上海SB271046 209481-20-9价格供应产品资料
SB-271046
分子式：C20H22ClN3O3S2   分子量：451.99
质量标准：>98%，5-HT6受体拮抗剂
产品描述
SB-271046是口服生物有效的，选择性5-HT6受体拮抗剂，pKi为8.9,比作用于其他5-HT受体亚型选择性高200倍。
靶点
5-HT6
        
IC50
8.92 (pKi)
        
体外研究
SB-271046 also potently displaces [125I]-SB-258585 from rat ａnd pig striatal ａnd human caudate putamen membranes with pKis of 9.02, 8.55 ａnd 8.81, respectively. SB-271046 competitively antagonizes 5-HT-induced stimulation of adenylyl cyclase activity with a pA2 of 8.71.SB-271046 is found to be a competitive antagonist with a pA2 of 8.7 in the functional adenylyl cyclase assay which is in good agreement with its binding affinity. SB-271046 demonstrates no significant inhibitory activity at the major human P450 enzymes.
体内研究
SB-271046 produces an increase in seizure threshold over a wide-dose range in the rat maximal electroshock seizure threshold (MEST) test, with a minimum effective dose of 0.1 mg/kg p.o. ａnd maximum effect at 4 hours post-dose. The level of anticonvulsant activity achieves correlated well with the blood concentrations of SB-271046 (EC50 of 0.16 μM) ａnd brain concentrations of 0.01 μM–0.04 μM at Cmax.SB-271046 is moderately brain penetrant (10%), subject to low blood clearance (7.7 mL/min/kg) with a good half-life in rats (4.8 hours), ａnd has excellent oral bioavailability (>80%).SB-271046 produces 3-fold ａnd 2-fold increases in extracellular glutamate levels in both frontal cortex ａnd dorsal hippocampus of rats, respectively, which may be used for the treatment of cognitive ａnd memory dysfunction.SB-271046 (20 mg/kg, orally gavage) 30 min prior to training Wistar rats, is found to reverse significantly the amnesia produced by administering scopolamine (0.8 mg/kg, i.p.) in the 6 hours post-training period. SB-271046 progressively ａnd significantly decreases platform swim angle ａnd escape latencies over the five sequential trials on four consecutive daily sessions compared to vehicle-treated controls in aged rats. SB-271046 also improves task recall as measured by significant increases in the searching of the target quadrant on post-training days 1 ａnd 3.SB-271046 (10 mg/kg, s.c.) produces a significant, tetrodotoxin-dependent, increase in extracellular levels of both glutamate ａnd aspartate within the frontal cortex of rats, reaching maximum values of 375.4% ａnd 215.3% of preinjection values, respectively.
溶解性
DMSO 40 mg/mL，水 <1 mg/mL，乙醇 <1 mg/mL
稳定性
2年 -20°C粉状，6月-80°C溶于DMSO
上海SB271046 209481-20-9价格供应订购流程
告知客服人员209481-20-9这个CAS号，并告知您的需求量，让客服人员为您介绍包装跟价格！！！
上海SB271046 209481-20-9价格供应注意事项
产品图片仅供参考，以实物为准！国产进口均可提供！！！由于网站规则的限制，产品无法全部上传，有需要实验室产品尽可联系客服询价，万种产品随亲挑选，正规生物公司，可开具正规机打发票。厂家直销，价格优势！
任何试剂严禁用手直接触摸及用嘴尝，酸性或碱性液体溅至皮肤不得用中和剂处理，防止放热烧伤。
上海SB271046 209481-20-9价格供应常见问题
1，取用药品时要做到三不原则：不能用手接触药品。不要把鼻孔凑到容器口直接去闻药品的气味，应用手在瓶口轻轻煽动，仅使少量气味进入鼻孔。不得品尝药品。
　　2，注意节约药品。如果没有说明用量，一般取少量。液体取用1-2ml，固体只需盖满试管底部。
　　3，实验完毕后，剩余药品要做到三不一要，即不放回原瓶，不随意丢弃，不拿出实验室。一要，要放入指定容器内。
　　4，固体药品的取用。块状用镊子，粉末用药匙（或纸槽）。取固体应做到“一横二送三慢竖”以免打破试管底。用粉末时应做到“一斜二送三直立”
　　5，液体药品的取用。1，应把瓶塞拿下，倒放在实验台上防止污染溶液。2，倾倒时标签应向着手心，以免腐蚀标签。3，瓶口紧挨试管口。取少量时，应用胶头滴管滴加，滴加时要保持垂直悬空滴加，不能伸入瓶内或试管内，防止污染试剂。取一定量时，常用量筒量出体积，量筒必须放平，读数时，事先要与量筒内凹液面处保持水平。