| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| 500mg |
| ln Vitro |
In RAW 264.7 macrophages, roxatidineacetate (0-120μM, 1 hour) suppresses inflammatory responses by blocking LPS-induced NF-κB and p38MAPK activation [2]. PMACI-induced p38MAPK activation is inhibited by roxatidineacetate (6.25 μM, 12.5 μM, and 25 μM; 30 min pretreatment), but phosphorylation of ERK and JNK is unaffected. Roxatidine had no effect on the levels of total ERK 1/2, JNK, or p38 MAPK in human mast cell-1 (HMC-1) cells [4].
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| ln Vivo |
Roxatidine acetate (0-300 mg/kg; oral; 26 days) slows the growth of colonic 38 tumor implants in mice [3]. Roxatidineacetate (oral gavage; 20 mg/kg; single dosage) suppresses compound 48/80-increased TNF-α, IL-6, and IL-1β production and mRNA expression. In addition, Roxatidine inhibits compound 48/80-induced procaspase-1 degradation and the formation of the matching cleavage band in mice [4].
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| Cell Assay |
Western Blot Analysis[2]
Cell Types: RAW 264.7 Tested Concentrations: 40, 80 and 120 μM Incubation Duration: 1 hour Experimental Results: Inhibition of LPS-induced PGE2, NO and histamine production as well as COX-2, iNOS and HDC expression. Inhibits the expression of TNF-α, IL-1β, IL-6 and VEGF-1. Nuclear translocation of p65 and p50 was attenuated in a concentration-dependent manner. Inhibits LPS-induced phosphorylation of p38 MAP kinase. Dramatically downregulates LPS-induced NO and PGE2 (prostaglandin E2) production. |
| Animal Protocol |
Animal/Disease Models: Male C57BL/6 colon38 mice (8 weeks old, 20 – 22 g) [3]
Doses: 30, 100 and 300 mg/kg daily, 1 ml/100 g body weight orally, from colon38 Day 29 started 3 days before implantation, or day 26 started simultaneously with colon 38 implantation. Experimental Results: After day 26, colon 38 tumor implant growth was inhibited in a dose-related manner. Inhibits VEGF levels in tumor tissues and Dramatically reduces serum VEGF levels. Animal/Disease Models: ICR male mice (6 weeks old) [4] Doses: 20 mg/kg Route of Administration: po (oral gavage); 20 mg/kg; single dose Experimental Results: Inhibition of compound 48/80 induction in allergic animal models allergic inflammation. |
| References |
[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.
[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. [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. [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. |
| Molecular Formula |
C19H28N2O4
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|---|---|
| Molecular Weight |
348.43662
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| CAS # |
78628-28-1
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| Related CAS # |
Roxatidine Acetate Hydrochloride;93793-83-0
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
CC(OCC(NCCCOC1=CC=CC(CN2CCCCC2)=C1)=O)=O
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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 | 2.8699 mL | 14.3497 mL | 28.6993 mL | |
| 5 mM | 0.5740 mL | 2.8699 mL | 5.7399 mL | |
| 10 mM | 0.2870 mL | 1.4350 mL | 2.8699 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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