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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- CAS No.: 53947-96-9
- 화학식: C32H41N5O6
- 분자량:591.71
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
All Parasite Isoforms
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Biological Activity
제품 설명
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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CAS No. 53947-96-9
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분자량 591.71
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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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.
순도&문서
References
[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)
Nummularine B Related Classifications
HY-P2209 Related Classifications
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