AE0047 Hydrochloride

Modify Date: 2024-01-11 20:42:35

AE0047 Hydrochloride structure	Common Name	AE0047 Hydrochloride
	CAS Number	116308-56-6	Molecular Weight	723.25600
	Density	N/A	Boiling Point	799.4ºC at 760mmHg
	Molecular Formula	C₄₁H₄₃ClN₄O₆	Melting Point	N/A
	MSDS	N/A	Flash Point	437.3ºC

Use of AE0047 Hydrochloride

AE0047 Hydrochloride is a calcium blocker, used in the research of hypertensive disease.

Name	5-O-[2-[4-(4-benzhydrylpiperazin-1-yl)phenyl]ethyl] 3-O-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate,hydrochloride
Synonym	More Synonyms

Description	AE0047 Hydrochloride is a calcium blocker, used in the research of hypertensive disease.
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel Research Areas >> Cardiovascular Disease
Target	Calcium Channel[1]
In Vitro	AE0047 Hydrochloride (4e) is a calcium antagonist[1]. AE0047 inhibits [3H]nimodipine binding to rat cardiac membrane homogenate with an IC50 of 0.26 nM[2]. AE0047 (1 μM) inhibits the high K+-evoked vascular smooth muscle contraction, and also inhibits [3H]PN200-110 binding with a Ki of 40.9 nM[3].
In Vivo	AE0047 (3 mg/kg) shows antihypertensive effect, and reduces systolic blood pressure with ED30 of 1.1 mg/kg[2]. AE0047 (1 or 3 mg/25g SP diet) inhibits blood pressure elevation and improves endothelium-dependent relaxation in response to acetylcholine in aorta isolated from stroke-prone spontaneously hypertensive rats (SHRSP)[4].
Cell Assay	K+ (30 mM) is applied to the bath every 15 min, followed by rinsing with fresh KH solution and a 15-min recovery. As a control response of the preparation to the vasoconstrictive stimulus, second and third contractile responses are averaged. AE0047 (1 μM), nifedipine (1 μM), manidipine (1 μM) or DMSO (0.1% v/v as vehicle) is added. After 1 hr, cumulative concentration-response curves to the K+ (10-90 mM) are obtained within 20 min, the tissues are then washed twice with fresh KH solution and additional K+ responses (0.5, 1.0, 2.0 and 4.0 h) are recorded for another 4 hr to monitor recovery after drug removal[3].
Animal Admin	Rats[4] Male stroke-prone spontaneously hypertensive rats are given free access to water and fed stroke-prone (SP) diet from 8 weeks of age. They are randomly assigned to one of five study groups: a control group, two groups receiving AE0047 (1 or 3 mg/25g SP diet), and two groups receiving benidipine (1 or 3 mg/25 g SP diet). Each drug is administered as an admixture of powdered SP diet for 10 weeks from 9 weeks of age. The drug dose ingested by the animals is calculated from the amount of diet consumed over 24 h. The results are approximately 3 and 10 mg/kg/day[4].
References	[1]. Ashimori A, et al. Novel 1,4-dihydropyridine calcium antagonists. II. Synthesis and antihypertensive activity of 3-[4-(substituted amino)phenylalkyl]ester derivatives. Chem Pharm Bull (Tokyo). 1991 Jan;39(1):91-9. [2]. Ashimori A, et al. Synthesis and pharmacological effects of optically active 2-[4-(4-benzhydryl-1-piperazinyl)phenyl]-ethyl methyl 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate hydrochloride. Chem Pharm Bull (Tokyo). 1991 Jan;39(1):108-11. [3]. Yamanaga K, et al. AE0047-mediated calcium channel blocking in vascular smooth muscles. Gen Pharmacol. 1997 Sep;29(3):337-43. [4]. Nishikawa M, et al. Protection against endothelial abnormalities by a novel calcium channel blocker, AE0047, in stroke-prone spontaneously hypertensive rats. Gen Pharmacol. 1999 Mar;32(3):299-305.

Boiling Point	799.4ºC at 760mmHg
Molecular Formula	C₄₁H₄₃ClN₄O₆
Molecular Weight	723.25600
Flash Point	437.3ºC
Exact Mass	722.28700
PSA	116.93000
LogP	8.35700
Vapour Pressure	1.45E-25mmHg at 25°C

Calbren

Watanidipine.2HCl

Watanidipine hydrochloride

Watanidipine dihydrochloride

AE0047 Hydrochloride