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.
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- CAS. Nr.: 7101-51-1
- Formel: C10H13NO4
- Molecular Weight:211.21
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Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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.
Chemical Information
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CAS. Nr. 7101-51-1
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Appearance Solid
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Molecular Weight 211.21
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Formel 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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Synonyms
Levodopa methylester
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Reinheit & Dokumentation
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Data Sheet (272 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[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
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Melevodopa Related Classifications
HY-122278 Related Classifications
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