Betulinic acid

製品コードS3603 バッチS360301

印刷

化学情報

 Chemical Structure Synonyms ALS-357, Lupatic acid, Betulic acid Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C30H48O3

分子量 456.7 CAS No. 472-15-1
Solubility (25°C)* 体外 DMSO 20 mg/mL (43.79 mM)
Ethanol 10 mg/mL (21.89 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 Betulinic acid (ALS-357, Lupatic acid, Betulic acid), a pentacyclic triterpenoid from Syzigium claviflorum, is a inhibitor of HIV-1 with EC50 of 1.4 μ M. It's reported that Betulinic acid acts as a new activator of NF-κB.Phase 1/2.
in vitro Betulinic acid shows anti-HIV activity by blocking HIV replication in H9 lymphocytes with an EC50 value of 1.4 μM and inhibiting uninfected H9 cell growth with an IC50 value of 13 μM. [1] Betulinic acid also acts as anti-melanoma agent through inhibiting aminopeptidase N activity with IC50 of 7.3 μM. [2] In addition, Betulinic acid inhibits eukaryotic topoisomerase I activity with IC50 of 5 μM and can be exploited as a strong candidate for anti-tumor drug. [3]
in vivo Betulinic acid inhibits prostate cancer cell and tumor (xenograft) growth in athymic nude mice bearing LNCaP cells and this is due, in part, to proteasome-dependent downregulation of Sp1, Sp3, Sp4 and several Sp-regulated genes. [4]

プロトコル(参考用のみ)

キナーゼアッセイ Topoisomerase I-DNA interaction
Annealed 25-mer duplex of oligonucleotide-1 and oligonicleotide-2 is incubated with 25 or 50 units of rat liver topoisomerase I at 8 °C for 15 min in the presence or absence of betulinic acid in binding buffer. After incubation the reaction mixtures are electrophoresed in 7% non-denaturing polyacrylamide gel at 4 °C in 0.167 × TBE buffer and DNA bands are stained with ethidium bromid
細胞アッセイ 細胞株 H9 lymphocytes
濃度
反応時間 3 days
実験の流れ H9 lymphocytes ( 1 × 107 cells/ml) are incubated in the presence or absence of HIV-1 (IIIB isolate) for 1 h at 37 °C. Cells are washed thoroughly to remove unadsorbed virions and resuspended in culture medium. Betulinic acid (diluted in test medium) is added to the culture medium. After incubation for 3 days at 37 °C, the cell densities of uninfected cultures are determined to assess toxicity of betulinic acid. A p24 antigen capture assay is used to determine the level of HIV infection in HIV-treated culture
動物実験 動物モデル LNCaP tumor xenograft model
投薬量 10 and 20 mg/kg/d
投与方法 Orally

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

Graphene oxide/gallium nanoderivative as a multifunctional modulator of osteoblastogenesis and osteoclastogenesis for the synergistic therapy of implant-related bone infection [ Bioact Mater, 2023, 25:594-614] PubMed: 37056253
N,N-Dimethyl-3β-hydroxycholenamide attenuates neuronal death and retinal inflammation in retinal ischemia/reperfusion injury by inhibiting Ninjurin 1 [ J Neuroinflammation, 2023, 20(1):91] PubMed: 37029422
Embelin attenuates lipopolysaccharide-induced acute kidney injury through the inhibition of M1 macrophage activation and NF-κB signaling in mice [ Heliyon, 2023, 9(3):e14006] PubMed: 36938407
Citrulline inhibits LPS-induced pyroptosis of RAW264.7 macrophages through NF-κB signaling pathway [ Immun Inflamm Dis, 2023, 11(4):e832] PubMed: 37102651
TAZ ameliorates the microglia-mediated inflammatory response via the Nrf2-ROS-NF-κB pathway [ Mol Ther Nucleic Acids, 2022, 28:435-449] PubMed: 35505966
Spironolactone Ameliorates Senescence and Calcification by Modulating Autophagy in Rat Tendon-Derived Stem Cells via the NF-κB/MAPK Pathway [ Oxid Med Cell Longev, 2021, 2021:5519587] PubMed: 34306308
Betulinic acid promotes the osteogenic differentiation of human periodontal ligament stem cells by upregulating EGR1 [ Acta Biochim Biophys Sin (Shanghai), 2021, gmab111] PubMed: 34519779
Long Noncoding RNA MALAT1 Regulates the Progression of Atherosclerosis by miR-330-5p/NF-κB Signal Pathway [ J Cardiovasc Pharmacol, 2021, 78(2):235-246] PubMed: 34554676
11q Deletion or ALK Activity Curbs DLG2 Expression to Maintain an Undifferentiated State in Neuroblastoma [ Cell Rep, 2020, 32(12):108171] PubMed: 32966799
Betulinic acid restores imatinib sensitivity in BCR-ABL1 kinase-independent, imatinib-resistant chronic myeloid leukemia by increasing HDAC3 ubiquitination and degradation [ Ann N Y Acad Sci, 2020, 1467(1):77-93] PubMed: 31930541

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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