Betulinic acid

製品コードS3603 バッチS360303

印刷

化学情報

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

47 mg/mL (102.91 mM)

Ethanol

5 mg/mL (10.94 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	2.350mg/ml (5.15mM)	Taking the 1 mL working solution as an example, add 50 μL of 47 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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	Syzigium claviflorum由来の五環性トリテルペノイドであるBetulinic acid（ALS-357、Lupatic acid、Betulic acid）は、EC50が1.4 µMのHIV-1阻害剤です。Betulinic acidは、NF-κBの新しい活性化因子として作用すると報告されています。フェーズ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. This compound also acts as anti-melanoma agent through inhibiting aminopeptidase N activity with IC50 of 7.3 μM. In addition, it inhibits eukaryotic topoisomerase I activity with IC50 of 5 μM and can be exploited as a strong candidate for anti-tumor drug.
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.

プロトコル(参考用のみ)

キナーゼアッセイ	Topoisomerase I-DNA interaction
キナーゼアッセイ	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 this compound. 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

参考

https://pubmed.ncbi.nlm.nih.gov/8176401/
https://pubmed.ncbi.nlm.nih.gov/9810272/
https://pubmed.ncbi.nlm.nih.gov/12118187/

https://pubmed.ncbi.nlm.nih.gov/17363604/

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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：

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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

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。