| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg | |||
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| Targets |
Zaltidine targets the histamine H2 receptor on gastric parietal cells. As an H2 receptor antagonist, it blocks the binding of histamine to H2 receptors, thereby reducing the stimulant effect of histamine on gastric acid secretion. This reduces gastric acid production. Zaltidine is a highly specific H2 receptor antagonist with antisecretory activity.
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| ln Vitro |
In vitro, Zaltidine is a highly specific H2 receptor antagonist with antisecretory activity. It reduces the stimulant effect of histamine on gastric acid secretion by binding to histamine H2 receptors on gastric parietal cells. Its activity is assessed using receptor binding assays and functional assays measuring gastric acid secretion.
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| ln Vivo |
In vivo activity data for Zaltidine are limited in the available literature. As an H2 receptor antagonist, it has been studied for its ability to reduce gastric acid secretion in vivo. Its anti-secretory action makes it a valuable tool for studying gastric acid secretion and related disorders, but systematic in vivo studies are not extensively documented.
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| Enzyme Assay |
In vitro receptor binding assays for Zaltidine are performed using membrane preparations expressing histamine H2 receptors. Radioligand competition binding assays are used to measure the compound's affinity for H2 receptors. Functional assays measure the compound's ability to inhibit histamine-induced gastric acid secretion in isolated gastric gland preparations or parietal cell cultures.
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| Cell Assay |
In vitro cellular assays for Zaltidine are performed using gastric parietal cells or gastric gland preparations. Cells are treated with histamine and increasing concentrations of the compound. Gastric acid secretion is measured by assessing proton production (e.g., using the [¹⁴C]-aminopyrine accumulation assay). The inhibition of acid secretion is quantified.
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| Animal Protocol |
In vivo animal experiments for Zaltidine are not extensively documented. As a research compound, in vivo studies would typically involve administration to animal models of gastric acid hypersecretion or peptic ulcer disease. The compound would be administered via oral or parenteral routes, and efficacy would be assessed by measuring gastric acid output, ulcer formation, and gastric pH.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Zaltidine have been characterized in part. The compound has a molecular weight of 222.27 and molecular formula C₈H₁₀N₆S. Its chemical name is 2-[4-(2-methyl-1H-imidazol-5-yl)-1,3-thiazol-2-yl]guanidine. It is supplied with purity >98%. Further PK studies are needed to determine its absorption, distribution, metabolism, and excretion profile.
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| Toxicity/Toxicokinetics |
Toxicological data for Zaltidine are not extensively reported. As a research-use compound, its safety profile has not been formally evaluated in comprehensive preclinical toxicology studies. The compound is intended for research purposes only and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling this compound.
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| References |
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| Additional Infomation |
Zaltidine is also known as CP-57361. It is a histamine H2 receptor antagonist with anti-secretory activity. It is used in gastrointestinal research to study gastric acid secretion, peptic ulcers, and gastroesophageal reflux disease (GERD). This product is for research use only.
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| Molecular Formula |
C8H10N6S
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|---|---|
| Molecular Weight |
222.2702
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| Exact Mass |
222.069
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| CAS # |
85604-00-8
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| Related CAS # |
85604-00-8;90274-23-0 (HCl);
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| PubChem CID |
56051
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.7g/cm3
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| Boiling Point |
622.9ºC at 760 mmHg
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| Flash Point |
330.5ºC
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| Index of Refraction |
1.844
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| LogP |
2.147
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
15
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| Complexity |
254
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
GIMNAEMRNXUAQP-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
2-[4-(2-methyl-1H-imidazol-5-yl)-1,3-thiazol-2-yl]guanidine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~7.69 mg/mL (~34.60 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.4990 mL | 22.4952 mL | 44.9903 mL | |
| 5 mM | 0.8998 mL | 4.4990 mL | 8.9981 mL | |
| 10 mM | 0.4499 mL | 2.2495 mL | 4.4990 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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