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 [1] [2] [3].
In Vivo, FK3453 (0.3 mM; intracavitary injection; single dose) suppresses TSLP production and reduces the weight of exudate fluid in the air pouch model of inflammation induced by LPS in ICR mice[2].
In Vitro, 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 [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].
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.
[2]. Segawa R, et al. Inhibition of thymic stromal lymphopoietin production by FK3453. J Pharmacol Sci. 2022;149(4):198-204.
[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.
In Vivo, FK3453 (0.3 mM; intracavitary injection; single dose) suppresses TSLP production and reduces the weight of exudate fluid in the air pouch model of inflammation induced by LPS in ICR mice[2].
In Vitro, 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 [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].
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.
[2]. Segawa R, et al. Inhibition of thymic stromal lymphopoietin production by FK3453. J Pharmacol Sci. 2022;149(4):198-204.
[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.