|1-(5-(2-氟苯基)-1-(吡啶-3-基磺酰基)-1H-吡咯-3-基)-N-甲基甲胺(E)-2-丁烯二酸盐|CsnPharm

CAS No.: 881681-01-2

Vonoprazan Fumarate/富马酸沃诺拉赞 Catalog No. CSN16112

Synonyms: TAK-438;富马酸沃诺拉赞

TAK-438, a potassium proton pump inhibitor, can reversibly inhibit H+/K+ ATPase with IC50 of 17 nM and does not affect Na+/K+ ATPase. It also controls gastric acid secretion.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 H+/K+ ATPase

IC50:19nM
描述The potassium-competitive acid blocker (P-CAB), a new class of acid suppressant, inhibits gastric H⁺,K⁺-ATPase activity by reversible and K⁺-competitive ionic binding to the enzyme. TAK-438 is a novel P-CAB that reversibly inhibits H⁺,K⁺-ATPase with IC₅₀ of 19 nM (pH 6.5), and exhibits potent gastric acid secretion inhibitory action in vivo. And TAK-438 was selected as a drug candidate for the treatment of gastroesophageal reflux disease (GERD), peptic ulcer, and other acid-related diseases ^[3]. Under weakly acidic conditions (pH 6.5), TAK-438 inhibited gastric H⁺,K⁺-ATPase activity in a concentration-dependent manner. Under neutral conditions (pH 7.5), the inhibitory activity of TAK-438 was almost the same as that under weakly acidic conditions. In Pylorus-Ligated rats, TAK-438 at doses of 0.5, 1, 2, and 4 mg/kg inhibited basal gastric acid secretion in a dose-dependent manner, and the ID₅₀ value was 1.26 mg/kg. In Anesthetized rats, TAK-438 inhibited 2DG-stimulated gastric acid secretion in a dose-dependent manner, and the ID_{50_{value of TAK-438 was 0.83 mg/kg. TAK-438 completely inhibited gastric acid secretion at the 4 mg/kg dose ^[4].}}
作用机制TAK-438 inhibited gastric H⁺,K⁺-ATPase in a K⁺-competitive manner ^[4].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03214094	-	-	Active, not recruiting	August 31, 2019	Japan ... more >> Takeda Selected Site Tokyo, Japan Collapse <<
NCT03214198	-	-	Recruiting	August 31, 2019	Japan ... more >> Takeda Selected Site Recruiting Tokyo, Japan Collapse <<
NCT03214081	-	-	Completed	-	Japan ... more >> Takeda Selected Site Tokyo, Japan Collapse <<

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参考文献

[1] Arikawa Y, Nishida H, et al. Discovery of a novel pyrrole derivative 1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl] -N-methylmethanamine fumarate (TAK-438) as a potassium-competitive acid blocker (P-CAB). J Med Chem. 2012 May 10;55(9):4446-56.
[2] Hori Y, Imanishi A, et al. 1-[5-(2-Fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl] -N-methylmethanamine monofumarate (TAK-438), a novel and potent potassium-competitive acid blocker for the treatment of acid-related diseases. J Pharmacol Exp Ther. 2010 Oct;335(1):231-8.
[3] Arikawa Y, Nishida H, Kurasawa O, Hasuoka A, Hirase K, Inatomi N, Hori Y, Matsukawa J, Imanishi A, Kondo M, Tarui N, Hamada T, Takagi T, Takeuchi T, Kajino M. Discovery of a novel pyrrole derivative 1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine fumarate (TAK-438) as a potassium-competitive acid blocker (P-CAB). J Med Chem. 2012 May 10;55(9):4446-56. doi: 10.1021/jm300318t. Epub 2012 Apr 30. PMID: 22512618.
[4] Hori Y, Imanishi A, Matsukawa J, Tsukimi Y, Nishida H, Arikawa Y, Hirase K, Kajino M, Inatomi N. 1-[5-(2-Fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine monofumarate (TAK-438), a novel and potent potassium-competitive acid blocker for the treatment of acid-related diseases. J Pharmacol Exp Ther. 2010 Oct;335(1):231-8. doi: 10.1124/jpet.110.170274. Epub 2010 Jul 12. Erratum in: J Pharmacol Exp Ther. 2016 Jul;358(1):1-2. PMID: 20624992.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1670 mL
- 10.8351 mL
- 21.6702 mL
- 5 mM
- 0.4334 mL
- 2.1670 mL
- 4.3340 mL
- 10 mM
- 0.2167 mL
- 1.0835 mL
- 2.1670 mL

