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Ilaprazole

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Chemical Structure| 172152-36-2 同义名 : IY-81149;(R,S)-Ilaprazole;trade name Noltec.
CAS号 : 172152-36-2
货号 : A570627
分子式 : C19H18N4O2S
纯度 : 97%
分子量 : 366.437
MDL号 : MFCD00942538
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(95.51 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 5 mg/mL(13.64 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
动物实验配方：
生物活性
靶点

  • Proton Pump
描述 The gastric H+,K+-ATPase, composed of the catalytic α subunit and the structural β subunit, is responsible for gastric acid secretion[1]. Ilaprazole is a novel proton pump inhibitor which inhibits H+,K+-ATPase with an IC50 of 6 μM. Ilaprazole is also a potent T-cell-originated protein kinase (TOPK; playing an indispensable role in the mitosis of cancer cells) inhibitor with a Kd of 111 μM[2]. On cumulation of 14C-aminopyrine in histamine stimulated parietal cells, the IC50 of ilaprazole was 9.0 nM. In rats, ilaprazole given intraduodenally immediately after pylorus ligation, dose-dependently inhibited gastric acid secretion. At 30 mg/kg, it showed 93% and 73% inhibition on acid output and volume compared to control, respectively. In Heidenhain pouch dog, the acid output was blocked dose-dependently by intravenous administration of ilaprazole at doses of 0.3 and 1 mg/kg[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.73mL

0.55mL

0.27mL

13.64mL

2.73mL

1.36mL

27.29mL

5.46mL

2.73mL
参考文献

[1]Shin JM, et al. Gastric H+,K+-ATPase. Compr Physiol. 2011 Oct;1(4):2141-53

[2]Zheng M, et al. Proton pump inhibitor ilaprazole suppresses cancer growth by targeting T-cell-originated protein kinase. Oncotarget. 2017 Jun 13;8(24):39143-39153

[3]Kwon D, et al. Effects of IY-81149, a newly developed proton pump inhibitor, on gastric acid secretion in vitro and in vivo. Arzneimittelforschung. 2001;51(3):204-13