Roxatidine Acetate Hydrochloride
Based on 1 Customer Validation
Roxatidine Acetate Hydrochloride is a potent, selective, competitive and orally active histamine H2-receptor antagonist. Roxatidine Acetate Hydrochloride has antisecretory potency against gastric acid secretion. Roxatidine Acetate Hydrochloride can also suppress inflammatory responses and can be used for gastric and duodenal ulcers research. Roxatidine Acetate Hydrochloride has antitumor activity.
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- Pureza : 99.57%
- No. CAS: 93793-83-0
- Fòrmula: C19H29ClN2O4
- Peso molecular:384.90
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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HY-B0281A
Ranitidine hydrochlorideHistamine H2-Receptor Antagonist -
HY-B0305AR
Roxatidine Acetate Hydrochloride (Standard)Histamine H2 Receptor Antagonist -
HY-B0310
NizatidineHistamine H2 receptor Antagonist -
HY-B0310R
Nizatidine (Standard)Histamine H2 receptor Antagonist -
HY-B0281AR
Ranitidine hydrochloride (Standard)Standard of Ranitidine hydrochloride
Ver todos los productos específicos de isoformas Histamine Receptor
More
Actividad biológica
Descripciòn
IC50 & Target
[1]|
H2 Receptor |
In Vitro
Roxatidine Acetate Hydrochloride (0-120 μM, 1 h) suppresses inflammatory responses via inhibition of NF-κB and p38 MAPK activation in LPS-induced RAW 264.7 macrophages[2].
Roxatidine Acetate Hydrochloride (6.25 ?μM, 12.5?μM, and 25?μM; pre-treatment for 30?min) suppresses the PMACI-induced activation of p38 MAPK, but does not affect the phosphorylation of ERK or JNK. The total ERK 1/2, JNK, and p38 MAPK levels are unaffected by roxatidine in human mast-cells-1 (HMC-1) cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:RAW 264.7
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Concentration:40, 80, and 120 μM
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Incubation Time:1 h
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Result:Suppressed LPS-induced PGE2, NO, and histamine production and COX-2, iNOS, and HDC expressions. Inhibited expressions of TNF-α, IL-1β, IL-6, and VEGF-1. Concentration-dependently attenuated the nuclear translocations of p65 and p50. Inhibited LPS-induced phosphorylation of p38 MAP kinase. Significantly down-regulated the LPS-induced productions of NO and PGE2 (prostaglandin E2).
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 Colon 38-bearing mice (8-week-old, 20 – 22 g)[3]
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Dosage:30, 100, and 300 mg/kg per day, 1 ml/100 g body weight
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Administration:Oral administration, 29 days beginning 3 days before Colon 38 implantation or 26 days beginning concomitantly with Colon 38 implantation
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Result:Suppressed growth of Colon 38 tumor implants in a dose-related manner after day 26. Suppressed VEGF levels in tumor tissue and significantly decreased serum VEGF levels.
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Animal Model:ICR male mice (6 weeks old)[1]
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Dosage:20 mg/kg
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Administration:Oral gavage; 20 mg/kg; single dose
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Result:Suppressed compound 48/80-induced allergic inflammation in anaphylactic animal model.
Chemical Information
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No. CAS 93793-83-0
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Appearance Solid
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Peso molecular 384.90
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Fòrmula C19H29ClN2O4
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Color White to off-white
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SMILES
O=C(NCCCOC1=CC=CC(CN2CCCCC2)=C1)COC(C)=O.Cl
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Synonyms
HOE 760
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvente y solubilidad
In Vitro:
DMSO : 50 mg/mL (129.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 50 mg/mL (129.90 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 140 mg/mL (363.73 mM); Clear solution; Need ultrasonic
Protocolo
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Murdoch D, et al. Roxatidine acetate. A review of its pharmacodynamic and pharmacokinetic properties, and its therapeutic potential in peptic ulcer disease and related disorders. Drugs. 1991 Aug;42(2):240-60. [Content Brief]
[2]. Cho EJ, et al. Roxatidine suppresses inflammatory responses via inhibition of NF-κB and p38 MAPK activation in LPS-induced RAW 264.7 macrophages. J Cell Biochem. 2011 Dec;112(12):3648-59. [Content Brief]
[3]. Tomita K, et al. Roxatidine- and cimetidine-induced angiogenesis inhibition suppresses growth of colon cancer implants in syngeneic mice. J Pharmacol Sci. 2003 Nov;93(3):321-30. [Content Brief]
[4]. Minho Lee, et al. Roxatidine attenuates mast cell-mediated allergic inflammation via inhibition of NF-κB and p38 MAPK activation. Sci Rep. 2017 Jan 31;7:41721. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 2.5981 mL | 12.9904 mL | 25.9808 mL | 64.9519 mL |
| 5 mM | 0.5196 mL | 2.5981 mL | 5.1962 mL | 12.9904 mL | |
| 10 mM | 0.2598 mL | 1.2990 mL | 2.5981 mL | 6.4952 mL | |
| 15 mM | 0.1732 mL | 0.8660 mL | 1.7321 mL | 4.3301 mL | |
| 20 mM | 0.1299 mL | 0.6495 mL | 1.2990 mL | 3.2476 mL | |
| 25 mM | 0.1039 mL | 0.5196 mL | 1.0392 mL | 2.5981 mL | |
| 30 mM | 0.0866 mL | 0.4330 mL | 0.8660 mL | 2.1651 mL | |
| 40 mM | 0.0650 mL | 0.3248 mL | 0.6495 mL | 1.6238 mL | |
| 50 mM | 0.0520 mL | 0.2598 mL | 0.5196 mL | 1.2990 mL | |
| 60 mM | 0.0433 mL | 0.2165 mL | 0.4330 mL | 1.0825 mL | |
| 80 mM | 0.0325 mL | 0.1624 mL | 0.3248 mL | 0.8119 mL | |
| 100 mM | 0.0260 mL | 0.1299 mL | 0.2598 mL | 0.6495 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Roxatidine Acetate Hydrochloride Related Classifications
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