Melatonin (Synonyms: 褪黑素; N-Acetyl-5-methoxytryptamine)
Melatonin 是一種由松果體分泌的ji素，可ji活褪黑ji素受體。Melatonin 在睡眠中起作用并具有重要的抗氧化和抗炎特性。Melatonin 是一種新型的選擇性 ATF-6 抑制劑，可通過(guò) COX-2 下調(diào)誘導(dǎo)人肝癌細(xì)胞凋亡。Melatonin 通過(guò)內(nèi)質(zhì)網(wǎng)應(yīng)激減弱palmitic acid-induced (HY-N0830)誘導(dǎo)的小鼠顆粒細(xì)胞凋亡。
生物活性
Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties[1][2][3]. Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation[4]. Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress[5].
IC50 & Target
Microbial Metabolite Human Endogenous Metabolite
體內(nèi)研究(In Vivo)
Melatonin increases the levels of activated PTEN, RSK-1, mTOR and AMPKα kinases, mildly inhibits ERK-1/2 phosphorylation and Bad phosphorylation, significantly inhibits phosphorylations of S6 Ribosomal Protein, 4E-BP1, GSK-3α and GSK-3β, and slightly increases PRAS40 phosphorylation in animals[1]. Melatonin ameliorates the neurotoxiciy and astrocyte activation induced by Aβ1-42 in the cerebral cortex. Melatonin also blocks the reduction in Reelin and Dab1 expression induced by Aβ1-42[2]. Melatonin treatment and lack of NLRP3-/- share similar inhibition of NF-κB and NLRP3 signaling pathway in mice. Melatonin treatment and lack of NLRP3-/- share some patterns of clock genes expression, and improve cardiomyocytes morphology in mice[3].
分子量：232.28
Formula：C13H16N2O2
CAS 號(hào)：73-31-4
中文名稱：褪黑素；褪黑激素；美拉酮寧；抑黑素；松果腺素；松果體素
運(yùn)輸條件：Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
溶解性數(shù)據(jù)
DMSO : 100 mg/mL (430.51 mM; Need ultrasonic)
Ethanol : 12.5 mg/mL (53.81 mM; Need ultrasonic)
H2O : 1.1 mg/mL (4.74 mM; Need ultrasonic)
| 濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 4.3051 mL | 21.5257 mL | 43.0515 mL |
| 5 mM | 0.8610 mL | 4.3051 mL | 8.6103 mL |
| 10 mM | 0.4305 mL | 2.1526 mL | 4.3051 mL |
請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。
以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用； 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶
- 1.
請(qǐng)依序添加每種溶劑： 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: ≥ 2.62 mg/mL (11.28 mM); Clear solution
- 2.
請(qǐng)依序添加每種溶劑： 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.62 mg/mL (11.28 mM); Clear solution
- 3.
請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (10.76 mM); Clear solution
- 4.
請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (10.76 mM); Clear solution
- 5.
請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (10.76 mM); Clear solution
- 6.
請(qǐng)依序添加每種溶劑： 10% EtOH 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (10.76 mM); Clear solution
- 7.
請(qǐng)依序添加每種溶劑： 10% EtOH 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (10.76 mM); Clear solution
- 8.
請(qǐng)依序添加每種溶劑： 10% EtOH 90% corn oil
Solubility: ≥ 2.5 mg/mL (10.76 mM); Clear solution
參考文獻(xiàn)
[1]. Kilic U, et al. Particular phosphorylation of PI3K/Akt on Thr308 via PDK-1 and PTEN mediates melatonin's neuroprotective activity after focal cerebral ischemia in mice. Redox Biol. 2017 Apr 5;12:657-665
[2]. Hu C, et al. Neuroprotective effect of melatonin on soluble Aβ1-42-induced cortical neurodegeneration via Reelin-Dab1 signaling pathway. Neurol Res. 2017 Apr 7:1-1
[3]. Rahim I, et al. Melatonin administration to wild-type mice and non-treated NLRP3 mutant mice share similar inhibition of the inflammatory response during sepsis. J Pineal Res. 2017 Mar 31
[4]. Bu LJ, et al. Melatonin, a novel selective ATF-6 inhibitor, induces human hepatoma cell apoptosis through COX-2 downregulation. World J Gastroenterol. 2017 Feb 14;23(6):986-998.
[5]. Zhi Chen, et al. Melatonin attenuates palmitic acid-induced mouse granulosa cells apoptosis via endoplasmic reticulum stress. J Ovarian Res. 2019 May 10;12(1):43
注：產(chǎn)品僅用于科研
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