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| 靶点 |
lipid regulating agent
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| 体外研究 (In Vitro) |
β-谷甾醇是最丰富的膳食植物甾醇之一。根据一项研究，β-谷甾醇能够预防白血病、卵巢癌、乳腺癌、前列腺癌、结肠癌、肺癌、胃癌和结肠癌。
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| 体内研究 (In Vivo) |
与哮喘对照组相比，给予L-BS或β-谷甾醇（BS）（1 mg/kg；i.p.）后，支气管肺泡灌洗液（BAL）中的总细胞和嗜酸性粒细胞显著减少（p<0.05），ROS的产生也减少。通过组织化学方法检测组织病理学特征，包括H&E和阿尔西安蓝和P.A.S染色。L-BS和β-谷甾醇（BS）均通过嗜酸性粒细胞浸润和杯状增生引起的粘液高分泌减轻炎症。L-BS的这些作用优于BS。L-BS和BS分别抑制肺组织和BAL液中IL-4和IL-5的mRNA和蛋白表达增加。ELISA法测定BAL液和血清中的IgE浓度，L-BS对BAL液中卵清蛋白特异性IgE有独特的抑制作用（p<0.05）。从正常和哮喘小鼠中分离脾细胞，并分别在不存在和存在100微克/毫升卵清蛋白的情况下孵育。L-BS阻断小鼠脾细胞的存活率（p<0.01）。这一发现表明L-BS和BS有可能成为哮喘的潜在治疗分子，并可能有助于改善目前的治疗药物。[2]
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| 细胞实验 |
小鼠脾细胞的存活率[2]
我们使用MTT测定试剂盒和annexinV异硫氰酸荧光素（FITC）凋亡检测试剂盒（Beckton Dickinson，San Jose，CA）进行MTT测定和凋亡测定以确定细胞活力。通过注射器泵送从正常和哮喘对照小鼠的脾脏中分离脾细胞。用补充有抗生素-抗真菌剂的10ml DMEM（Life Technologies，NY）洗涤三次后，将脾细胞与3ml RBC裂解缓冲液（Sigma，MI）在室温下孵育10分钟，然后用10ml洗涤介质洗涤两次。将在100μl含有10%FBS的DMEM培养基中的2×105个脾细胞接种到96孔培养板上。在不存在或存在100μg/ml卵清蛋白的情况下，将L-BS、BS或地塞米松（1μg/ml）添加到单个孔中，然后将平板在37°C的CO2培养箱中培养48小时。在每个孔中加入10μl MTT溶液后，将平板在37°C下在CO2培养箱中培养4小时，并向每个孔中添加100μl增溶溶液用于MTT测定。孵育24小时后，通过使用ELISA读取器（Bio-Tek Instruments，VT）在550nm处测量吸光度。对于凋亡测定，收获细胞并将其重悬于结合缓冲液中。加入膜联蛋白V-FITC和PI，并在室温下孵育15分钟。使用CellQuest软件通过FACSort细胞荧光计对细胞进行分析。针对膜联蛋白V和PI染色的阴性细胞被认为是活细胞或非凋亡细胞。 |
| 动物实验 |
Induction of asthma in mice[2]
Six to eight-week-old female BALB/c mice were obtained from Daehan Biolink Co. LTD. They were maintained in an air-conditioned room. The room temperature (about 22 ± 1 °C) and humidity (about 55 ± 10%) were automatically controlled. The mice were divided into five groups (n = 5), and airway inflammation was induced in four groups. Each mouse was immunized through intraperitoneal (i.p.) injection with 20 μg of chicken OVA and 1 mg of aluminum hydroxide on days 1 and 14, as shown in Fig. 2. The mice were exposed to a 5% ovalbumin solution aerosolized using an ultrasonic nebulizer for 1 h per day from days 21 to 27 after the second sensitization. The mice were placed in a Plexiglass chamber (30 × 30 × 15 cm3) that contained small ventilation holes on one side during the inhalation challenge. The aerosol was generated with a nebulization rate of 1 ml/min. Three groups of asthma-induced mice were treated through i.p. injection with 1 mg/kg of L-BS, BS or dexamethasone between days 14 and 27. Both L-BS and BS dissolved in DMSO diluted less than 1/100 by phosphate-buffered saline (PBS). The negative control group was sensitized and challenged with PBS without drug administration. |
| 参考文献 |
| 分子式 |
C29H50O
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|---|---|---|
| 分子量 |
414.71
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| 精确质量 |
414.3862
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| 元素分析 |
C, 83.99; H, 12.15; O, 3.86
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| CAS号 |
83-46-5
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| 相关CAS号 |
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| 外观&性状 |
White to off-white solid powder
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| LogP |
9.3
