=342±7g). McN5691 or VH alone is administered i.v. (right jugular vein) as a 15 min continuous infusion for each dose. Each animal receives three doses of McN5691 (0.3, 1.0 and 3.0 mg/kg) in a cumulative fashion or VH infused at an equal rate (0.0408 mL/min).

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

McN5691 相关分类

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  • 稀释计算器

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  • Do most proteins show cross-species activity?

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Keywords:

McN569199254-95-2RWJ26240McN 5691McN-5691RWJ 26240RWJ-26240Calcium ChannelCa2+ channelsCa channelsInhibitorinhibitorinhibit

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