| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
The primary molecular target of impromidine is the histamine H2 receptor, a G-protein-coupled receptor that mediates the effects of histamine on gastric acid secretion, cardiac contractility, and vascular smooth muscle relaxation. Impromidine acts as a full agonist at H2 receptors, activating Gs proteins and increasing cAMP levels. This stimulates gastric acid secretion from parietal cells and increases cardiac contractility. Impromidine shows selectivity for H2 over H1 receptors.
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|---|---|
| ln Vitro |
In vitro activity of impromidine has been characterized using radioligand binding assays and functional assays. In binding assays with H2 receptors, impromidine displaces radioligand binding with a Ki in the nanomolar range. In functional assays using cAMP accumulation or gastric acid secretion, it acts as a full agonist. Impromidine is more potent than histamine at H2 receptors.
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| ln Vivo |
In vivo activity of impromidine has been evaluated in animal models of gastric acid secretion and cardiovascular function. In rats and dogs, impromidine stimulates gastric acid secretion in a dose-dependent manner. It also increases heart rate and cardiac contractility. These effects are blocked by H2 receptor antagonists such as cimetidine.
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| Enzyme Assay |
In vitro H2 receptor binding assays for impromidine use membrane preparations from cells expressing recombinant H2 receptors or gastric mucosal membranes. Radiolabeled tiotidine or another H2 antagonist is used as the tracer. Impromidine is serially diluted and incubated with membranes and radioligand. Bound radioactivity is separated by filtration and quantified.
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| Cell Assay |
In vitro cell experiments with impromidine use parietal cells or cells expressing recombinant H2 receptors. Cells are cultured in standard media and treated with impromidine at concentrations ranging from 0.01 to 10 µM. cAMP accumulation is measured by ELISA. Gastric acid secretion is measured in isolated gastric glands.
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| Animal Protocol |
In vivo animal experiments with impromidine use rats or dogs. Impromidine is dissolved in saline and administered by intravenous injection or subcutaneous injection at doses ranging from 0.01 to 1 mg/kg. Gastric acid secretion is measured by pylorus ligation or pH monitoring. Heart rate and contractility are measured by ECG and echocardiography. All procedures follow institutional animal care guidelines.
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| Additional Infomation |
A highly effective and specific histamine H2 receptor agonist. It has been used as a diagnostic indicator of gastric secretion.
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| Molecular Formula |
C14H23N7S
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|---|---|
| Molecular Weight |
321.447
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| Exact Mass |
321.174
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| CAS # |
55273-05-7
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| Related CAS # |
65573-02-6 (tri-hydrochloride)
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| PubChem CID |
41376
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.34g/cm3
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| Boiling Point |
677.6ºC at 760 mmHg
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| Flash Point |
363.6ºC
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| Index of Refraction |
1.672
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| LogP |
2.302
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| tPSA |
130.57
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
22
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| Complexity |
339
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C(N=CN1)CSCCNC(=NCCCC2=CN=CN2)N
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| InChi Key |
MURRAGMMNAYLNA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H23N7S/c1-11-13(21-10-19-11)8-22-6-5-18-14(15)17-4-2-3-12-7-16-9-20-12/h7,9-10H,2-6,8H2,1H3,(H,16,20)(H,19,21)(H3,15,17,18)
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| Chemical Name |
2-[3-(1H-imidazol-5-yl)propyl]-1-[2-[(5-methyl-1H-imidazol-4-yl)methylsulfanyl]ethyl]guanidine
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| Synonyms |
Impromidinum; Impromidina; Impromidine
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 3.1109 mL | 15.5545 mL | 31.1090 mL | |
| 5 mM | 0.6222 mL | 3.1109 mL | 6.2218 mL | |
| 10 mM | 0.3111 mL | 1.5555 mL | 3.1109 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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