Caffeine
(Synonyms: 咖啡因,Methyltheobromine, NSC 5036) 目录号 : GN10350一种甲基黄嘌呤生物碱。
Cas No.:58-08-2
Sample solution is provided at 25 µL, 10mM.
Caffeine is a methylxanthine alkaloid naturally found in various plant parts that acts as an antagonist at central adenosine receptors at relevant physiological concentrations (IC50 = ~30 μM).[1],2 It alters fatigue, mood, alertness, motor reaction time, vascular hemodynamics, and pain sensation.[2],[3],[4] Caffeine has also been implicated in carcinogenesis, although the concentrations used to affect cell cycling and apoptosis in the laboratory may not be commonly achieved in vivo.[5]
咖啡因是一种甲基黄嘌呤生物碱，自然存在于各种植物部位中，在相关的生理浓度下（IC50 = ~30 μM）作为中枢腺苷受体的拮抗剂。它改变疲劳、情绪、警觉性、运动反应时间、血管血流动力学和疼痛感觉。咖啡因也被认为与癌症发生有关，尽管实验室用于影响细胞周期和凋亡的浓度可能在体内不常见。
Reference:
[1]. Snyder, S.H., Katims, J.J., Annau, Z., et al. Adenosine receptors and behavioral actions of methylxanthines. Proc. Natl. Acad. Sci. USA 78(5), 3260-3264 (1981).
[2]. Fredholm, B.B., Bättig, K., Holmén, J., et al. Actions of caffeine in the brain with special reference to factors that contribute to its widespread use. Pharmacological Reviews 51(1), 83-133 (1999).
[3]. Carrillo, J.A., and Benitez, J. Clinically significant pharmacokinetic interactions between dietary caffeine and medications. Clinical Pharmacokinetics 39(2), 127-153 (2000).
[4]. Pelligrino, D.A., Xu, H.L., and Vetri, F. Caffeine and the control of cerebral hemodynamics. J.Alzheimers Dis. 20, S51-S62 (2010).
[5]. Bode, A.M., and Dong, Z. The enigmatic effects of caffeine in cell cycle and cancer. Cancer Letters 247(1), 26-39 (2007).
| Cell experiment [1]: | |
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Cell lines |
Patient-derived AC-UPS01 and AC-RMS01 cell lines |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
0.25, 0.5, 1, 2.5 and 5 mM; 72 h |
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Applications |
Caffeine significantly inhibited the patient-derived UPS and RMS cell lines in a dose-dependent manner with IC50 values of 2.02 ± 0.22 mM and 2.37 ± 0.48 mM, respectively. Addition of 0.3 mM or 0.6 mM VPA to varying concentrations of CAF enhanced efficacy against both the AC-UPS01 and AC-RMS01 cell lines. |
| Animal experiment [2]: | |
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Animal models |
diet-induced obesity (DIO) mice |
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Dosage form |
10 μg per mouse, i.c.v. administration |
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Application |
In diet-induced obesity (DIO) mice, administration of caffeine into mouse brain significantly increased the numbers of c-Fos+ cells in the PVN, Arc and DMH nuclei, suggesting that caffeine stimulated the activities of neurons in the hypothalamic nuclei involved in energy balance control. Caffeine reduced the adipocyte sizes of epididymal white adipose tissue, plasma triglycerides (TG) levels and improved glucose tolerance. Mice gained significantly less body weights than the controls on day 7. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Igarashi K1,2,3, Kawaguchi K1,2, Kiyuna T1,2, et al. Efficacy In Vitro of Caffeine and Valproic Acid on Patient-Derived Undifferentiated Pleomorphic Sarcoma and Rhabdomyosarcoma Cell Lines. Anticancer Res. 2017 Aug;37(8):4081-4084. [2] Wu L1, Meng J1, Shen Q1, et al. Caffeine inhibits hypothalamic A1R to excite oxytocin neuron and ameliorate dietary obesity in mice. Nat Commun. 2017 Jun 27;8:15904. |
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| Cas No. | 58-08-2 | SDF | |
| 别名 | 咖啡因,Methyltheobromine, NSC 5036 | ||
| 化学名 | 1,3,7-trimethylpurine-2,6-dione | ||
| Canonical SMILES | CN1C=NC2=C1C(=O)N(C(=O)N2C)C | ||
| 分子式 | C8H10N4O2 | 分子量 | 194.19 |
| 溶解度 | 0.2mg/mL in ethanol, 3mg/mL in DMSO, 10mg/mL in DMF; 33.3mg/ml in Water(Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 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。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 5.1496 mL | 25.748 mL | 51.496 mL |
| 5 mM | 1.0299 mL | 5.1496 mL | 10.2992 mL |
| 10 mM | 0.515 mL | 2.5748 mL | 5.1496 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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，
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 saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet