CAY10471
Based on 1 Customer Validation
CAY10471 (TM30089) is a potent, selective, and orally active prostaglandin D2 receptor CRTH2 antagonist. CAY10471 attenuates the progression of tubulointerstitial fibrosis and chronic contact hypersensitivity (CHS) in animal model.
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: 99.9%
- CAS 番号: 627865-18-3
- 分子式: C21H21FN2O4S
- 分子量:416.47
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保管条件:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
生物活性
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CRTH2 |
CAY10471 (1 μM; 1-24 hours) decreases 15dPGJ2-induced phosphorylation of p38 MAP kinase significantly in PC12 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC12 cells
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Concentration:1 μM
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Incubation Time:1 or 24 hours
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Result:Blocked 15d-PGJ2-induced p38 MAP kinase activation.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c mice, DP−/− mice, CRTH2−/− mice[2]
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Dosage:2 mg/kg
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Administration:Oral treatment; once daily; challenged on day 22 or over 10 consecutive days
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Result:Significantly suppressed both CHS and IgE-CAI inflammatory responses.
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Animal Model:C57BL/6 mice[3]
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Dosage:20 mg/kg
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Administration:Oral treatment; twice daily; beginning 3/4/5 days before UUO
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Result:Slowed the progression of renal fibrosis in the obstructed kidneys.
化学情報
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CAS 番号 627865-18-3
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性状 Solid
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分子量 416.47
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分子式 C21H21FN2O4S
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Color White to off-white
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SMILES
O=C(CN1C2=C(CC(CC2)N(C)S(=O)(C3=CC=C(C=C3)F)=O)C4=C1C=CC=C4)O.[Rotation (+)]
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別名
TM30089
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
DMSO : 30 mg/mL (72.03 mM; Need ultrasonic and warming; 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). 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). 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 (279 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Hatanaka M, et al. 15d-prostaglandin J2 enhancement of nerve growth factor-induced neurite outgrowth is blocked by the chemoattractant receptor- homologous molecule expressed on T-helper type 2 cells (CRTH2) antagonist CAY10471 in PC12 cells. J Pharmacol Sci. 2010;113(1):89-93. Epub 2010 Apr 16. [Content Brief]
[2]. Matsushima Y, et al. Distinct roles of prostaglandin D2 receptors in chronic skin inflammation.Mol Immunol. 2011 Oct;49(1-2):304-10. [Content Brief]
[3]. Ito H, et al. PGD2-CRTH2 pathway promotes tubulointerstitial fibrosis.J Am Soc Nephrol. 2012 Nov;23(11):1797-809. [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). 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 | 2.4011 mL | 12.0057 mL | 24.0113 mL | 60.0283 mL |
| 5 mM | 0.4802 mL | 2.4011 mL | 4.8023 mL | 12.0057 mL | |
| 10 mM | 0.2401 mL | 1.2006 mL | 2.4011 mL | 6.0028 mL | |
| 15 mM | 0.1601 mL | 0.8004 mL | 1.6008 mL | 4.0019 mL | |
| 20 mM | 0.1201 mL | 0.6003 mL | 1.2006 mL | 3.0014 mL | |
| 25 mM | 0.0960 mL | 0.4802 mL | 0.9605 mL | 2.4011 mL | |
| 30 mM | 0.0800 mL | 0.4002 mL | 0.8004 mL | 2.0009 mL | |
| 40 mM | 0.0600 mL | 0.3001 mL | 0.6003 mL | 1.5007 mL | |
| 50 mM | 0.0480 mL | 0.2401 mL | 0.4802 mL | 1.2006 mL | |
| 60 mM | 0.0400 mL | 0.2001 mL | 0.4002 mL | 1.0005 mL |