规格 | 价格 | 库存 | 数量 |
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250mg |
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500mg |
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1g |
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2g |
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5g |
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10g |
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Other Sizes |
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靶点 |
Histamine H1 receptor
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体外研究 (In Vitro) |
Osthole (p<0.0001) 和 Fexofenadine (p<0.001) 抑制研究组中组胺诱导的 HRH-1 mRNA 表达增加。在用组胺/蛇床子素培养的细胞中也观察到了这个结果;其中与组胺相比,组合物质降低了 HRH-1 mRNA 表达 (p<0.0001)[1]。当蛇床子素以高达 100 μM 的剂量使用时,细胞活力评估未检测到明显的毒性。然而,当剂量达到 500 μM 时,基于这些观察,Osthole用于所有体外研究,剂量范围为10 至 100 μM。Osthole剂量依赖性地促进形成骨细胞湿度,如I型胶原(col1)、骨唾液蛋白(BSP) ) 和骨钙素 (OC) (培养2天)。Osthole以剂量依赖的方式促进小鼠原代成骨细胞的ALP活性[2]。
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体内研究 (In Vivo) |
将蛇床子素以每天 5 mg/kg 的剂量皮下注射到小鼠颅骨上可显着着刺激局部骨形成(对最后一次注射后 2 周采集的颅骨组织样本进行组织学分析,并用 H&E 橙色 G 染色)。形态学分析显示蛇床子素对骨形成有显着影响,与前期对比微管抑制TN-16同样有效。然而,当以每天1 mg/kg的剂量使用蛇床子素时,看不到这样的效果。腹膜内注射蛇床子素8周可显着逆转去势支架的骨质流失。用三硝基苯酚一品红染色的L4样本的组织学检查表明,用蛇床子素处理的去势支架的小梁结构部分恢复。形态学分析表明,Osthole 处理可显着增加总 BMD、骨小梁体积和骨小梁厚度,并减少骨小梁分离[2]。
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细胞实验 |
在第一个研究日,参与者的外周血样本在上午 7 点至 9 点之间抽取,并转移至含有 K3EDTA 的分组管中。然后他们制作新鲜的 PBMC。将 1% 热灭活人 AB 血清、1% 庆大霉素和 0.25% PHA 的溶液添加到分离的细胞中,以每孔 1×106 的密度接种到 24 孔板中使用 RPMI-1640。在添加活性试剂之前,每孔有 24 小时的时间,并用纯培养基作为物质的对照。再过三天,收获细胞[1]。
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动物实验 |
Mice: Four-week-old ICR Swiss mice receive subcutaneous injections over the calvarial surface twice a day for five days straight, either with or without Osthole treatment. The doses are 1 and 5 mg/kg per day, with three mice per group. As a positive control, microtubule inhibitor TN-16 (5 mg/kg per day, subcutaneous injection, twice daily for 2 days; 3 mice per group) is used. Three weeks after the start of treatment, all the mice are put to sleep, and the calvariae are removed, preserved for two days in 10% phosphate-buffered formalin, decalcified for two weeks in 10% EDTA, and then embedded in paraffin. Hematoxylin and eosine orange G are used to cut and stain histologic sections. Using the OsteoMeasure System for histomorphometry, the amount of new bone over the calvarial surface is measured. In order to quantify the mineral appositional rate (MAR) and bone-formation rate (BFR), mice undergo intraperitoneal injections of 20 mg/kg of double calcein at days 7 and 14, following which they are put to death 7 days later. Plastic sections of the labeling are inspected. The calvarial samples that have been dissected are embedded in methyl methacrylate after being fixed in 75% ethanol. A fluorescent microscope is used to examine unstained transverse sections that have a thickness of 3 µm. With the OsteoMeasure System, MAR and BFR are measured.
Rats: The rats are thirty six-month-old female Sprague-Dawley rats. The rats are randomly assigned by body weight into three groups for the surgery (n=10): group 1 is a sham surgery followed by PBS vehicle treatment (sham+VEH); group 2 is an ovariectomy followed by vehicle treatment (OVX+VEH); and group 3 is an ovariectomy followed by Osthole treatment (OVX+OST). The rats are given an intraperitoneal nembutal injection (30 mg/kg) to induce anesthesia. The eight-week course of treatment is administered beginning one month following surgery. For eight weeks, either vehicle or Osthole (100 mg/kg daily) is taken orally once daily. Dual-energy X-ray absorptiometry is used to measure the total bone mineral density (BMD, g/m2) of the rats prior to their euthanasia at the end of the experiments. Then, the left femoral shafts are utilized for biomechanical testing, and the fourth lumbar vertebrae (L4) are dissected for histomorphometric and micro-computed tomographic (µCT) analysis. |
参考文献 |
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分子式 |
C15H16O3
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分子量 |
244.29
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精确质量 |
244.11
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元素分析 |
C, 73.75; H, 6.60; O, 19.65
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CAS号 |
484-12-8
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相关CAS号 |
Osthole-d3
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外观&性状 |
Solid powder
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SMILES |
CC(=CCC1=C(C=CC2=C1OC(=O)C=C2)OC)C
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InChi Key |
MBRLOUHOWLUMFF-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C15H16O3/c1-10(2)4-7-12-13(17-3)8-5-11-6-9-14(16)18-15(11)12/h4-6,8-9H,7H2,1-3H3
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化学名 |
7-methoxy-8-(3-methylbut-2-enyl)chromen-2-one
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别名 |
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HS Tariff Code |
2934.99.9001
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外) |
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溶解度 (体内) |
配方 1 中的溶解度: ≥ 2.5 mg/mL (10.23 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。
例如,若需制备1 mL的工作液,可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中,混匀;然后向上述溶液中加入50 μL Tween-80,混匀;加入450 μL生理盐水定容至1 mL。 *生理盐水的制备:将 0.9 g 氯化钠溶解在 100 mL ddH₂O中,得到澄清溶液。 配方 2 中的溶解度: ≥ 2.5 mg/mL (10.23 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。 例如,若需制备1 mL的工作液,可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中,混匀。 *20% SBE-β-CD 生理盐水溶液的制备(4°C,1 周):将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中,得到澄清溶液。 View More
配方 3 中的溶解度: ≥ 2.5 mg/mL (10.23 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 4.0935 mL | 20.4675 mL | 40.9350 mL | |
5 mM | 0.8187 mL | 4.0935 mL | 8.1870 mL | |
10 mM | 0.4093 mL | 2.0467 mL | 4.0935 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。
Possible interrelation between effect of osthole on intracellular ion channels, cyclic adenosine monophosphate (cAMP), and cyclic guanosine monophosphate (cGMP) levels with some of its pharmacological activities. Evid Based Complement Alternat Med . 2015:2015:919616. td> |
Chemical structure of osthole, the principle component of Cnidium monnieri. Evid Based Complement Alternat Med . 2015:2015:919616. td> |
Effects of osthole on the histological manifestations of TNBS-induced colitis. Acta Pharmacol Sin . 2017 Aug;38(8):1120-1128. td> |
The protective effects of osthole against TNBS-induced colitis were mainly mediated by the cAMP/PKA-independent pathway. Acta Pharmacol Sin . 2017 Aug;38(8):1120-1128. td> |
Osthole stimulates local bone formation in mouse calvaria. J Bone Miner Res . 2010 Jun;25(6):1234-45. td> |
Osthole reverses bone loss induced by ovariectomy in rats. J Bone Miner Res . 2010 Jun;25(6):1234-45. td> |