Pranlukast

製品コードS1829 バッチS182903

印刷

化学情報

Synonyms

ONO-1078,ono-rs-411

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₇H₂₃N₅O₄

分子量

481.5

CAS No.

103177-37-3

Solubility (25°C)*

体外

DMSO

48 mg/mL (99.68 mM)

Water

Insoluble

Ethanol

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 40%PEG300 2 5%Tween80 3 50%ddH2O 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。	1.200mg/ml (2.49mM)	Taking the 1 mL working solution as an example, add 50 μL of 24 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% 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。	0.600mg/ml (1.25mM)	Taking the 1 mL working solution as an example, add 50 μL of 12 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	Pranlukast (ONO-1078,ono-rs-411) is an orally administered, and selective antagonist of the cysteinyl leukotrienes (LT) C(4), LTD(4) and LTE(4), used in the prophylactic treatment of chronic bronchial asthma.
in vitro	Pranlukast inhibits NF-kappa B activation in 1.3% DMSO-differentiated U-937 and Jurkat cells by about 40% & 30%, respectively. This compound and MK-571 inhibit NF-kappa B activation in 1.3% DMSO-differentiated U-937 and Jurkat cells in a dose-related manner. It and MK-571 inhibits LPS-induced IL-6 production in PBMC by about 65% and 15%, respectively. ^[1] This compound or zafirlukast significantly inhibits 10 mM LTD4-evoked 35SO4 output in a concentration-dependent fashion, with maximal inhibitions of 83% at 10 mM Pranlukast and 78% at 10 mM Zafirlukast, and IC50 values of 0.3 mM for Pranlukast and 0.6 mM for Zafirlukast. It (0.5 microM) causes a parallel rightward shift of the LTD4 concentration-response curve with a pKB of 7. This compound or Zafirlukast (5 microM each) significantly suppresses ovalbumin-induced secretion in tracheae from sensitized guinea-pigs by 70% and 65%, respectively. ^[2] It also inhibits NF-kappaB activation induced by phorbol 12-myristate 13-acetate (PMA). This chemical also significantly inhibits LPS-induced MUC2 mRNA expression by reverse transcription-polymerase chain reaction (RT-PCR) analysis in NCI-H292 cells. It also inhibits LPS-induced MUC2 gene expression in HM3-MUC2 cells. ^[3]
in vivo	Pranlukast significantly reduces lesion volume, and increases neuron densities in the cortex and hippocampal CA1 region in the ischemic hemispheres of mice. This compound also remarkably reduces the thickness of a scar wall in the ischemic hemispheres of mice. ^[4]

プロトコル(参考用のみ)

参考

https://pubmed.ncbi.nlm.nih.gov/12801316/
https://pubmed.ncbi.nlm.nih.gov/9647482/
https://pubmed.ncbi.nlm.nih.gov/15475658/

https://pubmed.ncbi.nlm.nih.gov/16051204/

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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：

Leukotriene receptor antagonists enhance HCC treatment efficacy by inhibiting ADAMs and suppressing MICA shedding [ Cancer Immunol Immunother, 2021, 70(1):203-213]	PubMed: 32683508

Leukotriene receptor antagonists enhance HCC treatment efficacy by inhibiting ADAMs and suppressing MICA shedding [ Cancer Immunol Immunother, 2021, 70(1):203-213]

PubMed: 32683508

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。