AE0047 Hydrochloride

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

For research use only. We do not sell to patients.

AE0047 Hydrochloride Chemical Structure

CAS No. : 116308-56-6

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Other Forms of AE0047 Hydrochloride:

Vatanidipine Get quote
Vatanidipine hydrochloride Get quote

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

Biological Activity
Protocol
Purity & Documentation
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Description	AE0047 Hydrochloride is a calcium blocker, used in the research of hypertensive disease.
IC₅₀ & 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 K_i of 40.9 nM^[3]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. AE0047 Hydrochloride Related Antibodies
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]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight	723.26
Formula	C₄₁H₄₃ClN₄O₆
CAS No.	116308-56-6
SMILES	O=C(C1=C(C)NC(C)=C(C(OC)=O)C1C2=CC(N(=O)=O)=CC=C2)OCCC3=CC=C(N4CCN(C(C5=CC=CC=C5)C6=CC=CC=C6)CC4)C=C3.Cl
Shipping	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation	Data Sheet (276 KB) Handling Instructions (2659 KB)
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. [Content Brief] [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. [Content Brief] [3]. Yamanaga K, et al. AE0047-mediated calcium channel blocking in vascular smooth muscles. Gen Pharmacol. 1997 Sep;29(3):337-43. [Content Brief] [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. [Content Brief]

Cell Assay ^[3]	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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[4]	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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. [Content Brief] [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. [Content Brief] [3]. Yamanaga K, et al. AE0047-mediated calcium channel blocking in vascular smooth muscles. Gen Pharmacol. 1997 Sep;29(3):337-43. [Content Brief] [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. [Content Brief]