ZaltidineH2-receptor antagonist CAS# 85604-00-8 |
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| Cas No. | 85604-00-8 | SDF | Download SDF |
| PubChem ID | 56051 | Appearance | Powder |
| Formula | C8H10N6S | M.Wt | 222.27 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | H2O : 7.69 mg/mL (34.60 mM; Need ultrasonic) | ||
| Chemical Name | 2-[4-(2-methyl-1H-imidazol-5-yl)-1,3-thiazol-2-yl]guanidine | ||
| SMILES | CC1=NC=C(N1)C2=CSC(=N2)N=C(N)N | ||
| Standard InChIKey | GIMNAEMRNXUAQP-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C8H10N6S/c1-4-11-2-5(12-4)6-3-15-8(13-6)14-7(9)10/h2-3H,1H3,(H,11,12)(H4,9,10,13,14) | ||
| 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. | ||
Zaltidine Dilution Calculator
Zaltidine Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 4.499 mL | 22.4952 mL | 44.9903 mL | 89.9807 mL | 112.4758 mL |
| 5 mM | 0.8998 mL | 4.499 mL | 8.9981 mL | 17.9961 mL | 22.4952 mL |
| 10 mM | 0.4499 mL | 2.2495 mL | 4.499 mL | 8.9981 mL | 11.2476 mL |
| 50 mM | 0.09 mL | 0.4499 mL | 0.8998 mL | 1.7996 mL | 2.2495 mL |
| 100 mM | 0.045 mL | 0.225 mL | 0.4499 mL | 0.8998 mL | 1.1248 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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Description: IC50 Value: N/A Zaltidine is a H2-receptor antagonist, which has the antisecretory action. in vitro: N/A in vivo: In eight healthy male volunteers single oral doses of 5 mg, 25 mg and 100 mg produced dose-related inhibition of basal and pentagastrin-stimulated acid output (M.A.O.) with an estimated ID50 of 40 mg for the latter. In eight subjects with duodenal ulceration single 100 mg and 200 mg doses produced 85% and 97% inhibition of M.A.O. at peak (3 h post-dose) and 20% and 23% inhibition at 24 h, respectively; inhibition of basal acid output was 97% at 3 h and 50% at 24 h with both doses [1]. One hundred and thirty-five patients were randomly allocated to 4 weeks' treatment with either 150 mg zaltidine once daily or placebo. Fifty-nine were treated for a full 4 weeks with zaltidine before the trial was stopped. Healing rates after 4 weeks of zaltidine and placebo were 86% and 19%, respectively (p less than 0.001) [2]. Clinical trial: N/A
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Zaltidine: an effective but hepatotoxic H2-receptor antagonist.[Pubmed:2902681]
Scand J Gastroenterol. 1988 Aug;23(6):655-8.
Zaltidine is a new H2-receptor antagonist. This study compares the safety and efficacy of Zaltidine with those of placebo in the short-term treatment of duodenal ulcer. One hundred and thirty-five patients were randomly allocated to 4 weeks' treatment with either 150 mg Zaltidine once daily or placebo. Fifty-nine were treated for a full 4 weeks with Zaltidine before the trial was stopped. Healing rates after 4 weeks of Zaltidine and placebo were 86% and 19%, respectively (p less than 0.001). Five patients in the Zaltidine group had increased serum aminotransferase levels at the final (4-week) visit. The values normalized when treatment was stopped. Liver biopsy specimens provide strong evidence of drug-induced injury. Hepatic damage was associated with plasma levels of Zaltidine in the upper half of the observed range. Zaltidine appears to be an effective treatment of duodenal ulcer. However, the incidence of hepatic damage (8%) seems higher than with commonly used H2-receptor antagonists.
The antisecretory effects of zaltidine, a novel long-acting H2-receptor antagonist, in healthy volunteers and in subjects with a past history of duodenal ulcer.[Pubmed:2876724]
Br J Clin Pharmacol. 1986 Oct;22(4):395-9.
The potency and duration of the antisecretory action of Zaltidine, a novel H2-receptor antagonist, have been examined in healthy volunteers and in patients with previous duodenal ulceration. In eight healthy male volunteers single oral doses of 5 mg, 25 mg and 100 mg produced dose-related inhibition of basal and pentagastrin-stimulated acid output (M.A.O.) with an estimated ID50 of 40 mg for the latter. In eight subjects with duodenal ulceration single 100 mg and 200 mg doses produced 85% and 97% inhibition of M.A.O. at peak (3 h post-dose) and 20% and 23% inhibition at 24 h, respectively; inhibition of basal acid output was 97% at 3 h and 50% at 24 h with both doses. The long duration of action of Zaltidine is ascribed to its relatively slow elimination from the plasma.
