Nummularine B
Nummularine B (Daechuine S27; N-Demethylamphibine H) is an anti-parasite agent. Nummularine B inhibits calmodulin-dependent phosphodiesterase activity with an IC50 of 16.8 μM. Nummularine B inhibits the growth of Plasmodium and Leishmania donovani in vitro. Nummularine B inhibits the calmodulin-dependent activity of actomyosin Ca2+-ATPase. Nummularine B is applicable to research related to malaria and visceral leishmaniasis.
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- No. CAS: 53947-96-9
- Fòrmula: C32H41N5O6
- Peso molecular:591.71
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
In Vitro
Nummularine B inhibits the growth of the K1 strain of Plasmodium falciparum, with an IC50 of 3.6 μM[1].
Nummularine B (20 min) inhibits calmodulin-dependent Ca2+-ATPase activity in actomyosin from rat posterior thigh muscle, with an IC50 of 27.0 μM[2].
Nummularine B (10 min) inhibits the activity of calmodulin-dependent phosphodiesterase from bovine brain-derived enzymes, with an IC50 value of 16.8 μM[2].
Nummularine B (Compound 11) (72 h (T. b. rhodesiense, L. donovani, P. falciparum); 96 h (T. cruzi)) potently inhibits Plasmodium falciparum with an IC50 of 14.7 μM; it also inhibits Leishmania donovani with an IC50 of 44.8 μM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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No. CAS 53947-96-9
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Peso molecular 591.71
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Fòrmula C32H41N5O6
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SMILES
C([C@@H](NC([C@@H](NC)C)=O)C(C)C)(=O)N1[C@]2([C@@](OC=3C=C(C(OC)=CC3)/C=C\NC(=O)[C@H](CC4=CC=CC=C4)NC2=O)(CC1)[H])[H]
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Synonyms
Daechuine S27; N-Demethylamphibine H
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Sequence
{Me-Ala}-Val-Cyclo({N-[(1Z)-2-(5-hydroxy-2-methoxyphenyl)ethenyl]-Pro}-Phe) (lactam bridge: Pro3-Phe4)
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Sequence Shortening
{Me-Ala}-V-Cyclo({N-[(1Z)-2-(5-hydroxy-2-methoxyphenyl)ethenyl]-Pro}-F) (lactam bridge: Pro3-Phe4)
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Structure Classification
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocolo
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
Pureza y Documentación
Referencias
[1]. Tuenter E, et al. Antiplasmodial Activity, Cytotoxicity and Structure-Activity Relationship Study of Cyclopeptide Alkaloids. Molecules. 2017;22(2):224. Published 2017 Feb 2. [Content Brief]
[2]. Hwang KH, et al. Inhibition of calmodulin-dependent calcium-ATPase and phosphodiesterase by various cyclopeptides and peptide alkaloids from the Zizyphus species. Arch Pharm Res. 2001;24(3):202-206. [Content Brief]
[3]. Sevik Kilicaslan O, et al. Antiprotozoal activity of natural products from Nigerien plants used in folk medicine. Front Pharmacol. 2023;14:1190241. Published 2023 Jun 23. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)