技术信息

CAS号

881681-01-2

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H20FN3O6S

运输

蓝冰

分子量

461.46

别名

TAK-438;富马酸沃诺拉赞

溶解度

DMSO	61.0 mg/mL (132.2 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

0.5% methylcellulose+water

17 mg/mL

suspension

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT03214094	-	-	Active, not recruiting	August 31, 2019	Japan ... more >> Takeda Selected Site Tokyo, Japan Collapse <<
NCT03214198	-	-	Recruiting	August 31, 2019	Japan ... more >> Takeda Selected Site Recruiting Tokyo, Japan Collapse <<
NCT03214081	-	-	Completed	-	Japan ... more >> Takeda Selected Site Tokyo, Japan Collapse <<
NCT03214952	-	-	Completed	-	Japan ... more >> Takeda Selected Site Tokyo, Japan Collapse <<
NCT03219723	-	-	Completed	-	Japan ... more >> Takeda Selected Site Tokyo, Japan Collapse <<
NCT02743949	Gastroesophageal Reflux	Phase 2	Completed	-	-
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NCT01456247	Gastric Ulcers ... more >> Duodenal Ulcers Collapse <<	Phase 3	Completed	-	-
NCT01568398	Gastric Ulcer ... more >> Duodenal Ulcer Collapse <<	Phase 3	Completed	-	Japan ... more >> Funabashi-shi, Chiba, Japan Noda-shi, Chiba, Japan Fukuoka-shi, Fukuoka, Japan Annaka-shi, Gunma, Japan Hiroshima-shi, Hiroshima, Japan Hakodate-shi, Hokkaido, Japan Kitahiroshima-shi, Hokkaido, Japan Sapporo-shi, Hokkaido, Japan Yubari-gun, Hokkaido, Japan Kanazawa-shi, Ishikawa, Japan Sanuki-shi, Kagawa, Japan Sendai-shi, Miyagi, Japan Nagasaki-shi, Nagasaki, Japan Sasebo-shi, Nagasaki, Japan Fuchu-shi, Tokyo, Japan Katsushika-ku, Tokyo, Japan Meguro-ku, Tokyo, Japan Minato-ku, Tokyo, Japan Nakano-ku, Tokyo, Japan Collapse <<
NCT02037477	-	-	Completed	-	-
NCT01452711	Gastric Ulcer	Phase 3	Completed	-	-
NCT01452724	Duodenal Ulcer	Phase 3	Completed	-	-
NCT01452698	Erosive Esophagitis	Phase 3	Completed	-	Japan ... more >> Nagoya-shi, Aichi, Japan Abiko-shi, Chiba, Japan Fukuoka-shi, Fukuoka, Japan Itoshima-shi, Fukuoka, Japan Kurume-shi, Fukuoka, Japan Onga-gun, Fukuoka, Japan Gifu-shi, Gifu, Japan Annaka-shi, Gunma, Japan Aki-gun, Hiroshima, Japan Hiroshima-shi, Hiroshima, Japan Sapporo-shi, Hokkaido, Japan Amagasaki-shi, Hyogo, Japan Kobe-shi, Hyogo, Japan Takarazuka-shi, Hyogo, Japan Sakade-shi, Kagawa, Japan Yokohama-shi, Kanagawa, Japan Kochi-shi, Kochi, Japan Susaki-shi, Kochi, Japan Kumamoto-shi, Kumamoto, Japan Kyoto-shi, Kyoto, Japan Nagasaki-shi, Nagasaki, Japan Oita-shi, Oita, Japan Okayama-shi, Okayama, Japan Fuziidera-shi, Osaka, Japan Shizuoka-shi, Shizuoka, Japan Otawara-shi, Tochigi, Japan Chiyoda-ku, Tokyo, Japan Chuo-ku, Tokyo, Japan Nakano-ku, Tokyo, Japan Ota-ku, Tokyo, Japan Setagaya-ku, Tokyo, Japan Yamagata-shi, Yamagata, Japan Collapse <<
