| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
H2 Receptor
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|---|---|
| ln Vitro |
With only a little amount of H1 activity and a significant selectivity towards H2 receptors, betzole (Ametazole) is a weak histamine agonist. The gastric inhibitory polypeptide (GIP) is secreted in response to betzole[1].
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| ADME/Pharmacokinetics |
Absorption, distribution, and excretion are rapid and complete.
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| Toxicity/Toxicokinetics |
Protein Binding
99% |
| References |
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| Additional Infomation |
Betazole is a pyrazole compound in which a hydrogen atom flanking a nitrogen atom is replaced by a 2-aminoethyl group. It is a histamine H2 receptor agonist used clinically to assess gastric secretion function. It has dual uses as a histamine agonist, diagnostic reagent, and gastrointestinal medication. It belongs to the pyrazole class of compounds and is a primary amino compound.
A histamine H2 receptor agonist used for the clinical assessment of gastric secretion function. Betazole is a histamine H2 receptor agonist with diagnostic applications. Betazole selectively targets and binds to H2 receptors, thereby mimicking the effects of histamine on these receptors. This may lead to increased gastric acid secretion. Betazole can be used for gastric function testing. A histamine H2 receptor agonist used clinically to assess gastric secretion function. Drug Indications For the clinical assessment of gastric secretion function. Mechanism of Action Betazole is a histamine analog. It has the same effect as histamine, acting by binding to H2 receptors, which are mediators of gastric acid secretion. This agonist effect leads to an increase in gastric acid secretion. Pharmacodynamics Betazol is a histamine H2 receptor agonist used to detect maximal gastric acid secretion or anacidity. This test can be used to diagnose conditions such as Zollinger-Ellison syndrome by measuring gastric acid secretion and basal secretion (more than 60% of the maximal acid secretion after betazol stimulation) after administration of betazol. Another test is to diagnose gastritis if gastric acid secretion is delayed and there is no response to betazol stimulation. Betazol can be used as a gastric secretion stimulant as an alternative to histamine, with the advantage of not causing side effects and therefore eliminating the need for antihistamines. |
| Molecular Formula |
C5H9N3
|
|---|---|
| Molecular Weight |
111.15
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| Exact Mass |
111.08
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| CAS # |
105-20-4
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| Related CAS # |
Betazole dihydrochloride;138-92-1
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| PubChem CID |
7741
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| Appearance |
Colorless to light yellow ointment
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| Density |
1.14g/cm3
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| Boiling Point |
284.1ºC at 760mmHg
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| Melting Point |
25°C
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| Flash Point |
150.3ºC
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| Vapour Pressure |
0.00303mmHg at 25°C
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| Index of Refraction |
1.567
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| LogP |
0.611
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
8
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| Complexity |
64.7
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(CN)C1=NNC=C1
|
| InChi Key |
JXDFEQONERDKSS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C5H9N3/c6-3-1-5-2-4-7-8-5/h2,4H,1,3,6H2,(H,7,8)
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| Chemical Name |
2-(1H-pyrazol-5-yl)ethanamine
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
DMSO: 250 mg/mL (2249.21 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (18.71 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (18.71 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (18.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 8.9969 mL | 44.9843 mL | 89.9685 mL | |
| 5 mM | 1.7994 mL | 8.9969 mL | 17.9937 mL | |
| 10 mM | 0.8997 mL | 4.4984 mL | 8.9969 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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