TAK-438 (Synonyms: TAK-438) |
| カタログ番号GC15418 |
カリウム競争性酸ブロッカー
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1260141-27-2
Sample solution is provided at 25 µL, 10mM.
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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 | |
| 同義語 | TAK-438 | ||
| Chemical Name | (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 | ||
| Formula | C17H16FN3O2S.C4H4O4 | M.Wt | 461.46 |
| 溶解度 | ≥ 18.9mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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