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SB-649868
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SB-649868图片
CAS NO:380899-24-1
包装:5mg, 10mg
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品名称
GSK649868
产品介绍

生物活性

SB-649868是一种口服有效的选择性 OX1 和 OX 2 受体拮抗剂,作用于 OX1 和 OX2 受体的pKi值分别为 9.4 和 9.5。雄性CD大鼠的药代动力学研究,以1 mg/kg,静脉注射和3 mg/kg po进行,表明对于在血浆中具有中等清除率的催眠药(Clp = 24 mL/min/kg),具有优异的药代动力学特征,半衰期短(<0.6 h),分布容积小(V ss = 1.1 l/kg),口服生物利用度极佳(F = 85%),血浆暴露量良好(Cmax)= 333 ng/mL)。SB-649868,在剂量为1,3和10 mg/kg的OX-A注射前3小时口服给药,引起剂量依赖性的OX-A诱导的梳理减少,如通过梳理的总时间和梳理次数所测量的(p < 0.01,以3和10 mg/kg po)。


化学数据

分子量477.55
分子式C26H24FN3O3S
CAS号380899-24-1
纯度>98%
溶解性(25°C)DMSO 10 mM
储存和运输条件固体粉末: -20°C 冷藏长期储存
常温运输及临时存放

实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)

细胞实验
细胞系Chinese Hamster Ovary (CHO) cells
方法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), 2 mg/mL glutamine, 600 μg/ml geneticin at 37 °C 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 400 μg/mL geneticin, at 37 °C 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 1×104cells per well and cultured for 24 h in the presence of 5 mM sodium butyrate while OX2-CHO cells are seeded at the cell density of 4×104cells per well and cultured for 24 h in culture medium. After washings Hank's Balanced Salt Solution (HBSS) at room temperature containing 20 mM HEPES pH 7.4, 50 mM, 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 °C. 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 615 nm and 665 nm are measured with Envision Multilabel flash lamp reader with 100 flashes and 400 μs integration time.
浓度final DMSO concentration not exceeding 0.5% for functional studies and 1% for binding studies
处理时间45 min

动物实验
动物模型
配制
剂量
给药处理

不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

小鼠大鼠豚鼠仓鼠
重量 (kg)0.020.151.80.40.0810
体表面积 (m2)0.0070.0250.150.050.020.5
Km系数36128520
动物 A (mg/kg) = 动物 B (mg/kg) × 动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。


储备液配制

以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass1 mg5 mg10 mg
1 mM2.094 mL10.4701 mL20.9402 mL
5 mM0.4188 mL2.094 mL4.188 mL
10 mM0.2094 mL1.047 mL2.094 mL