Shanghai Nianxing Industrial Co., Ltd
China
Product Name: McN5691 (RWJ26240)
Price: Check
Purity: 99.24%
Stocking Period: 10 Day
Contact: Yang
Email: sales@echemcloud.com

99254-95-2

99254-95-2 structure

99254-95-2 structure

Name: McN5691
Chemical Name: McN5691
CAS Number: 99254-95-2
Molecular Formula: C₃₀H₃₅NO₃
Molecular Weight: 457.604
Catalog: Signaling Pathways Membrane Transporter/Ion Channel Calcium Channel
Create Date: 2018-03-25 15:15:52
Modify Date: 2025-08-25 19:28:23
McN5691 is a voltage-sensitive calcium channel blocker.

Name	McN5691
Synonyms	N-[2-(3,4-Dimethoxyphenyl)ethyl]-4-[5-methoxy-2-(phenylethynyl)phenyl]-N-methyl-2-butanamine Benzenepropanamine, N-(2-(3,4-dimethoxyphenyl)ethyl)-5-methoxy-N,α-dimethyl-2-(phenylethynyl)- Benzenepropanamine, N-[2-(3,4-dimethoxyphenyl)ethyl]-5-methoxy-N,α-dimethyl-2-(2-phenylethynyl)- n-[2-(3,4-dimethoxyphenyl)ethyl]-4-[5-methoxy-2-(phenylethynyl)phenyl]-n-methylbutan-2-amine

Description	McN5691 is a voltage-sensitive calcium channel blocker.
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel Research Areas >> Cardiovascular Disease
Target	Calcium Channel[1]
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].
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].
Animal Admin	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, bodyweight=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).
References	[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. [2]. Wu WN, et al. Excretion and metabolism of the antihypertensive agent, RWJ-26240 (McN-5691) in dogs. Drug Metab Dispos. 1998 Feb;26(2):115-25. [3]. Flaim SF, et al. Effects of the novel calcium channel blocker, McN-5691, on cardiocirculatory dynamics and cardiac output distribution in conscious spontaneously hypertensive rat. J Cardiovasc Pharmacol. 1988 Apr;11(4):489-500.

Density	1.1±0.1 g/cm3
Boiling Point	595.6±50.0 °C at 760 mmHg
Molecular Formula	C₃₀H₃₅NO₃
Molecular Weight	457.604
Flash Point	156.4±27.3 °C
Exact Mass	457.261688
LogP	7.36
Vapour Pressure	0.0±1.7 mmHg at 25°C
Index of Refraction	1.590

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.