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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESugammadex sodiumCat. No.: HY-B0079CAS No.: 343306-79-6Synonyms: Org25969分式: CHNaOS分量: 2178.01作靶点: Others作通路: Others储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 H2O : 34 mg/mL (15.61 mM)* means
2、 soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 0.4591 mL 2.2957 mL 4.5913 mL5 mM 0.0918 mL 0.4591 mL 0.9183 mL10 mM 0.0459 mL 0.2296 mL 0.4591 mL请根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备液,并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Sugammadex sodium种合成的 环糊精衍物,作为新的神经肌阻断逆转剂起作。体内研究Inje
3、ction of sugammadex has no significant effects on blood pressure or heart rate. After injection of the highrocuronium dose, the 90% recovery of the train-of-four ratio takes 28 min (SD 7 min) after saline, 26 min (SD9.5 min) after 1 mg/kg sugammadex, and 8 min (SD 3.6 min) after 2.5 mg/kg sugammadex
4、 1. Sugammadex1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEcauses a rapid and complete reversal of rocuronium-induced neuromuscular block. The recovery time to trainof four ratio=0.9 after spontaneous recovery is 14.4 min (SD=3.4 min; n=14). This is reduced significantly to3.7 min (SD=3.3 min; n
5、=4) with sugammadex 0.5 mg/kg and to 1.9 min (SD=1.0 min; n=4) with sugammadex1.0 mg/kg 2. The estimated half-life of sugammadex in Rhesus monkey is 30 (SEM=4.9) min 3.PROTOCOLAnimal Female rhesus monkeys with a body weight of 5.2-7.1 kg are sedated with 10 mg/kg ketamineAdministration 1 intramuscul
6、arly. Two intravenous lines are placed: one for anesthetic administration, including rocuronium,the other for test drug administration. This is followed by intravenous injection of 25 mg/kg pentobarbitonesodium and a subsequent continuous infusion of 5-10 mg/kg/h. The monkeys are intubated endotrach
7、eally,and the lungs are ventilated with a mixture of oxygen and nitrous oxide (volume ratio of 2:3). Four animalsare each studied on three different occasions. The occasions differed by the administration of either saline ora low (1.0 mg/kg) or high (2.5 mg/kg) dose of sugammadex. Between the experi
8、ments, the monkeys recoverfor at least 6 weeks. Heart rate and oxygen saturation are determined at the ear with a pulse oximeter. Bloodpressure is determined with a cuff placed around the tail. Body temperature is measured by a rectal probeand kept at 37C-38C.MCE has not independently confirmed the
9、accuracy of these methods. They are for reference only.REFERENCES1. de Boer HD, et al. Reversal of profound rocuronium neuromuscular blockade by sugammadex in anesthetized rhesus monkeys.Anesthesiology. 2006 Apr;104(4):718-23.2. de Boer HD, et al. Sugammadex, a new reversal agent for neuromuscular b
10、lock induced by rocuronium in the anaesthetized Rhesusmonkey. Br J Anaesth. 2006 Apr;96(4):473-9. Epub 2006 Feb 7.3. de Boer HD, et al. Time course of action of sugammadex (Org 25969) on rocuronium-induced block in the Rhesus monkey, using asimple model of equilibration of complex formation. Br J Anaesth. 2006 Nov;97(5):681-6. Epub 2006 Oct 3.McePdfHeightCaution: Product has not been fully va
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