| Size | Price | Stock | Qty |
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| 5mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Niperotidine targets the histamine H2 receptor, a G protein-coupled receptor (GPCR). It acts as a selective antagonist at the H2 receptor. By blocking H2 receptors on gastric parietal cells, the compound inhibits gastric acid secretion. The compound is structurally related to ranitidine and belongs to the class of H2-receptor antagonists. Its mechanism involves competitive inhibition of histamine binding to the H2 receptor, thereby reducing acid production in the stomach. The compound also inhibits signaling pathways between GPCRs and G proteins.
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| ln Vitro |
In vitro studies have characterized Niperotidine as a histamine H2-receptor antagonist. The compound selectively blocks H2 receptors, inhibiting histamine-induced acid secretion in gastric parietal cell preparations. As an H2 antagonist structurally related to ranitidine, niperotidine's in vitro activity is comparable to other H2 receptor antagonists. The compound has been evaluated in various in vitro models of gastric acid secretion to confirm its mechanism of action and potency. Its binding affinity and selectivity for the H2 receptor have been characterized in radioligand binding studies.
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| ln Vivo |
An H2 blocker is niperotidine (pironyl-ranitidine). An antagonist of the H2 receptor with structural similarities to ranitidine is nipetidine. It is removed via enterohepatic circulation in urine or feces 60–120 minutes after oral dosing, when it reaches peak plasma levels [2].
In vivo studies have demonstrated that niperotidine is an effective H2 blocking agent. After oral administration, it reaches a plasmatic peak within 60-120 minutes. The compound inhibits nocturnal gastric acid secretion in healthy subjects. Niperotidine was proposed for the treatment of peptic ulcer based on its acid-suppressing effects. The compound undergoes enterohepatic circulation and is eliminated either in the urine or in the feces. Its in vivo profile is consistent with other H2 receptor antagonists. |
| Enzyme Assay |
The in vitro receptor binding assay for Niperotidine involves radioligand binding studies using membrane preparations from cells expressing the histamine H2 receptor. Competitive binding assays are performed with varying concentrations of niperotidine and a radiolabeled H2 receptor ligand to determine binding affinity (Ki or IC50). Functional assays measure the inhibition of histamine-stimulated cAMP production in cells expressing the H2 receptor. Data analysis using nonlinear regression models yields binding parameters and confirms the compound's interaction with the H2 receptor. Standard H2 receptor antagonist assays are employed.
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| Cell Assay |
In vitro cellular assays for Niperotidine are conducted using gastric parietal cells or cell lines expressing the histamine H2 receptor. Cells are treated with histamine to stimulate acid secretion, and varying concentrations of niperotidine are added to assess inhibition. Acid secretion is measured using pH indicators or by quantifying acid production. Alternatively, cAMP accumulation assays are performed, as H2 receptor activation stimulates cAMP production. The compound's ability to inhibit histamine-induced cAMP production is measured. Cell viability and specificity are confirmed using appropriate controls and receptor-selective antagonists.
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| Animal Protocol |
In vivo animal studies for Niperotidine are typically performed in rodents or dogs to evaluate gastric acid secretion inhibition. The compound is administered orally or intravenously, and gastric acid secretion is measured using pylorus ligation or gastric fistula models. The compound's effects on basal and stimulated acid secretion are assessed. Pharmacokinetic parameters including time to peak plasma concentration (60-120 min) and elimination routes are determined. Standard study designs with appropriate control groups are employed. Blood and urine samples are collected for pharmacokinetic analysis.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Niperotidine indicate that after oral administration, the compound reaches a plasmatic peak within 60-120 minutes. It is eliminated either in the urine or in the feces, with enterohepatic circulation. The compound has a molecular weight of 434.51 g/mol and a molecular formula of C20H26N4O5S. The compound's pharmacokinetic profile is consistent with other H2 receptor antagonists. Specific parameters such as half-life, bioavailability, and volume of distribution are not extensively reported in the available literature.
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| Toxicity/Toxicokinetics |
Toxicology data for Niperotidine are not extensively reported in the available literature. As an H2 receptor antagonist, the compound's safety profile would be similar to other drugs in this class, such as ranitidine and cimetidine. Common side effects of H2 antagonists include headache, dizziness, and gastrointestinal disturbances. Long-term use may be associated with vitamin B12 deficiency. However, specific toxicity data, including LD50 values and organ toxicity profiles, are not readily available. Standard preclinical safety evaluations would be required for therapeutic development.
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| References | |
| Additional Infomation |
See also: Niperotidine (note moved to).
Niperotidine (piperonyl-ranitidine) is a histamine H2-receptor antagonist structurally related to ranitidine. It inhibits gastric acid secretion by blocking H2 receptors on gastric parietal cells. The compound was proposed for the treatment of peptic ulcer and has a molecular formula of C20H26N4O5S and a molecular weight of 434.51 g/mol. After oral administration, it reaches a plasmatic peak within 60-120 minutes and undergoes enterohepatic circulation. It is a research compound and is not approved for therapeutic use. |
| Molecular Formula |
C20H26N4O5S
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|---|---|
| Molecular Weight |
434.50924
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| Exact Mass |
434.162
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| CAS # |
84845-75-0
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| PubChem CID |
3033952
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| Appearance |
Light yellow to brown solid powder
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| Density |
1.268g/cm3
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| Boiling Point |
566.324ºC at 760 mmHg
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| Flash Point |
296.302ºC
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| Index of Refraction |
1.591
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| LogP |
4.063
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
30
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| Complexity |
574
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN(C)CC1=CC=C(O1)CSCCN/C(=C\[N+](=O)[O-])/NCC2=CC3=C(C=C2)OCO3
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| InChi Key |
HXRSXEDVVARPHP-UDWIEESQSA-N
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| InChi Code |
InChI=1S/C20H26N4O5S/c1-23(2)11-16-4-5-17(29-16)13-30-8-7-21-20(12-24(25)26)22-10-15-3-6-18-19(9-15)28-14-27-18/h3-6,9,12,21-22H,7-8,10-11,13-14H2,1-2H3/b20-12+
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| Chemical Name |
(Z)-1-N'-(1,3-benzodioxol-5-ylmethyl)-1-N-[2-[[5-[(dimethylamino)methyl]furan-2-yl]methylsulfanyl]ethyl]-2-nitroethene-1,1-diamine
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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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~100 mg/mL (~230.14 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.75 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: 2.5 mg/mL (5.75 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3014 mL | 11.5072 mL | 23.0144 mL | |
| 5 mM | 0.4603 mL | 2.3014 mL | 4.6029 mL | |
| 10 mM | 0.2301 mL | 1.1507 mL | 2.3014 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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