AE0047 Hydrochloride
AE0047 Hydrochloride is a calcium blocker, used in the research of hypertensive disease.
For research use only. We do not sell to patients.
- CAS No.: 116308-56-6
- Formula: C41H43ClN4O6
- Molecular Weight:723.26
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Calcium Channel Isoforms
More
Biological Activity
Calcium Channel[1]
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 116308-56-6
-
Molecular Weight 723.26
-
Formula C41H43ClN4O6
-
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.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)