Roxatidine
Based on 1 Customer Validation
Roxatidine is an active metabolite of Roxatidine acetate hydrochloride, is an orally active histamine H2-receptor antagonist. Roxatidine, an anti-ulcer agent, suppresses histamine release (thus inhibiting proton secretion) and inhibits the production of VEGF-1, an important marker of inflammation and angiogenesis. Anti-allergic inflammatory effect. Roxatidine is promising for research of gastric and duodenal ulcers.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.25%
- CAS 番号: 78273-80-0
- 分子式: C17H26N2O3
- 分子量:306.41
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保管条件:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
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H2 Receptor |
Roxatidine (6.25-25 μM, 6 h 30 min) suppresses the PMACI-induced production of pro-inflammatory cytokines, NF-κB and caspase-1 activation, activation of p38 MAPK in HMC-1[1].
Roxatidine (40-120 μM, 1 h) inhibits the production of PGE2, NO, and histamine induced by LPS, as well as the expression of COX-2, iNOS, and HDC in RAW 264.7 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HMC-1 cells
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Concentration:6.25-25 μM
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Incubation Time:6 h 30 min
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Result:Down-regulated the PMACI-induced TNF-α, IL-6, and IL-1β production and their mRNA expression in a dose-dependent manner.
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Cell Line:HMC-1 cells
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Concentration:6.25-25 μM
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Incubation Time:60 min
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Result:Suppressed the PMACI-stimulated nuclear translocations of p65 subunit of NF-κB, phosphorylation and degradation of IκB-α, the PMACI-induced activation of p38 MAPK in HMC-1.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Compound 48/80-induced anaphylactic shock mouse model[1]
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Dosage:20 mg/kg
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Administration:p.o., a single dose for 1h before Compound 48/80 injection
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Result:Increased the survival rate to 20% at 60 min after compound 48/80 injection.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 78273-80-0
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性状 Oil
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分子量 306.41
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分子式 C17H26N2O3
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Color Colorless to light yellow
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SMILES
O=C(NCCCOC1=CC=CC(CN2CCCCC2)=C1)CO
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (326.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (271 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Portuguese - PT (392 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Lee M, et al. Roxatidine attenuates mast cell-mediated allergic inflammation via inhibition of NF-κB and p38 MAPK activation. Sci Rep. 2017;7:41721. Published 2017 Jan 31. [Content Brief]
[2]. Collins JD, et al. Pharmacokinetics of roxatidine in healthy volunteers. Drugs. 1988;35 Suppl 3:41-7. [Content Brief]
[3]. 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]
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. 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 | 1 mM | 3.2636 mL | 16.3182 mL | 32.6364 mL | 81.5911 mL |
| 5 mM | 0.6527 mL | 3.2636 mL | 6.5273 mL | 16.3182 mL | |
| 10 mM | 0.3264 mL | 1.6318 mL | 3.2636 mL | 8.1591 mL | |
| 15 mM | 0.2176 mL | 1.0879 mL | 2.1758 mL | 5.4394 mL | |
| 20 mM | 0.1632 mL | 0.8159 mL | 1.6318 mL | 4.0796 mL | |
| 25 mM | 0.1305 mL | 0.6527 mL | 1.3055 mL | 3.2636 mL | |
| 30 mM | 0.1088 mL | 0.5439 mL | 1.0879 mL | 2.7197 mL | |
| 40 mM | 0.0816 mL | 0.4080 mL | 0.8159 mL | 2.0398 mL | |
| 50 mM | 0.0653 mL | 0.3264 mL | 0.6527 mL | 1.6318 mL | |
| 60 mM | 0.0544 mL | 0.2720 mL | 0.5439 mL | 1.3599 mL | |
| 80 mM | 0.0408 mL | 0.2040 mL | 0.4080 mL | 1.0199 mL | |
| 100 mM | 0.0326 mL | 0.1632 mL | 0.3264 mL | 0.8159 mL |