NCT01568385	Gastric Ulcer ... more >> Duodenal Ulcer Collapse <<	Phase 3	Completed	-	Japan ... more >> Funabashi-shi, Chiba, Japan Noda-shi, Chiba, Japan Fukuoka-shi, Fukuoka, Japan Annaka-shi, Gunma, Japan Hiroshima-shi, Hiroshima, Japan Hakodate-shi, Hokkaido, Japan Kitahiroshima-shi, Hokkaido, Japan Sapporo-shi, Hokkaido, Japan Yubari-gun, Hokkaido, Japan Kanazawa-shi, Ishikawa, Japan Sanuki-shi, Kagawa, Japan Yashiro-shi, Kumamoto, Japan Nagasaki-shi, Nagasaki, Japan Sasebo-shi, Nagasaki, Japan Fuchu-shi, Tokyo, Japan Katsushika-ku, Tokyo, Japan Meguro-ku, Tokyo, Japan Nakano-ku, Tokyo, Japan Collapse <<
NCT01505127	H. Pylori Infection	Phase 3	Completed	-	Japan ... more >> Abiko-shi, Chiba, Japan Kashiwa-shi, Chiba, Japan Fukui-shi, Fukui, Japan Fukuoka-shi, Fukuoka, Japan Ishikari-shi, Hokkaido, Japan Sapporo-shi, Hokkaido, Japan Kobe-shi, Hyogo, Japan Nishinomiya-shi, Hyogo, Japan Marugame-shi, Kagawa, Japan Takamatsu-shi, Kagawa, Japan Kagoshima-shi, Kagoshima, Japan Ebina-shi, Kanagawa, Japan Yokohama-shi, Kanagawa, Japan Yatsushiro-shi, Kumamoto, Japan Kyoto-shi, Kyoto, Japan Oita-shi, Oita, Japan Hirakata-shi, Osaka, Japan Osaka-shi, Osaka, Japan Sakai-shi, Osaka, Japan Suita-shi, Osaka, Japan Takatsuki-shi, Osaka, Japan Toyonaka-shi, Osaka, Japan Saga-shi, Saga, Japan Kumagaya-shi, Saitama, Japan Tokorozawa-shi, Saitama, Japan Shizuoka-shi, Shizuoka, Japan Adachi-ku, Tokyo, Japan Chiyoda-ku, Tokyo, Japan Hachioji-shi, Tokyo, Japan Kokubunji-shi, Tokyo, Japan Nishi-tokyo-shi, Tokyo, Japan Oota-ku, Tokyo, Japan Ota-ku, Tokyo, Japan Setagaya-ku, Tokyo, Japan Shibuya-ku, Tokyo, Japan Collapse <<
NCT01474369	Non-erosive Gastroesophageal R... more >>eflux Disease Collapse <<	Phase 3	Completed	-	-
NCT03050307	Gastric Ulcer ... more >> Peptic Ulcer Gastrointestinal Diseases Digestive System Diseases Lansoprazole Anti-Ulcer Agents Gastrointestinal Agents Proton Pump Inhibitors Enzyme Inhibitors Molecular Mechanisms of Pharmacological Action Collapse <<	Phase 3	Recruiting	April 19, 2019	-
NCT02388724	Erosive Esophagitis	Phase 3	Completed	-	-
NCT02892409	Helicobacter Pylori	Phase 1	Completed	-	Korea, Republic of ... more >> Seoul, Korea, Republic of Collapse <<
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NCT03456960	Japanese Healthy Adult Male	Phase 1	Completed	-	Japan ... more >> Fukuoka Mirai Hospital Fukuoka, Japan Collapse <<
NCT01459367	Erosive Esophagitis	Phase 3	Completed	-	Japan ... more >> Kashiwa-shi, Chiba, Japan Yachiyo-shi, Chiba, Japan Saijo-shi, Ehime, Japan Fukuoka-shi, Fukuoka, Japan Kasuya-gun, Fukuoka, Japan Koriyama-shi, Fukushima, Japan Takayama-shi, Gifu, Japan Annaka-shi, Gunma, Japan Asahikawa-shi, Hokkaido, Japan Sapporo-shi, Hokkaido, Japan Itami-shi, Hyogo, Japan Kobe-shi, Hyogo, Japan Nishinomiya-shi, Hyogo, Japan Fujisawa-shi, Kanagawa, Japan Yokohama-shi, Kanagawa, Japan Kochi-shi, Kochi, Japan Kumamoto-shi, Kumamoto, Japan