ICI 162,846Potent H2 antagonist, active in vivo CAS# 84545-30-2 |
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Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
| Cas No. | 84545-30-2 | SDF | Download SDF |
| PubChem ID | 134778 | Appearance | Powder |
| Formula | C11H17F3N6O | M.Wt | 306.29 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble in ethanol and to 100 mM in DMSO | ||
| Chemical Name | 5-[3-[[N'-(2,2,2-trifluoroethyl)carbamimidoyl]amino]pyrazol-1-yl]pentanamide | ||
| SMILES | C1=CN(N=C1NC(=NCC(F)(F)F)N)CCCCC(=O)N | ||
| Standard InChIKey | ALCSGJCIESECFD-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C11H17F3N6O/c12-11(13,14)7-17-10(16)18-9-4-6-20(19-9)5-2-1-3-8(15)21/h4,6H,1-3,5,7H2,(H2,15,21)(H3,16,17,18,19) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | A potent histamine H2 receptor antagonist. |
ICI 162,846 Dilution Calculator
ICI 162,846 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.2649 mL | 16.3244 mL | 32.6488 mL | 65.2976 mL | 81.622 mL |
| 5 mM | 0.653 mL | 3.2649 mL | 6.5298 mL | 13.0595 mL | 16.3244 mL |
| 10 mM | 0.3265 mL | 1.6324 mL | 3.2649 mL | 6.5298 mL | 8.1622 mL |
| 50 mM | 0.0653 mL | 0.3265 mL | 0.653 mL | 1.306 mL | 1.6324 mL |
| 100 mM | 0.0326 mL | 0.1632 mL | 0.3265 mL | 0.653 mL | 0.8162 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Morphologic stomach findings in rats and mice treated with the H2 receptor antagonists, ICI 125,211 and ICI 162,846.[Pubmed:2903545]
Toxicol Pathol. 1988;16(2):299-304.
The gross and histopathologic findings seen in the stomachs of rats and mice treated with 2 different H2 receptor antagonists are presented. Studies with the first drug, ICI 125,211, elicited dysplasia/carcinoma lesions in 17 of 828 treated rats with 12 of the 17 lesions occurring in the pyloric region of the stomach. No tumors occurred in mice on study for 18 months. Studies conducted with another drug candidate, ICI 162,846, produced neuroendocrine carcinomas in the stomach of rats and mice. Twenty-five rats out of 312 treated male and female rats had neuroendocrine carcinomas in the gastric fundus with a higher tumor incidence in females. In a 24-month mouse study with ICI 162,846, 45 of 300 treated mice developed neuroendocrine carcinomas in the gastric fundus with a higher incidence in males.
Inhibition of human gastric secretion by ICI 162,846--a new histamine H2-receptor antagonist.[Pubmed:2874823]
Br J Clin Pharmacol. 1986 Jun;21(6):685-9.
The inhibitory effect of ICI 162,846, a new histamine H2-receptor antagonist, on gastric secretion of acid and pepsin was studied in 10 healthy male volunteers, aged 21-30 years. Single doses of 0.5, 1.0, 2.5 and 5.0 mg were given orally at 18:00 h. Overnight 12 h gastric secretion of acid was reduced by 69, 81, 91 and 95%, respectively. The inhibition of nocturnal output of pepsin was less than acid, with median decreases of 21, 42, 73 and 87%, respectively, of the output after administration of placebo. Intragastric concentration of acid, and values of intragastric pH, during the following 12 h of the day were not significantly affected by any of the doses of the drug. We conclude that ICI 162,846 is a powerful inhibitor of gastric secretion, with potential for use in the treatment of peptic diseases.
Acid blockade by omeprazole or ICI 162846 in a chronic duodenal ulcer model.[Pubmed:1716826]
Agents Actions. 1991 May;33(1-2):161-3.
Oral treatment with the H2-antagonist ICI 162,846 or omeprazole for five days inhibited both basal and pentagastrin stimulated acid secretion by 50% or more in mice. Either treatment increased the luminal secretion of histamine in the basal (12-fold) and stimulated (9-fold) states. Mice treated with the H2-antagonist had a 27% reduction (p less than 0.05) in mural histamine in the acid-producing area of the stomach. Mice were treated so as to induce duodenal ulcers (abscopal model) and were then treated with the H2-antagonist ICI 162,846, omeprazole or vehicle, orally for one week. Fewer duodenal ulcers were found in animals receiving drug treatments than in the oral vehicle group. Both the H2-receptor antagonist and the proton pump blocker inhibit acid production; acid blockade by either drug is accompanied by a massive increase in secretion of histamine. This rise was associated with depletion of the gastric histamine store only with H2-receptor blocker. Both means of acid inhibition reduce the formation of ulcers in this model.
