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SB-224289 hydrochloride  ≥95%

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包装规格：10mg in glass bottle
溶解性：溶于DMSO（14.29 mg/mL 超声）
产品描述：基本信息 产品编号： S10802 产品名称： SB-224289 hydrochloride CAS: 180084-26-8   储存条件 粉末 -20℃ 四年     分子式： C32H33ClN4O3 溶于液体 -80℃ 6个月 分子量 557.08 -20℃ 1个月 化学名：  [4-[2-methyl-4-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl]phenyl]-(1'-methylspiro[6,7-dihydro-2H-furo[2,3-f]indole-3,4'-piperidine]-5-yl)methanone;hydrochloride Solubility (25°C)：   体外:   DMSO 14.29 mg/mL (25.65mM; Need ultrasonic) Ethanol   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: ≥ 1.43 mg/mL (2.57mM); Clear solution 此⽅案可获得 ≥ 1.43 mg/mL (2.57mM，饱和度未知) 的澄清溶液。 以 1mL ⼯作液为例，取 100μL 14.299999 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: ≥ 1.43 mg/mL (2.57mM); Clear solution 此⽅案可获得 ≥ 1.43 mg/mL (2.57mM，饱和度未知) 的澄清溶液。以 1mL ⼯作液为例，取 100μL 14.299999 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: ≥ 1.43 mg/mL (2.57mM); Clear solution 此⽅案可获得 ≥ 1.43 mg/mL (2.57mM，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 14.299999 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 1.7951mL 8.9754mL 17.9507mL 5mM 0.3590mL 1.7951mL 3.5901mL 10mM 0.1795mL 0.8975mL 1.7951mL   生物活性 产品描述 一种选择性的 5-HT1B receptor 拮抗剂，具有抗焦虑作用。 靶点 5-HT1B Receptor   体外研究 SB-224289 has specific toxin-blocking ability and does not inhibit Cho1p. SB-224289 (100 μM-25μM) shows consistent efficacy at producing Pap-A resistance. SB-224289 does not directly inhibit the PS synthase enzyme in this in vitro assay. Moreover, SB-224289 specifically blocks the activity of papuamides and not other membrane disruptors. SB-224289 is unable to protect wild-type cells against KF, but it is able to provide protection against TPap-A. SB-224289 has a pKi of 8 at human cloned 5-HT1B receptors and displays more than 80 fold selectivity over the closely related 5-HT1D receptor and a range of other receptors. SB-224289 is a potent antagonist with pEC50 of 7.9±0.1. SB-224289 evokes a parallel rightward shift in the 5-HT concentration response curve with pA2 of 8.4±0.2. SB-224289 (100nM and 1μM) also significantly increases [3H]- 5HT release in electrically stimulated guinea-pig brain cortex slices 体内研究 SB-224289 (SB 224289) alone or in combination with cocaine, increases anxiety-like behavior. SB 224289 significantly reduces the amount of locomotor activity in the cocaine-treated rats. SB 224289-treated animals spend a significantly longer time in the corners than those treated with vehicle. SB 224289 is a potent antagonist with an ED50 of 3.6 mg/kg, p.o in SK&F-99101-induced hypothermia in the guinea-pig. SB 224289 (4 mg/kg, p.o) reverses sumatriptan-induced inhibition of 5- HT release showing that it is also a potent terminal 5-HT autoreceptor antagonist in vivo. SB 224289 (2-16 mg/kg, p.o) does not increase 5-HT levels in the fuinea-pig frontal cortex. However, SB 224289 (4 mg/kg, p.o) causes a significantly increase in levels of 5-HT in the fuinea-pig dentate gyrus.   推荐实验方法(仅供参考) Animal Administration Ninety minutes before each animal is tested, it receives an ip injection of either 5 mg/kg SB 224289 in a vehicle of 10% Trappsol in sterile water or vehicle alone (total volume 1mL/kg). This dosage of this drug is effective as a pharmacological agent. The rat is put back in its home cage until just before it is to be tested.
保存条件：-20℃ 充氮保存

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