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McN5691

Catalog No. T11979 CAS 99254-95-2

Synonyms: RWJ26240

McN5691 is a voltage sensitive calcium channel blocker.

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McN5691, CAS 99254-95-2

Pack Size	Availability	Price/USD
25 mg	6-8 weeks	$ 1,520.00
50 mg	6-8 weeks	$ 1,980.00
100 mg	6-8 weeks	$ 2,500.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

Storage & Solubility Information

Description	McN5691 is a voltage sensitive calcium channel blocker.
In vitro	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.
In vivo	McN5691, a chemical compound studied for its antihypertensive properties, undergoes extensive metabolism in dogs, with negligible amounts remaining unchanged in urine (less than 0.1%) and feces (19%) within the first 24 and 48 hours, respectively, and 36% detectable in plasma after 4 hours. A comparative study on McN5691 (McN-5691) revealed that its vascular resistance effects are notably higher in spontaneously hypertensive rats (SHR) compared to Wistar-Kyoto rats (WKY), with significant differences observed in the cerebellum and midbrain. Further investigation into McN5691's (RWJ-26240) excretion and metabolism in beagle dogs highlighted that a predominant portion of a radioactive dose (96.8%) is excreted through feces, with only a minor fraction (2.8%) eliminated via urine within seven days following the oral administration of 14C-McN5691, corroborating that over 87% of the dose is expelled through feces within the first 48 hours.

Synonyms	RWJ26240
Molecular Weight	457.6
Formula	C30H35NO3
CAS No.	99254-95-2

Storage

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

References and Literature

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.

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Keywords

McN5691 99254-95-2 Membrane transporter/Ion channel Metabolism Calcium Channel RWJ-26240 RWJ 26240 McN 5691 RWJ26240 McN-5691 inhibitor inhibit

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