Category: 71079-09-9

Yonezawa, Hidetoshi published the artcileDiscrepancy between the potency of various trypsin inhibitors to inhibit trypsin activity and the potency to release biologically active cholecystokinin-pancreozymin, Application of 2-(4-((4-Guanidinobenzoyl)oxy)phenyl)acetic acid methanesulfonic acid salt, the publication is Japanese Journal of Physiology (1984), 34(5), 849-56, database is CAplus and MEDLINE.

Injection of various trypsin??[9002-07-7] inhibitors into the lumen of the isolated perfused rat duodenum increased the amount of biol. active cholecystokinin-pancreozymin (CCK-BA) [9011-97-6] in the vascular perfusate. The potency to induce CCK-BA release of the various trypsin inhibitors diffeed. Injection of Et?p-(6-guanidinohexanoyloxy)benzoate?methanesulfonate (FOY-007) [56974-61-9] (100 ¦Ìmol); p-ethoxycarbamoylthio-6-guanidinocaproate phosphate (FOY-129) (110 ¦Ìmol); 4-(4-guanidinobenzoyloxy)phenylacetic?acid (FOY-251) [71079-09-9] (128 ¦Ìmol); N,N-dimethylcarbamoylmethyl-4-(4-guanidinobenoyloxy)phenylacetate?methanesulfonate (FOY-305) [59721-29-8] (80 ¦Ìmol); and p-aminobenzamidine-2HCl (p-ABA) [2498-50-2] (300 ¦Ìmol) caused release of CCK-BA amounting to 1042, 247, 252, 682, and 302 pM, resp. The potency to induce CCK-BA release was not correlated with the potency to inhibit trypsin activity. The present results do not support the hypothesis that a neg. feedback regulation of pancreatic enzyme secretion is exerted by intraluminal trypsin in the rat.

Japanese Journal of Physiology published new progress about 71079-09-9. 71079-09-9 belongs to catalysis-chemistry, auxiliary class Salt,Carboxylic acid,Carbamidine,Amine,Benzene,Ester,Protease,Ser/Thr Protease, name is 2-(4-((4-Guanidinobenzoyl)oxy)phenyl)acetic acid methanesulfonic acid salt, and the molecular formula is C14H10O4S2, Application of 2-(4-((4-Guanidinobenzoyl)oxy)phenyl)acetic acid methanesulfonic acid salt.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Eynde, Jean Jacques Vanden published the artcileCOVID-19: failure of the DisCoVeRy clinical trial, and now-new hopes?, COA of Formula: C17H19N3O7S, the publication is Pharmaceuticals (2021), 14(7), 664, database is CAplus and MEDLINE.

The DisCoVeRy clin. trial aimed at the evaluation of four treatments for patients suffering from severe to critical COVID-19: Hydroxychloroquine, eventually associated with azithromycin; the combination lopinavir/ritonavir; the combination with the addition of interferon ¦Â-1a; remdesivir. The trial was discontinued due to the lack of pos. results. Meanwhile, many other potential options have been considered either to target the virus itself, the interactions with the host cells, or the cytokine storm frequently observed during the infection. Several of those options are briefly reviewed. They include vaccines, small mols., antibodies, and stem cells.

Pharmaceuticals published new progress about 71079-09-9. 71079-09-9 belongs to catalysis-chemistry, auxiliary class Salt,Carboxylic acid,Carbamidine,Amine,Benzene,Ester,Protease,Ser/Thr Protease, name is 2-(4-((4-Guanidinobenzoyl)oxy)phenyl)acetic acid methanesulfonic acid salt, and the molecular formula is C17H19N3O7S, COA of Formula: C17H19N3O7S.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Matsushima, Masashi published the artcileInhibition of enteropeptidase by antitrypsin drugs, Safety of 2-(4-((4-Guanidinobenzoyl)oxy)phenyl)acetic acid methanesulfonic acid salt, the publication is Biomedical Research (2001), 22(5), 257-260, database is CAplus.

