FK3453
Based on 1 Customer Validation
FK3453 is a dual adenosine A1/A2 inhibitor and a TSLP inhibitor. FK3453 is also a substrate of aldehyde oxidase (AO). FK3453 can inhibit the production of TSLP and IL-33. FK3453 is useful for research on Parkinson’s disease and allergic disorders.
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: 560111-91-3
- 分子式: C17H17N5O
- 分子量:307.35
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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
Adenosine Receptor アイソフォーム固有の製品をすべて表示
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生物活性
FK3453 (1-10 µM; 0-24 h) inhibits constitutive TSLP production in KCMH-1 mouse keratinocytes in a concentration-dependent manner without reducing cell viability[2].
FK3453 (1-10 µM; 4.5 h) inhibits TSLP mRNA expression in PAM212 mouse keratinocytes treated with TPA (HY-18739)[2].
FK3453 (1-10 µM; 4.5-24.5 h) inhibits T4FP-induced and TPA-induced TSLP mRNA expression in NHEKs, as well as TPA-induced IL-33 mRNA expression[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PA (HY-18739) treated PAM212 cells
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Concentration:1, 3 and 10 μM
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Incubation Time:Pretreated with 30 min, then co-incubation for 4 h
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Result:Reduced the levels of TSLP mRNA in a ntration-dependent manner.
| Species | Dose | Route | T1/2β | Vdss | AUCinf | CLt | Cmax | Tmax | F | AUC0-∞ | T1/2 | AUC | CL |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 3.2 mg/kg | i.v. | / | / | / | 10.8 mL/min/kg | / | / | / | / | 0.4 h | / | / |
| Rat[1] | 3.2 mg/kg | p.o. | / | / | / | / | 544 ng/mL | / | 34.6 % | / | / | 1789.4 ng·h/mL | 29.8 mL/min/kg |
| Rat[3] | 0.1 (male) mg/kg | i.v. | 0.95 h | 0.69 L/kg | 111.9 ng·h/mL | 14.9 mL/min/kg | / | / | / | / | / | / | / |
| Rat[3] | 0.32 (male) mg/kg | i.v. | 0.50 h | 0.91 L/kg | 304.1 ng·h/mL | 17.6 mL/min/kg | / | / | / | / | / | / | / |
| Rat[3] | 3.2 (male) mg/kg | i.v. | 0.37 h | 0.48 L/kg | 5170.3 ng·h/mL | 10.8 mL/min/kg | / | / | / | / | / | / | / |
| Rat[3] | 0.1 (male) mg/kg | p.o. | / | / | 34.2 ng·h/mL | / | 41.0 ng/mL | 0.5 h | 30.5 % | / | / | / | / |
| Rat[3] | 0.32 (male) mg/kg | p.o. | / | / | 127.4 ng·h/mL | / | 36.8 ng/mL | 1.5 h | 41.9 % | / | / | / | / |
| Rat[3] | 3.2 (male) mg/kg | p.o. | / | / | / | / | 544.0 ng/mL | 1.0 h | 34.6 % | 1789.4 ng·h/mL | / | / | / |
| Rat[3] | 0.1 (female) mg/kg | i.v. | 0.73 h | 0.96 L/kg | 124.2 ng·h/mL | 14.1 mL/min/kg | / | / | / | / | / | / | / |
| Rat[3] | 1 (female) mg/kg | i.v. | 2.77 h | 0.77 L/kg | 4987.2 ng·h/mL | 7.8 mL/min/kg | / | / | / | / | / | / | / |
| Rat[3] | 1 (female) mg/kg | p.o. | / | / | 3372.4 ng·h/mL | / | 373.3 ng/mL | 1.7 h | 67.6 % | / | / | / | / |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR mice (five-week-old male, lipopolysaccharide-induced air pouch-type inflammation model)[2]
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Dosage:0.3 mM
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Administration:local injection into air pouch; single dose
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Result:Significantly inhibited LPS-induced increases in TSLP protein levels in pouch fluid and TSLP mRNA levels in pouch wall tissues.
Strongly decreased the weight of pouch fluids.
化学情報
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CAS 番号 560111-91-3
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性状 Solid
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分子量 307.35
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分子式 C17H17N5O
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Color White to off-white
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SMILES
O=C1C=CC(C2=C(C3=CC=CC=C3)N=C(N)N=C2)=NN1C(C)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
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 : 50 mg/mL (162.68 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 (275 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]. Sanoh S, et al. Prediction of human metabolism of FK3453 by aldehyde oxidase using chimeric mice transplanted with human or rat hepatocytes. Drug Metab Dispos. 2012;40(1):76-82. [Content Brief]
[2]. Segawa R, et al. Inhibition of thymic stromal lymphopoietin production by FK3453. J Pharmacol Sci. 2022;149(4):198-204. [Content Brief]
[3]. Akabane T, et al. Case report of extensive metabolism by aldehyde oxidase in humans: pharmacokinetics and metabolite profile of FK3453 in rats, dogs, and humans. Xenobiotica. 2011;41(5):372-384. [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. 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 | 3.2536 mL | 16.2681 mL | 32.5362 mL | 81.3405 mL |
| 5 mM | 0.6507 mL | 3.2536 mL | 6.5072 mL | 16.2681 mL | |
| 10 mM | 0.3254 mL | 1.6268 mL | 3.2536 mL | 8.1340 mL | |
| 15 mM | 0.2169 mL | 1.0845 mL | 2.1691 mL | 5.4227 mL | |
| 20 mM | 0.1627 mL | 0.8134 mL | 1.6268 mL | 4.0670 mL | |
| 25 mM | 0.1301 mL | 0.6507 mL | 1.3014 mL | 3.2536 mL | |
| 30 mM | 0.1085 mL | 0.5423 mL | 1.0845 mL | 2.7113 mL | |
| 40 mM | 0.0813 mL | 0.4067 mL | 0.8134 mL | 2.0335 mL | |
| 50 mM | 0.0651 mL | 0.3254 mL | 0.6507 mL | 1.6268 mL | |
| 60 mM | 0.0542 mL | 0.2711 mL | 0.5423 mL | 1.3557 mL | |
| 80 mM | 0.0407 mL | 0.2034 mL | 0.4067 mL | 1.0168 mL | |
| 100 mM | 0.0325 mL | 0.1627 mL | 0.3254 mL | 0.8134 mL |
FK3453 関連分類
HY-404647 関連分類
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