Meldonium

製品コードS4130 バッチS413003

化学情報

	Synonyms	MET-88, Quaterin	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₆H₁₄N₂O₂
	分子量	147.19	CAS No.	76144-81-5
Solubility (25°C)*	体外	Water	29 mg/mL (197.02 mM)
		Ethanol	29 mg/mL (197.02 mM)
		DMSO	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Meldonium（MET-88、Quaterin）は、ガンマ-ブチロベタイン（GBB）ヒドロキシラーゼによるL-カルニチン生合成の阻害剤であり、腎臓のカルニチン再吸収の競合阻害剤でもあります。
in vitro	Meldonium (40 μM) inhibits the reaction of γ-butyrobetaine hydroxylase with γ-butyrobetaine with K_m and V_max of 36.8 μM and 0.08 nmol/min/mg protein, respectively.
in vivo	Meldonium administered orally to rats for 10 days (150 mg/kg) elicits a reduction in myocardial free camitine and long-chain acyl carnitine content by 63.7 and 74.3%, respectively. This compound treatment (100 mg/kg, orally) subsequent administration of isoproterenol results in a reduction in free camitine concentration by 48.7% in comparison with the rats receiving isoproterenol. A prior administration of this chemical effectively protects the myocardium from isoproterenol-induced variations in the content of ATP and myocardial energy charge, as well as preventing a rise in creatine phosphokinase and lactic dehydrogenase activity. This compound (200 mg/kg) long-term treatment significantly increases the rate of insulin-stimulated glucose uptake by 35% and the expression of glucose transporter 4 (1.7-fold increase), hexokinase II (2.1-fold increase), insulin receptor proteins (2.5-fold increase) and carnitine palmitoyltransferases IA (2.2-fold increase) in mouse hearts. This chemical long-term treatment statistically significantly decreases fed state blood glucose from 6 to 5 mM. It reduces the azidothymidine-induced alterations in mouse brain tissue. This compound (50 mg/kg) normalizes the increase in caspase-3, cellular apoptosis susceptibility protein (CAS) and iNOS expression. It also normalizes the changes in cytochromec oxidase (COX) expression, reduces the expression of glial fibrillary acidic protein (GFAP) and cellular infiltration. This chemical displays protective effects in experimental model of type 2 diabetes in Goto-Kakizaki rats. It (200 mg/kg) treatment decreases both the fed- and fasted-state blood glucose. This compound strongly inhibits fructosamine accumulation and loss of pain sensitivity (by 75%) and also ameliorates the enhanced contractile responsiveness of Goto-Kakizaki rat aortic rings to phenylephrine. In addition, in this chemical-treated hearts, the necrosis zone following coronary occlusion is significantly decreased by 30%.

プロトコル(参考用のみ)

キナーゼアッセイ	γ-Butyrobetaine hydroxylase activity assay
キナーゼアッセイ	γ-Butyrobetaine hydroxylase activity is assessed by the amount of carnitine formed from γ-butyrobetaine. Camitine is assayed radiometrically with the aid of camitine acetyltransferase and ¹⁴C-acetyl-CoA. The ¹⁴C-acetyl carnitine is isolated by ion-exchange chromatography on Dowex 2 × 8 (Cl^--form, 200-400 mesh) following enzymatic reactions. The incubation mixture (final volume 125 μL) consists of γ-butyrobetaine (75 μL, 6.65-26.6 μM), Meldonium solution (10 μL, 50-500 μM), 20 μL of ascorbate and α-ketoglutarate mixture (500 μL 37.5 mM sodium ascorbate, 375 μL 25 mM αketoglutarate, 125 μL 1 M potassium phosphate buffer, pH 6.7), 10 μL of γ-butyrobetaine hydroxylase and catalase mixture (150 μL of isolated γ-butyrobetaine hydroxylase solution, -77 mU, 50μL catalase solution -2 mg, 50 μL 100 mM potassium phosphate buffer, pH 6.7, 250 μL H₂O), ferrous ammonium sulphate (10μL, 6.25 mM). Following incubation for 30 min at 30 ℃ the samples are supplemented with 25 μL 1.6 M KOH and kept for 20 min at 56 ℃. Then, 35 μL of the neutralising solution are added (1 mL 1 M HEPES acid, 400μL 0.5 M glutathione, 10 μL 100 mM EDTA, 250 μL 2 M H_{3/sub>PO₄, water to 1.75 mL). Following neutralisation the sample should have pH 7.6. After adding 10 μL of l-¹⁴C-acetyl-CoA (2 nm, 15 nCi) and 5 μL of camitine acetyltransferase (21 μg protein) the mixture is incubated for 30 min at 30 ℃ and each sample is supplemented with 290 mg of dry Dowex resin 2 × 8 (Cl^--form, 200-400 mesh) and 600 μL H₂O. The samples are shaken for 10 min, spun down (2000 g × 5 min) and the supematant (0.4 mL), is mixed with Bray’s scintillation fluid (10 mL). Radioactivity is measured in an counter.}

参考

https://pubmed.ncbi.nlm.nih.gov/3342076/
https://pubmed.ncbi.nlm.nih.gov/18801379/
https://pubmed.ncbi.nlm.nih.gov/20036318/

https://pubmed.ncbi.nlm.nih.gov/19594753/

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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Dissection of immunotherapeutic predictive versus prognostic transcriptional programs identifies SLC22A5-centric carnitine metabolism-driven resistance to anti-PD-(L)1 treatment in non-small cell lung cancer [ Drug Resist Updat, 2025, 84:101313]	PubMed: 41045681
αKG-mediated carnitine synthesis promotes homologous recombination via histone acetylation [ bioRxiv, 2024, 2024.02.06.578742]	PubMed: 38370789
CRIP1 suppresses BBOX1-mediated carnitine metabolism to promote stemness in hepatocellular carcinoma [ EMBO J, 2022, 41(15):e110218]	PubMed: 35775648
Identification of BBOX1 as a Therapeutic Target in Triple-Negative Breast Cancer [ Cancer Discov, 2020, CD-20-0288]	PubMed: 32690540

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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