Navarixin (SCH-527123)

製品コードS8506 バッチS850602

印刷

化学情報

 Chemical Structure Synonyms MK-7123, PS-291822 Storage
(From the date of receipt)
3 years -20°C powder
化学式

C21H23N3O5

分子量 397.42 CAS No. 473727-83-2
Solubility (25°C)* 体外 DMSO 79 mg/mL (198.78 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 40%PEG300 5%Tween80 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。

3.900mg/ml (9.81mM) Taking the 1 mL working solution as an example, add 50 μL of 78 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 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。

1.300mg/ml (3.27mM) Taking the 1 mL working solution as an example, add 50 μL of 26 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 Navarixin (SCH-527123, MK-7123, PS-291822) is a potent, orally bioavailable CXCR2/CXCR1 antagonist with IC50 values of 2.6 nM and 36 nM, respectively.
in vitro

Navarixin (SCH-527123, MK-7123, PS-291822) is a potent, orally bioavailable CXCR2/CXCR1 antagonist with IC50 values of 2.6 nM and 36 nM, respectively.

in vivo

SCH52712, a novel, orally active CXCR1/2 receptor antagonist, inhibits neutrophil recruitment, mucus production, and goblet cell hyperplasia in animal models of pulmonary inflammation.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Cell-free assays
濃度 IC50 values of 2.6 and 36 nM for CXCR2 and CXCR1, respectively.
反応時間
実験の流れ
動物実験 動物モデル Male BALB/c mice
投薬量 3 mg/kg
投与方法 o.g.

参考

  • https://pubmed.ncbi.nlm.nih.gov/17181143/
  • https://pubmed.ncbi.nlm.nih.gov/17496165/

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:

Modulating the CXCR2 Signaling Axis Using Engineered Chemokine Fusion Proteins to Disrupt Myeloid Cell Infiltration in Pancreatic Cancer [ Biomolecules, 2025, 15(5)645] PubMed: 40427538
WNT1-inducible signaling pathway protein 1 activation through C-X-C motif chemokine ligand 5/C-X-C chemokine receptor type 2/leukemia inhibitory factor/leukemia inhibitory factor receptor signaling promotes immunosuppression and neuroendocrine differentiation in prostate cancer [ iScience, 2024, 27(8):110562] PubMed: 39175775
Empowering pancreatic tumor homing with augmented anti-tumor potency of CXCR2-tethered CAR-NK cells [ Mol Ther Oncol, 2024, 32(1):200777] PubMed: 38596297
Epigenetic Regulation of CXC Chemokine Expression by Environmental Electrophiles Through DNA Methyltransferase Inhibition [ Int J Mol Sci, 2024, 25(21)11592] PubMed: 39519144
Metformin potentiates nephrotoxicity by promoting NETosis in response to renal ferroptosis [ Cell Discov, 2023, 9(1):104] PubMed: 37848438
Metformin potentiates nephrotoxicity by promoting NETosis in response to renal ferroptosis [ Cell Discov, 2023, 9(1):104] PubMed: 37848438
Megakaryocyte-Derived IL-8 Acts as a Paracrine Factor for Prostate Cancer Aggressiveness through CXCR2 Activation and Antagonistic AR Downregulation [ Biomol Ther (Seoul), 2023, 31(2):210-218] PubMed: 36787954
Senescent Human Pancreatic Stellate Cells Secrete CXCR2 Agonist CXCLs to Promote Proliferation and Migration of Human Pancreatic Cancer AsPC-1 and MIAPaCa-2 Cell Lines [ Int J Mol Sci, 2022, 23-169275] PubMed: 36012531

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。