马来酸替加色罗  ≥98%

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包装规格:50mg in glass bottle
溶解性:溶于水(1mg/mL 超声),溶于DMSO(≥35mg/mL)
产品描述:基本信息 产品编号: T10813 产品名称: Tegaserod maleate CAS: 189188-57-6   储存条件 粉末 -20℃ 四年     分子式: C16H23N5O.C4H4O4 溶于液体 -80℃ 两年 分子量 417.46 -20℃ 1个月 化学名:  (Z)-but-2-enedioic acid;1-[(E)-(5-methoxy-1H-indol-3-yl)methylideneamino]-2-pentylguanidine Solubility (25°C):   体外:   DMSO 83 mg/mL (198.82mM) Ethanol 8 mg/mL (19.16mM) Water Insoluble 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 (5.99mM); Clear solution 此⽅案可获得 ≥ 2.5 mg/mL (5.99mM,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% corn oil Solubility: ≥ 2.5 mg/mL (5.99mM); Clear solution 此⽅案可获得 ≥ 2.5 mg/mL (5.99mM,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 2.3954mL 11.9772mL 23.9544mL 5mM 0.4791mL 2.3954mL 4.7909mL 10mM 0.2395mL 1.1977mL 2.3954mL 50mM 0.0479mL 0.2395mL 0.4791mL   生物活性 产品描述 一种选择性的、5-HT4 受体的部分激动剂和 5-HT2B 受体的拮抗剂。Tegaserod maleate 在胃肠道中表现出促进的作用。 靶点 5-HT4 Receptor (Agonist) 5-HT2B Receptor (Antagonist) 体外研究 Tegaserod was metabolized in human liver microsomes to O-desmethyl tegaserod at a low rate. Tegaserod had significant binding affinity for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors (pKi=7.5, 8.4 and 7.0, respectively). Tegaserod (0.1-3μM) inhibits 5-HT-mediated contraction of the rat isolated stomach fundus potently (pA2=8.3), consistent with 5-HT2B receptor antagonist activity. 体内研究 Tegaserod increases the amplitude of excitatory postsynaptic currents mediated by nicotinic acetylcholine receptors which may contribute to the prokinetic effects by facilitating excitatory neurotransmission in mice. Tegaserod (0.1 mg/kg) significantly accelerates the gastric emptying rate of glucose in db/db mice, reducing the fraction of the meal remaining in the stomach at 30 min by 80%. Tegaserod (5, 10, 50, 100μg/mL) promotes hindlimb motor function at 6 weeks after spinal cord injury compared to the control group receiving vehicle only. Animal Model: Female C57BLKS/J db/db mice. Dosage: 0.1, 0.5, 1.0, 2.0 mg/kg. Administration: IP 15 min prior to gastric loading. Result: Produced a dramatic decrease in the fraction of the meal remaining in the stomach for doses as low as 0.1 mg/kg (0.1 mg/kg). Accelerated gastric emptying, with a reduction of nearly 80% in the fraction remaining at 30 min (P < 0.0001) (0.1 mg/kg). Induced a significant decrease in the gastric emptying rate as the amount of the meal remaining at 30 min was significantly greater (2.0 mg/kg). Resulted in inhibition of tegaserod-induced increased gastric emptying (0.1 mg/kg).   Animal Model: Three- to four-month-old female C57BL/6J mice. Dosage: 5, 10, 50, 100μg/mL. Administration: Alzet pumps into non-injured spinal cords. Result: Showed a less intense astrogliosis within and in the vicinity of the compression lesion site when compared to vehicle-only-treated mice. Showed a smaller lesion area when compared to vehicle-onlytreated mice.Showed a higher staining intensity of 5-HT-immunoreactive axons 1 mm rostral, but not caudal to the lesion center as determined in cross-sections and quantification by ImageJ analysis.
保存条件:-20℃