GlpBio

AE0047 Hydrochloride

目录号: GC32672纯度: >98%
COASDSData Sheet
AE0047Hydrochloride是一种calcium阻滞剂，可用于高血压症的研究。
AE0047 Hydrochloride
Cas No.: 116308-56-6
规格价格库存数量操作
1mg¥3,570.00现货
1
5mg¥7,140.00现货
1
10mg¥12,138.00现货
1
20mg¥21,420.00现货
1
电话: 400-920-5774Email: sales@glpbio.cn

文献被引

本产品暂无引用记录;以下为 GlpBio 产品在 Nature / Cell / Science 等顶刊的客户引用样例
  • Nature cover
    Nature
    641, 529–536 (2025)
  • Nature cover
    Nature
    628, 630–638 (2024)
  • Nature cover
    Nature
    632, 686–694 (2024)
  • Nature cover
    Nature
    618, 1017–1023 (2023)
  • Nature cover
    Nature
    610, 366–372 (2022)
  • Cell cover
    Cell
    187(9):2288-2304 (2024)
  • Cell cover
    Cell
    183(7):1867-1883 (2020)
  • Science cover
    Science
    388(6745) (2025)
  • Science cover
    Science
    387(6739) (2025)
  • Science cover
    Science
    387(6734) (2025)
  • Cell Research cover
    Cell Research
    35, 97–116 (2025)
  • Cell Research cover
    Cell Research
    34, 683–706 (2024)
  • Cell Research cover
    Cell Research
    33, 273–287 (2023)
  • Cell Research cover
    Cell Research
    33, 546–561 (2023)
  • Cell Research cover
    Cell Research
    33, 904–922 (2023)
  • Cell Research cover
    Cell Research
    31, 1291–1307 (2021)

产品描述 Description

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

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].

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].

[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.

实验参考方法 Experimental Reference Method

Cell experiment:

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 experiment:

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.

产品文档 Product Documents

Purity:>98%
COASDSData Sheet

化学性质Chemical Properties

CAS 号
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
分子式
C41H43ClN4O6
分子量
723.26 g/mol
溶解性
Soluble in DMSO
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol