Melevodopa
Melevodopa (Levodopa methylester) is an orally active methylated prodrug of Levodopa (HY-N0304), a dopamine precursor. When used in combination with Carbidopa (HY-B0311) in an effervescent tablet formulation, Melevodopa inhibits motor fluctuations in Parkinson's disease. Melevodopa suppresses subcutaneous tumor growth, pulmonary metastasis proliferation, and primary mass invasiveness of melanoma. Melevodopa induces lipid peroxidation by increasing malondialdehyde levels in melanoma and improves the survival rate of melanoma-bearing mice. Melevodopa can be used in research related to Parkinson's disease (with motor fluctuations) and melanoma.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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- CAS 番号: 7101-51-1
- 分子式: C10H13NO4
- 分子量:211.21
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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生物活性
Melevodopa (1000 mg/kg; i.p.; daily; 15 days; preceded by Benserazide (HY-121275) 100 mg/kg 90-minute pre-injection) alters B16-BL6 melanoma lung colony size distribution toward smaller colonies in both basal and tyrosine/phenylalanine-restricted diet-fed mice, but does not change total lung colony count[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:B6D2F1 (female); C57BL/6 (male, female; inoculated subcutaneously with 106 viable B16 melanoma cells)[2]
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Dosage:1000 mg/kg; preceded by carbidopa 100 mg/kg (90-minute pre-injection)
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Administration:i.p.; daily; 15 days
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Result:Inhibited tumor growth during 15-day treatment period and for 8 days after treatment cessation, with mean tumor volume never reaching that of untreated mice.
Increased median survival from 22 days to 27 days (23% increase) in basal diet-fed mice, and from 28 days to 38 days (36% increase) in restricted diet-fed mice.
Reduced tumor invasion into the pulmonary cavity in mice fed either diet.
Decreased food intake by 0.3 g in basal diet-fed mice and 1.3 g in restricted diet-fed mice during treatment period.
Increased tumor malondialdehyde levels 1.4-fold in basal diet-fed mice and 2.4-fold in restricted diet-fed mice compared to intradietary untreated controls.
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Animal Model:B6D2F1 (female; inoculated intravenously with 2×104 viable B16-BL6 melanoma cells to induce experimental lung metastases)[2]
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Dosage:1000 mg/kg; preceded by benserazide 100 mg/kg (90-minute pre-injection)
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Administration:i.p.; daily; 15 days
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Result:Shifted lung tumor colony size distribution to a higher proportion of small (17.9% vs 8.9% in untreated) and medium (38.3% vs 25.2% in untreated) colonies, and a lower proportion of large colonies (43.8% vs 65.9% in untreated) in basal diet-fed mice.
Shifted colony size distribution to a higher proportion of small colonies (51.4% vs 27.8% in untreated) and a lower proportion of medium (43.3% vs 48.3% in untreated) and large (5.3% vs 23.9% in untreated) colonies in restricted diet-fed mice.
Did not significantly alter the number of lung colonies in either diet group.
化学情報
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CAS 番号 7101-51-1
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性状 Solid
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分子量 211.21
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分子式 C10H13NO4
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Color White to off-white
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SMILES
N[C@H](C(OC)=O)CC1=CC=C(C(O)=C1)O
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別名
Levodopa methylester
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
純度とドキュメンテーション
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取扱説明書 (2659 KB)
参考文献
[1]. Stocchi F, et al. Melevodopa/carbidopa effervescent formulation in the treatment of motor fluctuations in advanced Parkinson's disease. Movement disorders : official journal of the Movement Disorder Society. 2010 Sep 15;25(12):1881-7. [Content Brief]
[2]. Meadows GG, et al. Ascorbate in the treatment of experimental transplanted melanoma. The American journal of clinical nutrition. 1991 Dec;54(6 Suppl):1284S-1291S. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Melevodopa 関連分類
HY-122278 関連分類
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