We have investigated the inhibitory effects on porcine enteropeptidase of some typical synthetic amidino- and guanidino-compounds developed as antitrypsin drugs. The results indicated that enteropeptidase is inhibited by these compounds almost as strongly as trypsin; their IC₅₀ values were in the range of 0.008-4 ¦ÌM, which were much lower than that of the well-known trypsin/enteropeptidase inhibitor benzamidine.

Biomedical Research published new progress about 71079-09-9. 71079-09-9 belongs to catalysis-chemistry, auxiliary class Salt,Carboxylic acid,Carbamidine,Amine,Benzene,Ester,Protease,Ser/Thr Protease, name is 2-(4-((4-Guanidinobenzoyl)oxy)phenyl)acetic acid methanesulfonic acid salt, and the molecular formula is C17H19N3O7S, Safety of 2-(4-((4-Guanidinobenzoyl)oxy)phenyl)acetic acid methanesulfonic acid salt.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Beckh, Karlheinz published the artcileHepatic and pancreatic metabolism and biliary excretion of the protease inhibitor camostat mesilate, Computed Properties of 71079-09-9, the publication is International Journal of Pancreatology (1991), 10(3-4), 197-205, database is CAplus and MEDLINE.

The hepatic metabolism and biliary and pancreatic excretion of the serine protease inhibitor camostat mesilate and its metabolites FOY-251 and GBA were studied in rats in vivo and in situ liver-perfusion experiments After oral feeding (100 mg/kg) and i.v. infusion (5 mg/kg.h) of camostat mesilate, the original compound and both metabolites appeared in bile, but could not be detected in pancreatic juice. In plasma, only FOY-251 and GBA were detected. In the perfused rat liver, camostat mesilate (10 ¦ÌM) was eliminated by 33.8% and its molar rate of degradation to FOY-251 was 25.1%. During the study period about 0.1% of camostat mesilate and FOY-251 appeared in bile. The liver perfusion of FOY-251 or GBA revealed very low hepatic extraction rates of 10.3 and 2.4%, resp. In conclusion, the low hepatic extraction rate of camostat mesilate and its metabolites leads to high concentrations of the active metabolite FOY-251 in plasma. Camostat mesilate and its metabolites are effectively excreted into bile, but not in rat pancreatic juice.

International Journal of Pancreatology published new progress about 71079-09-9. 71079-09-9 belongs to catalysis-chemistry, auxiliary class Salt,Carboxylic acid,Carbamidine,Amine,Benzene,Ester,Protease,Ser/Thr Protease, name is 2-(4-((4-Guanidinobenzoyl)oxy)phenyl)acetic acid methanesulfonic acid salt, and the molecular formula is C17H19N3O7S, Computed Properties of 71079-09-9.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Otsuki, Makoto published the artcileTherapeutic effects of camostat on caerulein-induced acute pancreatitis in rats, Application In Synthesis of 71079-09-9, the publication is Biomedical Research (1989), 10(Suppl. 1), 25-31, database is CAplus.

Acute pancreatitis was induced in rats by 4 s.c. injections of caerulein (20 ¦Ìg/kg) at hourly intervals. The animals were then given either 100 mg camostat/kg or 0.05M phosphate buffer via gastric tube 30 min after the last caerulein injection. The elevation of serum amylase activity in rats treated with caerulein was reduced by camostat treatment, and the peak value was seen 1 h earlier than that in the rats that did not receive camostat. This was accompanied by an alleviation of the histol. signs of acute pancreatitis, such as cellular infiltration and acinar cell vacuolization. After oral administration, camostat and its metabolite 4-(4-guanidinobenzoyloxy)phenylacetic acid were detectable in plasma for >6 h in concentrations high enough to have antiprotease activity. In addition, camostat stimulated endogenous secretin release. Oral administration of camostat may reduce the severity of caerulein-induced pancreatitis by releasing endogenous secretin and by its antiprotease activity.

