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酒石酸酮色啉盐  ≥98%

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包装规格：250mg 1g 5g in glass bottle
溶解性：溶于水（6 mg/mL 超声），溶于DMSO（150 mg/mL 超声）
产品描述：基本信息 产品编号： K10102  产品名称： Ketanserin tartrate CAS: 83846-83-7   储存条件 粉末 2-8℃ 四年     分子式： C22H22FN3O3.C4H6O6 溶于液体 -80℃ 两年 分子量 545.51 -20℃ 1个月 化学名：  2,3-dihydroxybutanedioic acid;3-[2-[4-(4-fluorobenzoyl)piperidin-1-yl]ethyl]-1H-quinazoline-2,4-dione Solubility (25°C)：   体外:   DMSO 150 mg/mL (274.97mM; Need ultrasonic) Ethanol   Water 6 mg/mL (11.00mM; Need ultrasonic) 体内(现配现用):   1.请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility: ≥ 2.5 mg/mL (4.58mM); Clear solution 此⽅案可获得 ≥ 2.5 mg/mL (4.58mM，饱和度未知) 的澄清溶液。 以 1mL ⼯作液为例，取 100μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400μL PEG300 中，混合均匀；向上述体系中加⼊ 50μL Tween-80，混合均匀；然后继续加⼊ 450μL ⽣理盐⽔定容⾄ 1mL。 2.请依序添加每种溶剂：10% DMSO→90% (20% SBE-β-CD in saline) Solubility: ≥ 2.5 mg/mL (4.58mM); Clear solution 此⽅案可获得 ≥ 2.5 mg/mL (4.58mM，饱和度未知) 的澄清溶液。 以 1mL ⼯作液为例，取 100μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900μL 20% 的 SBE-β-CD ⽣理盐⽔⽔溶液中，混合均 匀。 3.请依序添加每种溶剂： 10% DMSO→90% corn oil Solubility: ≥ 2.5 mg/mL (4.58mM); Clear solution 此⽅案可获得 ≥ 2.5 mg/mL (4.58mM，饱和度未知) 的澄清溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。 以 1mL ⼯作液为例，取 100μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900μL ⽟⽶油中，混合均匀。 ＜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 1.8331mL 9.1657mL 18.3315mL 5mM 0.3666mL 1.8331mL 3.6663mL 10mM 0.1833mL 0.9166mL 1.8331mL   生物活性 产品描述 一种选择性的 5-HT2 receptor 拮抗剂。Ketanserin tartrate 也抑制 hERG 电流 (IhERG)，IC50 为 0.11μM，这种作用具有浓度依赖性。 靶点 5-HT2 Receptor hERG current 0.11μM (IC50) 体外研究 Ketanserin at 0.3μM inhibits the voltage-dependent step current (IhERG.step) and tail current (IhERG.tail) of hERG channels with a 5-min exposure. The synergistic effect observed for AA with 5-HT is, also, blocked by the 5-HT receptor blockers cyproheptadine (IC50=22.0±7μM), Ketanserin (IC50=152±23μM). Ketanserin (50-350μM) inhibits the synergism by blocking the receptor in a dose-dependent manner. The IC50 value of Cyproheptadine is 22±7μM and Ketanserin is 152±23μM. Ketanserin inhibits platelet aggregation with an IC50 of 240 (169-339）nM. 体内研究 Ketanserin is a 5-HT2A receptor antagonist. Ketanserin significantly reduces BDNF protein levels in numerous brain regions (CA1 and CA3 of the hippocampus, prefrontal cortex, central amygdaloid nucleus, dorsomedial hypothalamic nucleus, dentate gyrus, shell of the nucleus accumbens and midbrain periaqueductal gray). 5-HT2A antagonist Ketanserin can significantly reduce BDNF mRNA levels in various brain regions.   推荐实验方法(仅供参考) Cell Assay The established HEK 293 cell line stably expressing hERG channels is cultured in Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% foetal bovine serum, 400μg/mL G418. The HEK 293 cell line stably expressing recombinant human cardiac KCNQ1/KCNE1 channel current (IKs) is maintained in DMEM containing 10% foetal bovine serum and 100μg/mL hygromycin. Cells used for electrophysiology are seeded on a glass coverslip. The mutant hERG channels are constructed, and are transiently expressed in HEK 293 cells using 10μL of Lipofectamine 2000 with 4μg of hERG mutant cDNA in pCDNA3 vector   Animal Administration RatA total of 155 specific-pathogen-free 2-month-old male Sprague-Dawley rats, weighing 180-220 g, are used. The rats are randomly divided into the following six groups: 5-HT1A receptor agonist (8-OH-DPAT) PS group (DPAT-PS group, n=30); 5-HT1A receptor antagonist (MDL73005) PS group (MDL-PS group, n=30); 5-HT2A receptor agonist (DOI) PS group (DOI-PS group, n=30); 5-HT2A receptor antagonist (Ketanserin) PS group (Ketan-PS group, n=30); the solvent control no-stress group (0.9% physiological saline group, CON group); and the PS only group (PS group, n=30). The DPAT-PS, MDL-PS, DOI-PS, Ketan-PS and PS groups are further divided into six subgroups (n=5 each) according to the time between the stress and analysis; immediately after stress, and 0.5, 1, 2, 6 and 24 hours after stress. The CON group (n=5) receive normal feed. For the Ketan-PS group, Ketanserin, dissolved in 0.9% physiological saline, is injected intraperitoneally at 5 mg/kg at 1 hour before each stress exposure.
保存条件：2-8℃

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