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.
For research use only. We do not sell to patients.
- Purity: 99.98%
- CAS No.: 560111-91-3
- Formula: C17H17N5O
- Molecular Weight:307.35
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
All Adenosine Receptor Isoforms
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Biological Activity
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.
Chemical Information
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CAS No. 560111-91-3
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Appearance Solid
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Molecular Weight 307.35
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Formula C17H17N5O
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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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
References
[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 |
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