化合物 McN5691 T11979

Product Introduction
Bioactivity


英文名: McN5691

描述: McN5691 is a voltage sensitive calcium channel blocker.

体外活性: 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].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.

体内活性: 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].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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: RWJ-26240 | RWJ 26240 | McN 5691 | McN5691 | McN-5691

相关产品: Pulegone | GV-58 | L-Phenylalanine-15N | Clopimozide | Calcium channel-modulator-1 | Nitrendipine | Z944 | YM-58483 | ω-Conotoxin FVIA | GSK-7975A

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途