Cetraxate hydrochloride
(Synonyms: 盐酸西曲酸酯,DV-1006) 目录号 : GC62175
Cetraxate hydrochloride (DV-1006) 是一种具有粘膜保护作用的，具有口服活性的抗溃疡试剂 (anti-ulcer)，可用于胃溃疡研究。Cetraxate hydrochloride 是一种有效的顶体蛋白酶 (acrosomal proteinase acrosin) 抑制剂，Ki 和 IC50 分别为 0.94 μM 和 3.3 μM。
Cas No.:27724-96-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cetraxate hydrochloride (DV-1006), an orally active anti-ulcer agent with mucosal protective effects, can be used for gastric ulcers research[1]. Cetraxate hydrochloride is a potent acrosomal proteinase acrosin inhibitor with a Ki and an IC50 of 0.94 μM and 3.3 μM, respectively[2].
[1]. Fumihiko Katagiri, et al. Cetraxate raises levels of calcitonin gene-related peptide and substance P in human plasma. J Pharm Pharmacol. 2004 Apr;56(4):557-61.
[2]. H Sumi, et al. Inhibitors of the acrosomal proteinase acrosin: human urinary trypsin inhibitor (UTI) and 4-(2-carboxyethyl) phenyl trans 4-aminomethylcyclohexanecarboxylate hydrochloride (DV-1006). Experientia. 1980 Sep 15;36(9):1103-4.
| Cas No. | 27724-96-5 | SDF | |
| 别名 | 盐酸西曲酸酯,DV-1006 | ||
| 分子式 | C17H24ClNO4 | 分子量 | 341.83 |
| 溶解度 | DMSO : 83.33 mg/mL (243.78 mM; Need ultrasonic) | 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 | 2.9254 mL | 14.6272 mL | 29.2543 mL |
| 5 mM | 0.5851 mL | 2.9254 mL | 5.8509 mL |
| 10 mM | 0.2925 mL | 1.4627 mL | 2.9254 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 |
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| % 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。
Anti-ulcer agent, Cetraxate hydrochloride (Neuer), prevents subcellular redistribution of lysosomal enzyme in caerulein-induced pancreatitis in the rat
J Int Med Res 1994 Mar-Apr;22(2):107-12.PMID:8020637DOI:10.1177/030006059402200207.
The protective effect of an anti-ulcer agent, Cetraxate hydrochloride [4-(2-carboxyethyl)phenyltrans-4-amino- methylcyclohexanecarboxylate hydrochloride], on the exocrine pancreas in caerulein-induced pancreatitis of rats was investigated. Hyperamylasaemia, pancreatic oedema and activation of trypsinogen in the pancreatic tissue, as well as subcellular redistribution of the lysosomal enzyme, cathepsin B, from the lysosomal fraction to the zymogen fraction, were prevented by infusion of 20 mg/kg.h cetraxate for 2 h before caerulein infusion and throughout the 3.5 h of caerulein infusion (5 micrograms/kg.h). The results indicate that cetraxate plays its protective roles against pancreatitis by inhibiting the redistribution of lysosomal enzyme and by activation of trypsinogen; such activities may be clinically useful in preventing pancreatic injuries, particularly in patients with chronic pancreatitis.
[The synthesis of 4'-(2-carboxyethyl)phenyl trans-4-aminomethyl cyclohexane carboxylate hydrochloride (Cetraxate hydrochloride) by means of enzymatic debenzylation]
Yakugaku Zasshi 1989 Mar;109(3):157-62.PMID:2754616DOI:10.1248/yakushi1947.109.3_157.
Cetraxate hydrochloride (1) (antiulcer agent) has been industrially produced by the chemical protective method of p-hydroxy propionic acid derivatives. Screening of enzymes which quantitatively hydrolyzed cetraxate benzyl ester hydrochloride (2) into 1 was undertaken to establish a novel enzymatic method of production of 1. It was found that the enzyme activity for debenzylation of 2 is contained in cellulase enzymes originated from Aspergillus sp. Lower alkyl groups or phenyl groups of p-hydroxy propionic acid derivatives are likewise selectively hydrolyzed by the cellulase enzyme. This enzymatic synthetic method is very useful for the industrial preparation of 1.
Cetraxate raises levels of calcitonin gene-related peptide and substance P in human plasma
J Pharm Pharmacol 2004 Apr;56(4):557-61.PMID:15099451DOI:10.1211/0022357023169.
Cetraxate hydrochloride (cetraxate), an anti-ulcer drug, produces a dose-related increase in mucosal blood flow. Recently, it was found that capsaicin-sensitive afferent nerves play an important role in gastric mucosal defence. Capsaicin stimulates afferent nerves and enhances the release of calcitonin gene-related peptide (CGRP) and substance P in the stomach. We studied the effect of cetraxate on human plasma CGRP and substance P in healthy subjects. Cetraxate (800 mg) or placebo were orally administered to five healthy males. Blood samples were taken before, and at 20, 40, 60, 90, 120, 180 and 240 min after administration, followed by the extracting procedure, and submitted to a highly sensitive enzyme immunoassay system for CGRP and substance P. Single administration of cetraxate caused significant increases in plasma CGRP concentration at 60-120 min compared with placebo. Cetraxate significantly increased plasma substance P levels at 40-90 min compared with placebo. In this study, we hypothesized that cetraxate might indirectly stimulate capsaicin-sensitive afferent nerves and increase mucosal blood flow, and that this may be a key mechanism underlying its gastroprotective action.
Enzymatic preparation of D-beta-acetylthioisobutyric acid and Cetraxate hydrochloride using a stereo- and/or regioselective hydrolase, 3,4-dihydrocoumarin hydrolase from Acinetobacter calcoaceticus
Appl Microbiol Biotechnol 2002 Nov;60(3):288-92.PMID:12436309DOI:10.1007/s00253-002-1116-3.
3,4-Dihydrocoumarin hydrolase (DCH) from Acinetobacter calcoaceticus F46, which was previously found on screening for aromatic lactone-hydrolyzing enzymes, catalyzes the hydrolysis of several linear esters. The substrate specificity of the enzyme toward linear esters was quite characteristic, i.e., (1) it was specific toward methyl esters, (2) it recognized the configuration at the 2-position, and (3) it hydrolyzed diesters to monoesters. DCH hydrolyzed the methyl esters of beta-acetylthioisobutyrate and cetraxate. The products of these reactions were identified as D-beta-acetylthioisobutyrate and cetraxate, respectively, i.e., the hydrolysis reactions catalyzed by DCH were stereo- and/or regioselective. With recombinant Escherichia coli cells expressing the DCH gene as a catalyst, stereospecific hydrolysis of methyl beta-acetylthioisobutyrate and regioselective hydrolysis of methyl cetraxate proceeded efficiently.
Inhibitory effect of prolonged oral administration of Cetraxate hydrochloride on experimentally-induced intestinal metaplasia in Wistar rats
Arzneimittelforschung 1987 Sep;37(9):1045-8.PMID:3435599doi
The effect of Cetraxate hydrochloride (Neuer) on the induction of intestinal metaplasia by intragastric instillation of 5% NaOH solution was investigated in Wistar rats. Oral administration of cetraxate, beginning 2 days after NaOH treatment, resulted in a significant increase in antral mucosal blood flow and a significant reduction in the incidence and amount of intestinal metaplasia in experimental week 25, but no significant changes in basal acid secretion or antral mucosal pH. On histological examination, goblet cell metaplasia were frequently seen. These results show that the increased gastric blood flow produced by Cetraxate hydrochloride may be associated with the suppression of induction of intestinal metaplasias.