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| tPSA |
20.2Ų
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| SMILES |
CC[C@H](CC[C@@H](C)[C@H]1CC[C@@H]2[C@@]1(CC[C@H]3[C@H]2CC=C4[C@@]3(CC[C@@H](C4)O)C)C)C(C)C
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| InChi Key |
KZJWDPNRJALLNS-VJSFXXLFSA-N
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| InChi Code |
InChI=1S/C29H50O/c1-7-21(19(2)3)9-8-20(4)25-12-13-26-24-11-10-22-18-23(30)14-16-28(22,5)27(24)15-17-29(25,26)6/h10,19-21,23-27,30H,7-9,11-18H2,1-6H3/t20-,21-,23+,24+,25-,26+,27+,28+,29-/m1/s1
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| 化学名 |
(3S,8S,9S,10R,13R,14S,17R)-17-[(2R,5R)-5-ethyl-6-methylheptan-2-yl]-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol
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| 别名 |
(-)-beta-Sitosterol; 22,23-Dihydrostigmasterol; 24-alpha-Ethylcholesterol; AI3-26020; alpha-Dihydrofucosterol; Rhamnol; Angelicin; beta-Sitosterol; CCRIS 5529; Azuprostat; Cinchol; Cupreol; Harzol; Nimbosterol; Prostasal; Quebrachol; Triastonal
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| HS Tariff Code |
2934.99.03.00
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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) |
Solubility in Formulation 1: 20 mg/mL (48.23 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: Solubility in Formulation 1: ≥ 1 mg/mL (2.4 mM) (saturation unknown) in 10% EtOH + + 40% PEG300 + 5% Tween80 + + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution. For example, if 1 mL of working solution is to be prepared, you can take 100 μL of 25 mg/mL EtOH + stock solution and add to 400 μL of PEG300, mix well; Then add 50 μL of Tween 80 to the above solution, mix well; Finally, add 450 μL of saline to the above solution, mix well. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1 mg/mL (2.4 mM) (saturation unknown) in 10% EtOH + + 90% (20% SBE-β-CD in saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution. For example, if 1 mL of working solution is to be prepared, you can take 100 μL of 25 mg/mL EtOH + stock solution and add to 900 μL of 20% SBE-β-CD in saline, mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 1 mg/mL (2.4 mM) (saturation unknown) in 10% EtOH + + 90% Corn oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can take 100 μL of 25 mg/mL EtOH + stock solution and add to 900 μL of corn oil, mix well (clear solution). Solubility in Formulation 4: ~5 mg/mL (12.1 mM) in 15% Cremophor EL + + 85% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution. Solubility in Formulation 5: ~10 mg/mL (24.1 mM) in Corn Oil , clear solution. 请根据您的实验动物和给药方式选择适当的溶解配方/方案： 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 | 2.4113 mL | 12.0566 mL | 24.1132 mL | |
| 5 mM | 0.4823 mL | 2.4113 mL | 4.8226 mL | |
| 10 mM | 0.2411 mL | 1.2057 mL | 2.4113 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) 。
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01736865 | Completed | Drug: Placebo Drug: Cholecalciferol |
Type 2 Diabetes | Tufts Medical Center | December 2012 | Phase 2 Phase 3 |
Ara-SH
NTR 368 TFA
ERK-IN-6
Difopein TFA
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