Orismilast
Based on 1 Customer Validation
Orismilast (LEO-32731) is an orally active and selective PDE4 inhibitor used for the research of inflammatory diseases. Orismilast demonstrates potent inhibition of PDE4B and PDE4D subtype splice variants.
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: 99.88%
- CAS 番号: 1353546-86-7
- 分子式: C19H15Cl2F2NO7S
- 分子量:510.29
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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PDE4B3 3 nM (IC50) |
PDE4D7 3 nM (IC50) |
PDE4D5 3 nM (IC50) |
PDE4B2 6 nM (IC50) |
PDE4D3 8 nM (IC50) |
PDE4D4 8 nM (IC50) |
PDE4D1 9 nM (IC50) |
PDE4D2 9 nM (IC50) |
PDE4A4 11 nM (IC50) |
PDE4B1 16 nM (IC50) |
PDE4A1 16 nM (IC50) |
PDE4A10 52 nM (IC50) |
PDE4C2 104 nM (IC50) |
Orismilast inhibits tumour necrosis factor α (TNFα), and the secretion of T-helper (Th)1 (TNFα and IFNγ), Th17 (IL-22 and IL-23), and Th2 (IL-4, IL-5, and IL-13) related cytokines in PBMC[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PBMC.
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Concentration:0-30 nM.
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Incubation Time:72 h.
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Result:Inhibited pro-inflammatory TNFα release.
Inhibited the secretion of cytokines across all investigated T-helper cell sublineages, with most the profound effect on Th1-cell effector cytokines but also demonstrates potent inhibition on Th17 cells and Th2 cells related cytokines.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/cABomTac mice (sensitized to oxazolone on the right ear with a single application of 10 μl oxazolone (0.8% in acetone) on Day 7)[2].
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Dosage:10 and 30mg/kg.
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Administration:Orally.
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Result:Both the 10 mg/kg and 30mg/kg doses of oral orismilast resulted in a significant reduction in ear thickness over time (p<0.0001, respectively;) with no impact on bodyweight during the treatment period.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1353546-86-7
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性状 Solid
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分子量 510.29
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分子式 C19H15Cl2F2NO7S
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Color White to off-white
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SMILES
O=S1(CCC2(OC3=C(C=CC(C(CC4=C(C=[N+](C=C4Cl)[O-])Cl)=O)=C3O2)OC(F)F)CC1)=O
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別名
LEO-32731
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (195.97 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. 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. 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 (277 KB)
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取扱説明書 (2659 KB)
参考文献
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. 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 | 1.9597 mL | 9.7983 mL | 19.5967 mL | 48.9917 mL |
| 5 mM | 0.3919 mL | 1.9597 mL | 3.9193 mL | 9.7983 mL | |
| 10 mM | 0.1960 mL | 0.9798 mL | 1.9597 mL | 4.8992 mL | |
| 15 mM | 0.1306 mL | 0.6532 mL | 1.3064 mL | 3.2661 mL | |
| 20 mM | 0.0980 mL | 0.4899 mL | 0.9798 mL | 2.4496 mL | |
| 25 mM | 0.0784 mL | 0.3919 mL | 0.7839 mL | 1.9597 mL | |
| 30 mM | 0.0653 mL | 0.3266 mL | 0.6532 mL | 1.6331 mL | |
| 40 mM | 0.0490 mL | 0.2450 mL | 0.4899 mL | 1.2248 mL | |
| 50 mM | 0.0392 mL | 0.1960 mL | 0.3919 mL | 0.9798 mL | |
| 60 mM | 0.0327 mL | 0.1633 mL | 0.3266 mL | 0.8165 mL | |
| 80 mM | 0.0245 mL | 0.1225 mL | 0.2450 mL | 0.6124 mL | |
| 100 mM | 0.0196 mL | 0.0980 mL | 0.1960 mL | 0.4899 mL |
Orismilast 関連分類
HY-117960 関連分類
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