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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作靶點(diǎn): Others作通路: Others儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) H2O : 34 mg/mL (15.61 mM)* means
2、 soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液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請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度,選擇合適的溶劑配制儲(chǔ)備液,并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Sugammadex sodium種合成的 環(huán)糊精衍物,作為新的神經(jīng)肌阻斷逆轉(zhuǎn)劑起作。體內(nèi)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 您邊的抑制劑師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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