规格 | 价格 | 库存 | 数量 |
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体外研究 (In Vitro) |
L-赖氨酸(布洛芬)(24 小时)抑制 COX-1 和 COX-2 的活性,IC50 值分别为 13 μM 和 370 μM[1]。布洛芬(500 μM,48 小时)L-赖氨酸会导致 AGS 细胞(胃腺癌细胞系)凋亡,并抑制血管生成和细胞增殖[2]。在 AGS 细胞中,布洛芬(500 μM,48 小时)L-赖氨酸上调野生型 P53 和 Bax 基因 RNA 水平,同时下调 Akt、VEGF-A、PCNA、Bcl2、OCT3/4 和 CD44 基因的转录[2]。在原代 CF 鼻上皮细胞和囊性纤维化 (CF) 细胞模型中,布洛芬(500 μM,24 小时)L-赖氨酸刺激微管向细胞外周伸长,并恢复微管依赖性细胞内胆固醇转运[3]。通过光敏作用,布洛芬(500 μM,24 小时)L-赖氨酸可放大 MCF-7 和 MDA-MB-231 细胞中紫外线诱导的细胞死亡[4]。
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体内研究 (In Vivo) |
在产后乳腺癌模型中,布洛芬(300 mg/kg;口服;每天,持续 14 天)和 L-赖氨酸可减少肿瘤的整体发展并改善抗肿瘤免疫特征,而不会引起阴性自身免疫反应[5]。在慢性奥沙利铂诱导的周围神经病变的大鼠模型中,L-赖氨酸可降低神经病变的发生率,布洛芬也有同样的作用(60 mg/kg;ih;每隔一天,持续 15 天)[6]。与布洛芬(20 mg/kg;口服;每 12 小时一次,总共 5 剂)联合使用时,L-赖氨酸可减少肌肉生长(平均肌纤维横截面积),而不改变冈上肌腱对运动的适应控制[7]。在慢性肺部感染的大鼠模型中,布洛芬(35 mg/kg;口服;每天两次)和 L-赖氨酸可减轻对铜绿假单胞菌的炎症反应[8]。
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细胞实验 |
细胞活力测定[2]
细胞类型: AGS 细胞 测试浓度: 100-1000 μM 孵育时间: > 24 小时、48 小时 实验结果: 抑制 AGS 细胞活力,IC50 值为 630 μM(台盼蓝染色,24 小时)、456 μM(中性红测定,24 小时)、549 μM(台盼蓝染色,48 小时)和 408 μM(中性红测定,48 小时)。 |
动物实验 |
Animal/Disease Models: Syngeneic (D2A1) orthotopic Balb/c mouse model of PPBC (postpartum)[5]
Doses: 300 mg/kg, daily for 14 days Route of Administration: Fed in animal feedings (added to pulverized standard chow and mixed dry, then mixed with water, made into chow pellets and dried thoroughly) Experimental Results: Suppresed tumor growth, decreased presence of immature monocytes and increased numbers of T cells. Enhanced Th1 associated cytokines as well as promoted tumor border accumulation of T cells. Animal/Disease Models: Oxaliplatin‑induced peripheral neuropathy[6] Doses: 60 mg/kg, every second day for 15 days Route of Administration: subcutaneous (sc) injection Experimental Results: Lowered sensory nerve conduction velocity (SNCV). |
参考文献 |
[1]. Noreen Y, et al. Development of a radiochemical cyclooxygenase-1 and -2 in vitro assay for identification of natural products as inhibitors of prostaglandin biosynthesis. J Nat Prod. 1998 Jan;61(1):2-7.
[2]. Hassan Akrami, et al. Inhibitory effect of ibuprofen on tumor survival and angiogenesis in gastric cancer cell. Tumour Biol. 2015 May;36(5):3237-43. [3]. Sharon M Rymut, et al. Ibuprofen regulation of microtubule dynamics in cystic fibrosis epithelial cells. Am J Physiol Lung Cell Mol Physiol. 2016 Aug 1;311(2):L317-27. [4]. Emmanuelle Bignon, et al. Ibuprofen and ketoprofen potentiate UVA-induced cell death by a photosensitization process. Sci Rep. 2017 Aug 21;7(1):8885. [5]. Nathan D Pennock, et al. Ibuprofen supports macrophage differentiation, T cell recruitment, and tumor suppression in a model of postpartum breast cancer. J Immunother Cancer. 2018 Oct 1;6(1):98. [6]. Thomas Krøigård, et al. Protective effect of ibuprofen in a rat model of chronic oxaliplatin-induced peripheral neuropathy. Exp Brain Res. 2019 Oct;237(10):2645-2651. [7]. Sarah Ilkhanipour Rooney, et al. Ibuprofen Differentially Affects Supraspinatus Muscle and Tendon Adaptations to Exercise in a Rat Model. Am J Sports Med. 2016 Sep;44(9):2237-45. [8]. M W Konstan, et al. Ibuprofen attenuates the inflammatory response to Pseudomonas aeruginosa in a rat model of chronic pulmonary infection. Implications for antiinflammatory therapy in cystic fibrosis. Am Rev Respir Dis. 1990 Jan;141(1):186-92. |
分子式 |
C19H32N2O4
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分子量 |
352.47
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CAS号 |
57469-77-9
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相关CAS号 |
Ibuprofen;15687-27-1
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SMILES |
CC(CC1=CC=C(C(C(O)=O)C)C=C1)C.N[C@@H](CCCCN)C(O)=O
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InChi Key |
IHHXIUAEPKVVII-ZSCHJXSPSA-N
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InChi Code |
1S/C13H18O2.C6H14N2O2/c1-9(2)8-11-4-6-12(7-5-11)10(3)13(14)15;7-4-2-1-3-5(8)6(9)10/h4-7,9-10H,8H2,1-3H3,(H,14,15);5H,1-4,7-8H2,(H,9,10)/t;5-/m.0/s1
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化学名 |
L-Lysine mono(4-isobutyl-alpha-methylbenzeneacetate)
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别名 |
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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) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 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 | 2.8371 mL | 14.1856 mL | 28.3712 mL | |
5 mM | 0.5674 mL | 2.8371 mL | 5.6742 mL | |
10 mM | 0.2837 mL | 1.4186 mL | 2.8371 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) 。