Biomedical Research published new progress about 71079-09-9. 71079-09-9 belongs to catalysis-chemistry, auxiliary class Salt,Carboxylic acid,Carbamidine,Amine,Benzene,Ester,Protease,Ser/Thr Protease, name is 2-(4-((4-Guanidinobenzoyl)oxy)phenyl)acetic acid methanesulfonic acid salt, and the molecular formula is C17H19N3O7S, Application In Synthesis of 71079-09-9.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Otsuki, Makoto published the artcileBeneficial effects of the synthetic trypsin inhibitor camostate in cerulein-induced acute pancreatitis in rats, COA of Formula: C17H19N3O7S, the publication is Digestive Diseases and Sciences (1990), 35(2), 242-50, database is CAplus and MEDLINE.

The therapeutic effect and the mechanism of action of the synthetic trypsin inhibitor camostate were studied in a rat model of acute interstitial pancreatitis induced by caerulein. Rats with acute pancreatitis were given either 100 mg/kg body weight camostate or water via an orogastric tube 30 min after the caerulein injection. The elevation of serum amylase activity was reduced by camostate treatment and the peak value was seen 1 h earlier than that observed in the control group. Camostate also inhibited the reduction in pancreatic content of lipase and amylase seen during exptl. pancreatitis. These effects were accompanied by alleviation of the histol. signs of acute pancreatitis such as cellular infiltration and acinar cell vacuolization. After oral administration, camostate and its metabolite were absorbed from the intestine and were detectable in plasma for >6 h in concentrations high enough to have antiprotease activity. In addition, camostate in the duodenum was able to increase pancreatic juice flow and protein output and to stimulate endogenous secretin release. Thus, oral administration of camostate reduces the severity of caerulein-induced acute pancreatitis by releasing endogenous secretin and by its antiprotease activity.

Digestive Diseases and Sciences published new progress about 71079-09-9. 71079-09-9 belongs to catalysis-chemistry, auxiliary class Salt,Carboxylic acid,Carbamidine,Amine,Benzene,Ester,Protease,Ser/Thr Protease, name is 2-(4-((4-Guanidinobenzoyl)oxy)phenyl)acetic acid methanesulfonic acid salt, and the molecular formula is C17H19N3O7S, COA of Formula: C17H19N3O7S.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Goeke, B. published the artcileStudies on the effect of FOY-305 on the pancreatic secretion of rats in vivo, HPLC of Formula: 71079-09-9, the publication is Verhandlungen der Deutschen Gesellschaft fuer Innere Medizin (1984), 1067-70, database is CAplus.

FOY-305??[59721-29-8] (0.1-5.0 mg/kg/h) administered i.v. to rats inhibited trypsin??[9002-07-7], but not amylase, activity in pancreatic juice was dependent on the dose. Pancreatic juice volume was not affected. FOY-251??[71079-09-9], a metabolite of FOY-305, was found in pancreatic juice and homogenates of rat pancreas after FOY-305 treatment and may be responsible for the antitryptic activity.

Verhandlungen der Deutschen Gesellschaft fuer Innere Medizin published new progress about 71079-09-9. 71079-09-9 belongs to catalysis-chemistry, auxiliary class Salt,Carboxylic acid,Carbamidine,Amine,Benzene,Ester,Protease,Ser/Thr Protease, name is 2-(4-((4-Guanidinobenzoyl)oxy)phenyl)acetic acid methanesulfonic acid salt, and the molecular formula is C17H19N3O7S, HPLC of Formula: 71079-09-9.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Goeke, B. published the artcileEffect of a specific serine protease inhibitor on the rat pancreas: systemic administration of camostat and exocrine pancreatic secretion, HPLC of Formula: 71079-09-9, the publication is Digestion (1984), 30(3), 171-8, database is CAplus and MEDLINE.

Camostat??[59721-28-7], a synthetic serine?protease??[37259-58-8] inhibitor, specifically inhibits the trypsin??[9002-07-7] activity in vitro. Immediately after i.v. administration of camostat (5, 2.5, 0.5, and 0.1 mg/kg/h) the trypsin activity in the biliary-pancreatic juice was diminished dose-dependently in anesthetized rats. Amylase??[9000-92-4] release was not influenced. Camostat and its metabolites were detected by high-pressure liquid chromatog. in the pancreatic juice and tissue; in plasma, only the metabolites were found. Therefore, the inhibitory action of camostat on the trypsin activity in the biliary-pancreatic juice may be due to penetration of camostat into the juice.