Kyoto-shi, Kyoto, Japan Sendai-shi, Miyagi, Japan Nagasaki-shi, Nagasaki, Japan Kishiwada-shi, Osaka, Japan Osaka-shi, Osaka, Japan Suita-shi, Osaka, Japan Takatsuki-shi, Osaka, Japan Saga-shi, Saga, Japan Kumagaya-shi, Saitama, Japan Saitama-shi, Saitama, Japan Tokorozawa-shi, Saitama, Japan Bunkyo-ku, Tokyo, Japan Chuo-ku, Tokyo, Japan Hachioji-shi, Tokyo, Japan Kokubunji-shi, Tokyo, Japan Shibuya-ku, Tokyo, Japan Shinjuku-ku, Tokyo, Japan Toshima-ku, Tokyo, Japan Shimonoseki-shi, Yamaguchi, Japan Tsuru-shi, Yamanashi, Japan Collapse <<
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NCT02954848	Non-erosive Gastroesophageal R... more >>eflux Disease Collapse <<	Phase 3	Completed	-	Japan ... more >> Abiko, Chiba, Japan Yachiyo, Chiba, Japan Kasuya-gun, Fukuoka, Japan Kasuya, Fukuoka, Japan Kitakyusyu, Fukuoka, Japan Yukuhashi, Fukuoka, Japan Koriyama, Fukushima, Japan Asahikawa, Hokkaido, Japan Sapporo, Hokkaido, Japan Yokohama, Kanagawa, Japan Suzaki, Kochi, Japan Kitakatsuragi, Nara, Japan Fujimi, Saitama, Japan Hiki-gun, Saitama, Japan Satte, Saitama, Japan Otawara, Tochigi, Japan Arakawa-ku, Tokyo, Japan Nakano-ku, Tokyo, Japan Setagaya-ku, Tokyo, Japan Shibuya-ku, Tokyo, Japan Toshima-ku, Tokyo, Japan Fukuoka, Japan Hiroshima, Japan Kochi, Japan Kumamoto, Japan Nagasaki, Japan Oita, Japan Osaka, Japan Shizuoka, Japan Yamagata, Japan Collapse <<
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NCT02141711	Erosive Esophagitis(EE) ... more >> Gastroesophageal Reflux Disease (GERD) Collapse <<	Phase 1	Completed	-	United Kingdom ... more >> Hammersmith Medicines Research London, United Kingdom, NW10 7EW Collapse <<
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NCT01452776	Erosive Esophagitis	Phase 3	Completed	-	Japan ... more >> Nagoya-shi, Aichi, Japan Abiko-shi, Chiba, Japan Fukuoka-shi, Fukuoka, Japan Itoshima-shi, Fukuoka, Japan Kurume-shi, Fukuoka, Japan Onga-gun, Fukuoka, Japan Gifu-shi, Gifu, Japan Annaka-shi, Gunma, Japan Aki-gun, Hiroshima, Japan Hiroshima-shi, Hiroshima, Japan Sapporo-shi, Hokkaido, Japan Amagasaki-shi, Hyogo, Japan Kobe-shi, Hyogo, Japan Takarazuka-shi, Hyogo, Japan Sakaide-shi, Kagawa, Japan Yokohama-shi, Kanagawa, Japan Kochi-shi, Kochi, Japan Susaki-shi, Kochi, Japan Kumamoto-shi, Kumamoto, Japan Kyoto-shi, Kyoto, Japan Nagasaki-shi, Nagasaki, Japan Oita-shi, Oita, Japan Okayama-shi, Okayama, Japan Fuziidera-shi, Osaka, Japan Shizuoka-shi, Shizuoka, Japan Otawara-shi, Tochigi, Japan Chiyoda-ku, Tokyo, Japan Chuo-ku, Tokyo, Japan Nakano-ku, Tokyo, Japan Ota-ku, Tokyo, Japan Setagaya-ku, Tokyo, Japan Yamagata-shi, Yamagata, Japan Collapse <<
NCT02774902	Healthy Volunteers	Phase 1	Completed	-	-

Vonoprazan Fumarate/富马酸沃诺拉赞 Catalog No. CSN16112

靶点选择性

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