TAK-438
(Synonyms: 富马酸沃诺拉赞) 目录号 : GC15418
A selective and reversible proton pump inhibitor
Cas No.:1260141-27-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
TAK-438 is a potassium-competitive acid blocker (P-CAB) that reversibly inhibits gastric H+, K+-ATPase, [1] [2] with ID50 values of 0.86 mg/kg to histamine-stimulated acid secretion in anesthetized rats [1].
Gastric H+, K+-ATPase has a key role in the final secretion step of gastric acid, transporting H+, via an electroneutral exchange of H+ for K+, into the secretory canaliculus in parietal cells [1].
In cultured gastric glands, TAK-438 treatment resulted in a longer and stronger acid formation inhibition. The inhibition effect of TAK-438 on acid secretion seemed to be associated with gastric parietal cell physiology. After cultured gastric glands were incubated with TAK-438 for 2 h and hence the incubation buffer was replaced with the CK buffer, the acid formation stimulated by forskolin slowly recovered, but the acid formation was inhibited immediately in a concentration-dependent manner [2].
In rats, 1-4, 5-8, and 9-12 h after the administration of TAK-438 at 3 mg/kg p.o., acid secretion stimulated by histamine was strongly inhibited. 24 to 27 h after administration of TAK-438, there was an inhibition rate of 40%, and this was a significant and sustained inhibition. In Heidenhain pouch dogs treated with doses of 0.1 to 1 mg/kg TAK-438 p.o., the acid secretion stimulated by histamine was inhibited dose-dependently, and this effect lasted for > 48 h. 1, 3, and 6 h after administration of 1 mg/kg TAK-438 completely inhibited the acid secretion stimulated by histamine [1].
References:
[1]. Yasunobu Hori, Jun Matsukawa, Toshiyuki Takeuchi, et al. A Study Comparing the Antisecretory Effect of TAK-438, a Novel Potassium-Competitive Acid Blocker, with Lansoprazole in Animals. Journal of Pharmacology and Experimental Therapeutics, 2011, 337:797-804.
[2]. Jun Matsukawa, Yasunobu Hori, Haruyuki Nishida, et al. A comparative study on the modes of action of TAK-438, a novel potassium-competitive acid blocker, and lansoprazole in primary cultured rabbit gastric glands. Biochemical Pharmacology, 2011, 81:1145-1151.
| Cas No. | 1260141-27-2 | SDF | |
| 别名 | 富马酸沃诺拉赞 | ||
| 化学名 | (E)-but-2-enedioic acid;1-[5-(2-fluorophenyl)-1-pyridin-3-ylsulfonylpyrrol-3-yl]-N-methylmethanamine | ||
| Canonical SMILES | CNCC1=CN(C(=C1)C2=CC=CC=C2F)S(=O)(=O)C3=CN=CC=C3.C(=CC(=O)O)C(=O)O | ||
| 分子式 | C17H16FN3O2S.C4H4O4 | 分子量 | 461.46 |
| 溶解度 | ≥ 18.9mg/mL in DMSO | 储存条件 | 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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.167 mL | 10.8352 mL | 21.6704 mL |
| 5 mM | 0.4334 mL | 2.167 mL | 4.3341 mL |
| 10 mM | 0.2167 mL | 1.0835 mL | 2.167 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。