Digestion published new progress about 71079-09-9. 71079-09-9 belongs to catalysis-chemistry, auxiliary class Salt,Carboxylic acid,Carbamidine,Amine,Benzene,Ester,Protease,Ser/Thr Protease, name is 2-(4-((4-Guanidinobenzoyl)oxy)phenyl)acetic acid methanesulfonic acid salt, and the molecular formula is C17H19N3O7S, HPLC of Formula: 71079-09-9.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Nishihata, Toshiaki published the artcileIntestinal absorption of N,N’-dimethylcarbamoylmethyl 4-(4-guanidinobenzoyloxy)phenylacetate methanesulfonate in rats, Synthetic Route of 71079-09-9, the publication is Chemical & Pharmaceutical Bulletin (1988), 36(7), 2544-50, database is CAplus and MEDLINE.

The intestinal absorption of N,N‘-dimethylcarbamoylmethyl 4-(4-guanidinobenzoyloxy)phenylacetate methanesulfonate (FOY305) in rats was investigated using a rat intestinal loop method. Plasma drug concentrations and the disappearance of the drug from the intestinal lumen were measured. The absorption of FOY305 after administration into a rectal loop was greater than those after administration into variously positioned small intestinal loops. The low absorption of FOY305 after administration into the small intestine was due to the rapid degradation of FOY305 by esterase activity in the small intestinal lumen. The results are discussed with respect to the development of an oral or rectal dosage form of FOY305.

Chemical & Pharmaceutical Bulletin published new progress about 71079-09-9. 71079-09-9 belongs to catalysis-chemistry, auxiliary class Salt,Carboxylic acid,Carbamidine,Amine,Benzene,Ester,Protease,Ser/Thr Protease, name is 2-(4-((4-Guanidinobenzoyl)oxy)phenyl)acetic acid methanesulfonic acid salt, and the molecular formula is C17H19N3O7S, Synthetic Route of 71079-09-9.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Kohri, Naonori published the artcileDevelopment of camostat mesilate troche for the prevention of induced mucositis in the mouth at cancer chemotherapy, Recommanded Product: 2-(4-((4-Guanidinobenzoyl)oxy)phenyl)acetic acid methanesulfonic acid salt, the publication is Yakuzaigaku (2001), 61(1), 34-45, database is CAplus.

We prepared a troche containing camostat mesilate for the prevention of the mucositis in the mouth induced by cancer chemotherapy. The troche was formed by the direct compression of a powder mixture of camostat mesilate, a flavoring agent, hydroxypropyl cellulose, and magnesium stearate. A troche containing 10% or 20% hydroxypropyl cellulose and a flavoring agent of coffee or green apple diminished the bitterness of camostat mesilate. It was found that the metabolizing rate of camostat in saliva was much slower than that in blood, although metabolites in saliva were the same kinds as those in blood. The amounts of camostat retained in the mouth after administration of the troche to healthy subjects were much larger than those after applying a gargle which had a bitter taste. Moreover, the troche containing the flavoring agent of green apple showed smaller amounts of camostat and its metabolites retained in the mouth compared to the troche containing the flavoring agent of coffee. It is considered that the increase in the secreting volume of saliva after administration of the troche containing the flavoring agent of green apple would prevent the retaining of camostat and its metabolites in the mouth. Moreover, the administration of a troche is more convenient than that of a gargle for patients. The troche prepared in this study would be a substitute dosage form for the gargle and promote the quality of life in patients.

Yakuzaigaku published new progress about 71079-09-9. 71079-09-9 belongs to catalysis-chemistry, auxiliary class Salt,Carboxylic acid,Carbamidine,Amine,Benzene,Ester,Protease,Ser/Thr Protease, name is 2-(4-((4-Guanidinobenzoyl)oxy)phenyl)acetic acid methanesulfonic acid salt, and the molecular formula is C17H19N3O7S, Recommanded Product: 2-(4-((4-Guanidinobenzoyl)oxy)phenyl)acetic acid methanesulfonic acid salt.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia