AZD8309
Based on 1 Customer Validation
AZD8309 is an orally active antagonist of CXCR2. AZD8309 has the ability to regulate the transmigration of neutrophils. AZD8309 can be used in the study of inflammatory diseases.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.98%
- CAS 番号: 333742-48-6
- 分子式: C15H14F2N4O2S2
- 分子量:384.42
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保管条件:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
生物活性
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CXCR2 4 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
1 nM
Compound: 30b
|
Displacement of [125I]IL8 from human recombinant CXCR2 expressed in HEK293 cells by SPA assay
Displacement of [125I]IL8 from human recombinant CXCR2 expressed in HEK293 cells by SPA assay
|
[PMID: 18240390] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL6 mice (25-30 g) with experimental pancreatitis[1]
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Dosage:50 mg/kg
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Administration:Oral gavage; twice daily starting 3 h prior to pancreatitis induction
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Result:Significantly reduced MPO in the pancreas and lungs (8 h & 24 h) and reduced intrapancreatic trypsin and elastase activity (8 h) in caerulein-pancreatitis.
Reduced serum cytokine levels as well as histopathological damage.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 333742-48-6
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性状 Solid
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分子量 384.42
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分子式 C15H14F2N4O2S2
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Color White to off-white
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SMILES
O=C1SC2=C(N=C(N=C2N1)SCC3=CC=CC(F)=C3F)N[C@@H](CO)C
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶剤 & 溶解度
DMSO : 50 mg/mL (130.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Malla SR, et al. Effect of oral administration of AZD8309, a CXCR2 antagonist, on the severity of experimental pancreatitis. Pancreatology. 2016 Sep-Oct;16(5):761-9. [Content Brief]
[2]. Walters I, Austin C, Austin R, et al. Evaluation of a series of bicyclic CXCR2 antagonists. Bioorg Med Chem Lett. 2008;18(2):798-803. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6013 mL | 13.0066 mL | 26.0132 mL | 65.0330 mL |
| 5 mM | 0.5203 mL | 2.6013 mL | 5.2026 mL | 13.0066 mL | |
| 10 mM | 0.2601 mL | 1.3007 mL | 2.6013 mL | 6.5033 mL | |
| 15 mM | 0.1734 mL | 0.8671 mL | 1.7342 mL | 4.3355 mL | |
| 20 mM | 0.1301 mL | 0.6503 mL | 1.3007 mL | 3.2517 mL | |
| 25 mM | 0.1041 mL | 0.5203 mL | 1.0405 mL | 2.6013 mL | |
| 30 mM | 0.0867 mL | 0.4336 mL | 0.8671 mL | 2.1678 mL | |
| 40 mM | 0.0650 mL | 0.3252 mL | 0.6503 mL | 1.6258 mL | |
| 50 mM | 0.0520 mL | 0.2601 mL | 0.5203 mL | 1.3007 mL | |
| 60 mM | 0.0434 mL | 0.2168 mL | 0.4336 mL | 1.0839 mL | |
| 80 mM | 0.0325 mL | 0.1626 mL | 0.3252 mL | 0.8129 mL | |
| 100 mM | 0.0260 mL | 0.1301 mL | 0.2601 mL | 0.6503 mL |