| Size | Price | Stock | Qty |
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| 500mg |
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| 1g |
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| 2g |
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| 5g |
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| Other Sizes |
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Purity: ≥98%
Roxatidine Acetate HCl (HOE-760; TZU0460; HOE760; TZU-0460; Gastralgin; Altat; Roxit), the hydrochloride salt of Roxatidine Acetate, is a specific and competitive histamin H2-receptor antagonist with antiulcer activity. It suppresses histamin H2-receptor with an IC50 of 3.2 μM. The production of ulcers and gastric acid secretion are inhibited by roxatidine acetate. The medication roxatidine acetate is used to treat a number of conditions, including gastritis, erosive esophagitis, gastro-oesophageal reflux disease, and gastric ulcers.
| Targets |
Histamine H2 receptor ( IC50 = 3.2 μM )
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| ln Vitro |
Roxatidine Acetate Hydrochloride (0-120 μM, 1 h) inhibits NF-κB and p38 MAPK activation in LPS-induced RAW 264.7 macrophages, thereby suppressing inflammatory responses[2].
Roxatidine acetate hydrochloride (6.25 μM, 12.5 μM, and 25 μM; 30 min pre-treatment) inhibits the activation of p38 MAPK induced by PMACI, but has no effect on ERK or JNK phosphorylation. In human mast-cells-1 (HMC-1) cells, roxatidine has no effect on the levels of total ERK 1/2, JNK, and p38 MAPK[4]. |
| ln Vivo |
Roxatidine Acetate Hydrochloride (0-300 mg/kg; p.o.; 26 days) inhibited the growth of Colon 38 tumor implants in mice[3].
Roxatidine Acetate Hydrochloride (oral gavage; 20 mg/kg; single dose) suppresses the increased mRNA expression and production of TNF-α, IL-6, and IL-1β caused by Compound 48/80. Furthermore, procaspase-1's compound 48/80-induced degradation and the corresponding cleaved bands' appearance in mice are both reduced by roxatidine acetate hydrochloride[4]. |
| Cell Assay |
Cell Line: RAW 264.7
Concentration: 40, 80, and 120 μM Incubation Time: 1 h Result: suppressed PGE2, NO, and histamine production as well as the expressions of COX-2, iNOS, and HDC brought on by LPS. suppressed the expression of VEGF-1, IL-1β, TNF-α, and IL-6. p65 and p50 nuclear translocations were attenuated in a concentration-dependent manner. p38 MAP kinase phosphorylation induced by LPS was inhibited. markedly reduced the NO and PGE2 (prostaglandin E2) productions induced by LPS. |
| Animal Protocol |
Male C57BL/6 Colon 38-bearing mice (8-week-old, 20 – 22 g)[3]
30, 100, and 300 mg/kg per day, 1 ml/100 g body weight Oral administration, 29 days beginning 3 days before Colon 38 implantation or 26 days beginning concomitantly with Colon 38 implantation |
| References |
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| Molecular Formula |
C19H29CLN2O4
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| Molecular Weight |
384.9
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| Exact Mass |
384.18
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| Elemental Analysis |
C, 59.29; H, 7.59; Cl, 9.21; N, 7.28; O, 16.63
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| CAS # |
93793-83-0
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| Related CAS # |
Roxatidine acetate; 78628-28-1
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| Appearance |
Solid powder
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| SMILES |
CC(=O)OCC(=O)NCCCOC1=CC=CC(=C1)CN2CCCCC2.Cl
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| InChi Key |
FEWCTJHCXOHWNL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H28N2O4.ClH/c1-16(22)25-15-19(23)20-9-6-12-24-18-8-5-7-17(13-18)14-21-10-3-2-4-11-21;/h5,7-8,13H,2-4,6,9-12,14-15H2,1H3,(H,20,23);1H
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| Chemical Name |
[2-oxo-2-[3-[3-(piperidin-1-ylmethyl)phenoxy]propylamino]ethyl] acetate;hydrochloride
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| Synonyms |
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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, avoid exposure to moisture. |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 140 mg/mL (363.73 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5981 mL | 12.9904 mL | 25.9808 mL | |
| 5 mM | 0.5196 mL | 2.5981 mL | 5.1962 mL | |
| 10 mM | 0.2598 mL | 1.2990 mL | 2.5981 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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