Ketorolac-tromethamine-salt-Ketorolac-tris-salt-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEKetorolac tromethamine saltCat. No.: HY-B0138CAS No.: 74103-07-4Synonyms: Ketorolac tris salt; Ketorolac Tromethamine; RS37619tromethamine salt分式: CHNO分量: 376.4作靶點: COX作通路: Immunology/Inflammation儲存式: 4C, protect from light* In

2、solvent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性數(shù)據(jù)體外實驗 DMSO : 30 mg/mL (79.70 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.6567 mL 13.2837 mL 26.5675 mL5 mM 0.5313 mL 2.6567 mL 5.3135 mL10 mM 0.2657 mL 1.3284 mL 2.6567 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解

3、度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄清的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (5.53 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD

4、in saline)Solubility: 2.08 mg/mL (5.53 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (5.53 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Ketorolac tromethamine salt (Ketorolac tris salt)種甾體抗炎劑，為選擇性的 COX 抑制劑，對 COX-1 和 COX-2 的

5、 IC50 值分別為 20 nM 和 120 nM。IC50 & Target COX-1 COX-220 nM (IC50) 120 nM (IC50)體外研究 Ketorolac is a non-steroidal anti-inflammatory agent, acting as a nonselective COX inhibitor, with IC50s of 20nM for COX-1 and 120 nM for COX-2 1.體內(nèi)研究 Ketorolac tromethamine (0.4%) causes nearly complete inhibition on

6、LPS endotoxin-induced increases inFITC-dextran in the anterior chamber, and increases in aqueous PGE2 concentrations in the aqueous humorin rabbits 1.Ketorolac (30 mg/kg, i.v.) rapidly reverses hyperalgesia in rats. Ketorolac also reducescarrageenan-induced hyperalgesia and paw PG production, and ca

7、uses reduction in PGE2 levels in rats 1.Ketorolac (4 mg/kg/day, p.o.) has no detrimental effect in the volume fraction of bone trabeculae formedinside the alveolar socket in rats 2. Ketorolac (60 g/10 L) reduces the histological changes such asischemic cell death, including cytoplasmic eosinophilia

8、with disintegration of cytoarchitecture and nuclearpyknosis in rats. Ketorolac also effectively reduces neuronal death and improves hindlimb motor function,and the long-term survival is similar to that in the control group 3.PROTOCOLAnimal Rats 2Administration 2 Treated rats receive oral doses of 1

9、mL aqueous solution of paracetamol (80 mg/kg/rat/day), Ketorolac (4mg/kg/day) or etoricoxib (10 mg/kg/day) administered by gavage from the day of surgery until death, 2 weekslater. Control rats receive tap water (1 mL/day by gavage). The animals are housed under climate-controlledenvironment (12 h l

10、ight/12 h dark, 20-24C) with free access to standard laboratory chow and tap water 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Waterbury LD, et al. Comparison of cyclooxygenase inhibitory activity and ocular anti-inflammatory effects

11、of ketorolac tromethamineand bromfenac sodium. Curr Med Res Opin. 2006 Jun;22(6):1133-40.2. Fracon RN, et al. Treatment with paracetamol, ketorolac or etoricoxib did not hinder alveolar bone healing: a histometric study in rats. JAppl Oral Sci. 2010 Dec;18(6):630-4.3. Hsieh YC, et al. Intrathecal ketorolac pretreatment reduced spinal cord ischemic injury in rats. Anesth Analg. 2005 Apr;100(4):1134-9.McePdfHeight2/2 Master of Small Molecules 您邊的抑制劑師www.MedChemECaution: Product