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Methotrexate metabolite

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Chemical Structure| 19741-14-1 同义名 : DAMPA
CAS号 : 19741-14-1
货号 : A532297
分子式 : C15H15N7O2
纯度 : 95%
分子量 : 325.325
MDL号 : MFCD00075774
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 4 mg/mL(12.3 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Methotrexate metabolite (DAMPA), is the active metabolite of methotrexate. Methotrexate is a folate antagonist and is widely used as an immunosuppressant and chemotherapeutic agent[1].Methotrexate metabolite is an antimalarial drug that inhibits parasite growth under physiological folate conditions with an IC50 value of 446 nM for antifolate-sensitive strains and 812 nM for highly resistant strains. Methotrexate metabolite has no activity against mammalian cells. Methotrexate metabolite is inactive in mammalian cells. Methotrexate metabolite has the least inhibitory effect on dihydrofolate reductase among the metabolites of methotrexate[2][3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.07mL

0.61mL

0.31mL

15.37mL

3.07mL

1.54mL

30.74mL

6.15mL

3.07mL
参考文献

[1]Schofield RC, et al. Development and validation of a turbulent flow chromatography and tandem mass spectrometry method for the quantitation of methotrexate and its metabolites 7-hydroxy methotrexate and DAMPA in serum. J Chromatogr B Analyt Technol Biomed Life Sci. 2015 Oct 1;1002:169-75.

[2]Nduati E, et al., 2,4-diaminopteridine-based compounds as precursors for de novo synthesis of antifolates: a novel class of antimalarials. Antimicrob Agents Chemother. 2005 Sep;49(9):3652-7.

[3]Widemann BC, et al., Pharmacokinetics and metabolism of the methotrexate metabolite 2, 4-diamino-N(10)-methylpteroic acid. J Pharmacol Exp Ther. 2000 Sep;294(3):894-901.