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SB-649868  ≥98%

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包装规格：1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO(100mg/mL超声）
产品描述：基本信息 产品编号： S11205  产品名称： SB-649868 CAS: 380899-24-1   储存条件 粉末 -20℃ 四年     分子式： C26H24FN3O3S 溶于液体 -80℃ 6个月 分子量： 477.55 -20℃ 1个月 化学名：  (S)-N-((1-(5-(4-Fluorophenyl)-2-methylthiazole-4-carbonyl)piperidin-2-yl)methyl)benzofuran-4-carboxamide Solubility (25°C)：   体外:   DMSO   Ethanol   Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 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；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.0940mL 10.4701mL 20.9402mL 5mM 0.4188mL 2.0940mL 4.1880mL 10mM 0.2094mL 1.0470mL 2.0940mL   生物活性 产品描述 一种口服有效的选择性食欲素 OX1 和 OX 2 受体拮抗剂。 靶点 pKi:9.4 (OX1),9.5 (OX2)   体外研究 SB-649868 is identified as one the most in vitro potent dual OX1 and OX2 receptor antagonist known at that time (pKi=9.4 and 9.5 at the OX1 and OX2 receptor,respectively) .SB-649868 antagonizes orexin-A-induced inositol 1 phosphate (IP1) accumulation with the following pKB value (OX1=9.67;OX2=9.64).SB-649868 displaces the [3H]ACT-078573 receptor binding with the following pKi values:OX1=9.27;OX2=8.91.Increasing concentrations of SB-649868 (0.3nM-30nM) induces a rightward shift of the orexin-A CRCs with a depression of the agonist efficacy suggesting a clear non-surmountable behavior.The calculated apparent pKb values are 9.67±0.03 and 9.64±0.07 for OX1 and OX2. 体内研究 Pharmacokinetic studies in the male CD rat,performed at 1mg/kg,iv and 3mg/kg,po,demonstrate an excellent pharmacokinetic profile for a hypnotic agent featuring moderate clearance in plasma (Clp=24mL/min/kg), short half-life of (<0.6h) and a low volume of distribution (Vss=1.1l/kg),coupled with excellent oral bioavailability (F=85%) and good exposure in plasma (Cmax=333ng/mL).A brain to blood ratio (B/B) of 0.1:1 is observed 1h after iv administration,a value in line with the expected partition between the two compartments based on the lower tissue binding observed in vitro in brain tissues (fraction unbound/brain=5.28%) with respect to plasma proteins (fraction unbound/plasma=1.34%).SB-649868,administered orally 3h before OX-A injection at doses of 1,3 and 10mg/kg,causes a dose-dependent reduction of OX-A induced grooming as measured by total time spent grooming and number of grooming bouts (p<0.01 at 3 and 10mg/kg po).From dissociation kinetic studies using [3H]ACT-078573,the calculated long half-life,(t1/2) supports the nonsurmountability profile of SB-649868 (t1/2=35.91 min) at OX1 orexin receptor.The long or moderately long t1/2values for SB649868 at OX2 orexin receptor (t1/2=8.09 min).   推荐实验方法(仅供参考) 细胞实验:   Chinese Hamster Ovary (CHO) cells stably transfected with human OX1 orexin receptor are cultured in Dulbecco's modified Eagle's medium F12 Ham,supplemented with 10% fetal bovine serum (FBS),2mg/mL glutamine,600μg/ml geneticin at 37℃ in an atmosphere of 95% air and 5% CO2.CHO cells stably transfected with human OX2 orexin receptor are cultured in alpha-MEM supplemented with 10% FBS,100 units/mL penicillin G,100 units/mL streptomycin and 400μg/mL geneticin,at 37℃ in an atmosphere of 95% air and 5% CO2.Accumulation of IP1 is measured using IP-One HTRF terbium cryptate-based assay.OX1-CHO cells are seeded into white 384-well plate at the cell density of 1×104 cells per well and cultured for 24h in the presence of 5mM sodium butyrate while OX2-CHO cells are seeded at the cell density of 4×104 cells per well and cultured for 24h in culture medium.After washings Hank's Balanced Salt Solution (HBSS) at room temperature containing 20mM HEPES pH 7.4,50mM,LiCl and 0.1% Bovine Serum Albumin (BSA) cells are pre-incubated for 45 min with antagonist and then treated with agonist for 60 min at 37℃.Detection reagents,IP1-d2 tracer and anti-IP1-cryptate are diluted in lysis buffer and added to the cells.Following 60 min incubation at room temperature,time-resolved fluorescence at 615nm and 665nm are measured with Envision Multilabel flash lamp reader with 100 flashes and 400μs integration time.
保存条件：-20℃

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