| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
The primary target is the histamine H2 receptor found on gastric parietal cells. By antagonizing this receptor, it blocks the action of histamine, leading to a significant reduction in gastric acid secretion. Additionally, it suppresses inflammatory responses via inhibition of NF-kappaB and p38 MAPK activation. It also inhibits the production of the inflammation and angiogenesis marker VEGF-1.
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| ln Vitro |
Roxatidine is a histamine H2 receptor antagonist that blocks histamine-induced gastric acid secretion. In LPS-induced RAW 264.7 macrophages, it suppresses inflammatory responses via inhibition of NF-kappaB and p38 MAPK activation. It also reduces the production of VEGF-1, a marker for inflammation and angiogenesis. It attenuates the degradation of the extracellular matrix in osteoarthritis models.
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| ln Vivo |
Roxatidine is clinically used in vivo for the prevention and healing of gastric and duodenal ulcers and bleeding. It is an anti-ulcer drug that can inhibit histamine release (thus inhibiting proton secretion) and inhibit the production of VEGF-1, an important marker of inflammation and angiogenesis. It has anti-allergic inflammatory effects in animal models and attenuates degradation of extracellular matrix in osteoarthritis models.
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| Enzyme Assay |
For a cell-free receptor binding assay, membranes from cells expressing the human histamine H2 receptor are incubated with a radiolabeled H2 antagonist (e.g., [3H]-tiotidine) and increasing concentrations of Roxatidine (0.1 nM to 10 uM) in binding buffer (50 mM Tris-HCl, pH 7.5). After incubation at 25degC for 60-90 min, the mixture is filtered, and bound radioactivity is counted. The Ki value for Roxatidine is calculated from competition curves. Typically, these assays are performed in duplicate or triplicate to determine the binding affinity.
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| Cell Assay |
For in vitro cellular assays, RAW 264.7 macrophages are seeded in 24-well plates and treated with Roxatidine (0.1-100 uM) for 1 hour prior to stimulation with lipopolysaccharide (LPS, 1 ug/mL) for 24 hours. The culture supernatant is collected to measure the production of nitric oxide (NO) via the Griess assay and cytokine levels (TNF-alpha, IL-1beta, IL-6) by ELISA. Cells are also lysed for Western blot analysis of NF-kappaB p65 and p38 MAPK phosphorylation levels. The compound suppresses inflammatory responses via inhibition of these pathways.
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| Animal Protocol |
A typical in vivo protocol for testing anti-ulcer efficacy uses a rat model of gastric ulcer induced by indomethacin (20 mg/kg, PO) or ethanol. Roxatidine (10-50 mg/kg) is administered orally 30 minutes prior to ulcer induction. Animals are sacrificed 4-6 hours later, the stomachs are excised, and the ulcerated area is measured and scored. Gastric pH is measured to assess acid suppression. The reduction in ulcer index compared to control groups is calculated to determine the protective effect.
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| ADME/Pharmacokinetics |
Roxatidine (MW: 306.4, Formula: C17H26N2O3) is the active metabolite of the prodrug roxatidine acetate, which undergoes rapid and near-complete (>95%) oral absorption and is converted by esterases in the small intestine, plasma, and liver to its active metabolite, roxatidine. Its pharmacokinetics are characterized by rapid absorption and a plasma half-life suitable for once- or twice-daily dosing in clinical settings. It is soluble in DMSO up to 25 mg/ml.
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| Toxicity/Toxicokinetics |
Roxatidine is a clinically approved drug and has a well-documented safety profile. Common side effects include mild headache, diarrhea, and constipation. It is well-tolerated in clinical use. When used in research, standard precautions for handling pharmaceuticals should be followed. It is not associated with significant acute toxicity in animal models at therapeutic doses. The compound is intended for research use in laboratory settings or as a pharmaceutical reference standard.
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| References | |
| Additional Infomation |
Roxatidine is an organic molecular entity.
Roxatidine acetate hydrochloride (the prodrug) is a marketed anti-ulcer medication in some countries (e.g., Japan, South Korea). It belongs to the class of H2-receptor antagonists and works by reducing gastric acid secretion. Roxatidine (the active metabolite) is used as a research standard to study H2 receptor pharmacology, anti-ulcer mechanisms, and its anti-inflammatory effects. It is not approved in the US but is used in research worldwide. |
| Molecular Formula |
C17H26N2O3
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|---|---|
| Molecular Weight |
306.39994
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| Exact Mass |
306.194
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| CAS # |
78273-80-0
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| Related CAS # |
Roxatidine-d10 hemioxalate
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| PubChem CID |
91276
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| Appearance |
Colorless to light yellow solid powder
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| Density |
1.137 g/cm3
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| Boiling Point |
524.3ºC at 760 mmHg
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| Flash Point |
270.9ºC
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| LogP |
1.878
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
22
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| Complexity |
319
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CCN(CC1)CC2=CC(=CC=C2)OCCCNC(=O)CO
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| InChi Key |
BCCREUFCSIMJFS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H26N2O3/c20-14-17(21)18-8-5-11-22-16-7-4-6-15(12-16)13-19-9-2-1-3-10-19/h4,6-7,12,20H,1-3,5,8-11,13-14H2,(H,18,21)
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| Chemical Name |
2-hydroxy-N-[3-[3-(piperidin-1-ylmethyl)phenoxy]propyl]acetamide
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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) |
DMSO : ~100 mg/mL (~326.37 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 | 3.2637 mL | 16.3185 mL | 32.6371 mL | |
| 5 mM | 0.6527 mL | 3.2637 mL | 6.5274 mL | |
| 10 mM | 0.3264 mL | 1.6319 mL | 3.2637 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.
Link: https://clinicaltrials.gov/ct2/show/NCT02555852
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