| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
Revaprazan targets the gastric H(+)/K(+)-ATPase (proton pump). As a potassium-competitive acid blocker, it inhibits the proton pump in a reversible and K+-competitive manner. Unlike PPIs, which require acid activation to form a covalent bond, Revaprazan inhibits the pump directly without acid activation. It also targets the Akt signaling pathway to exert anti-inflammatory effects.
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|---|---|
| ln Vitro |
In vitro, Revaprazan reversibly inhibits gastric H(+)/K(+)-ATPase activity, suppressing acid production. It also demonstrates anti-inflammatory activity by inhibiting Helicobacter pylori-induced COX-2 expression through inactivation of Akt signaling. The compound provides protection to the gastric mucosa and inhibits the degradation of IkappaB-alpha. Its acid suppression is comparable to that of PPIs.
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| ln Vivo |
In vivo, Revaprazan effectively suppresses gastric acid secretion. It provides protection to the gastric mucosa. The compound has been studied for its therapeutic potential in chronic gastritis. Its mechanism of acid suppression is distinct from PPIs, as it does not require acid activation. Revaprazan has been used in clinical studies for the treatment of gastric acid-related disorders.
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| Enzyme Assay |
In vitro enzyme inhibition assays are performed using purified gastric H(+)/K(+)-ATPase from pig or rabbit gastric mucosa. The enzyme is incubated with Revaprazan in a buffer containing 20 mM Pipes-Tris (pH 6.5), 2 mM MgCl2, and 2 mM ATP. The reaction is initiated by adding KCl, and the enzyme activity is measured by determining the amount of inorganic phosphate released using a colorimetric method. IC50 values are calculated from dose-response curves.
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| Cell Assay |
In vitro cell-based assays are performed using gastric parietal cells or cell lines such as HGT-1. Cells are cultured in appropriate medium and treated with serial dilutions of Revaprazan for 24-72 hours. Acid production is measured using the [14C]-aminopyrine accumulation assay. COX-2 expression is assessed by Western blotting or qRT-PCR. Akt phosphorylation is evaluated by Western blotting. Cell viability is assessed using MTT assays.
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| Animal Protocol |
In vivo efficacy studies are conducted in animal models of gastric acid secretion, such as rats or dogs. Revaprazan is administered via oral or intravenous routes. Gastric acid secretion is measured by collecting gastric juice or by using a gastric fistula model. In models of chronic gastritis, animals are treated with the compound and gastric mucosal damage is assessed by histopathological examination. Anti-inflammatory effects are evaluated by measuring COX-2 expression and inflammatory cytokine levels in gastric tissues.
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| References |
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| Additional Infomation |
Revaprazan belongs to the isoquinoline class of drugs. Revaprazan is currently being studied in the clinical trial NCT01750437 (a phase II clinical trial evaluating the safety, tolerability, and efficacy of YH1885L in patients with non-erosive reflux disease). See also: Revaprazan hydrochloride (note moved to).
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| Molecular Formula |
C22H23FN4
|
|---|---|
| Molecular Weight |
362.45
|
| Exact Mass |
362.191
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| CAS # |
199463-33-7
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| Related CAS # |
178307-42-1 (HCl);199463-33-7;
|
| PubChem CID |
204104
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| Appearance |
Typically exists as solid at room temperature
|
| LogP |
5.237
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| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
27
|
| Complexity |
481
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1C=CC(NC2=NC(C)=C(C)C(N3CCC4=CC=CC=C4[C@@H]3C)=N2)=CC=1
|
| InChi Key |
LECZXZOBEZITCL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H23FN4/c1-14-15(2)24-22(25-19-10-8-18(23)9-11-19)26-21(14)27-13-12-17-6-4-5-7-20(17)16(27)3/h4-11,16H,12-13H2,1-3H3,(H,24,25,26)
|
| Chemical Name |
N-(4-fluorophenyl)-4,5-dimethyl-6-(1-methyl-3,4-dihydro-1H-isoquinolin-2-yl)pyrimidin-2-amine
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| Synonyms |
SB-641257; SB 641257; Revaprazan
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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 | 2.7590 mL | 13.7950 mL | 27.5900 mL | |
| 5 mM | 0.5518 mL | 2.7590 mL | 5.5180 mL | |
| 10 mM | 0.2759 mL | 1.3795 mL | 2.7590 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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