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m-Methoxybenzamide Sale

(Synonyms: 3-甲氧基苯甲酰胺,3-MBA) 目录号 : GC47693

A PARP inhibitor

m-Methoxybenzamide Chemical Structure

Cas No.:5813-86-5

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5 g
¥839.00
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10 g
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25 g
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产品描述

m-Methoxybenzamide is an inhibitor of poly(ADP-ribose) polymerase (PARP; Ki = <2 µM).1 It also inhibits human placental ADP ribosyl transferase activity by 93% when used at a concentration of 100 µM.2 m-Methoxybenzamide (100, 200, and 300 mg/kg) increases the pain threshold in the paw pinch test in rats.3

1.Purnell, M.R., and Whish, W.J.Novel inhibitors of poly(ADP-ribose) synthetaseBiochem. J.185(3)775-777(1980) 2.Burtscher, H.J., Auer, B., Klocker, H., et al.Isolation of ADP-ribosyltransferase by affinity chromatographyAnal. Biochem.152(2)285-290(1986) 3.Sanders, R., Dill, R.E., Dorris, R.L., et al.Analgesic effects of 3-methoxybenzamide in ratsJ. Pharm. Pharmacol.41(4)268-269(1989)

Chemical Properties

Cas No. 5813-86-5 SDF
别名 3-甲氧基苯甲酰胺,3-MBA
Canonical SMILES COC1=CC=CC(C(N)=O)=C1
分子式 C8H9NO2 分子量 151.2
溶解度 DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.50 mg/ml,Ethanol: 1 mg/ml 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 6.6138 mL 33.0688 mL 66.1376 mL
5 mM 1.3228 mL 6.6138 mL 13.2275 mL
10 mM 0.6614 mL 3.3069 mL 6.6138 mL
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Research Update

ADP-ribosyltransferase in Plasmodium (malaria parasites)

Biochem J 1983 Mar 1;209(3):687-93.PMID:6307262DOI:10.1042/bj2090687.

The nuclei of Plasmodium yoelii nigeriensis contain an enzyme, ADP-ribosyltransferase, that will incorporate the ADP-ribose moiety of NAD+ into acid-insoluble product. The time, pH and temperature optima of this incorporation are 30 min, 8.5 and 25 degrees C respectively. Maximum stimulation of the enzyme activity is obtained with 1.0 mM-dithiothreitol or 2.0 mM-2-mercaptoethanol. Ca2+ and Mg2+ ions at optimum concentrations of 5 mM and 10 mM respectively stimulated the activity of the enzyme by 21% and 91%. The enzyme activity is, however, inhibited by 24% in the presence of 10 mM-MnSO4. The substrate, NAD+, exhibits an apparent Km of 500 microM, and the activity of the enzyme is inhibited by four chemical classes of inhibitors: nicotinamides, methylxanthines, thymidine and aromatic amides. The inhibitors are effective in the following increasing order: nicotinamide less than 3-aminobenzamide less than thymidine less than 5-methylnicotinamide less than theophylline less than m-Methoxybenzamide less than theobromine. The enzyme activity is also inhibited by some DNA-binding anti-malarial drugs.