Zelnecirnon (RPT193) is an orally active inhibitor of CCR4, blocks the recruitment of Th2 inflammatory immune cells into inflamed tissues. Zelnecirnon can be used for allergic inflammation in atopic dermatitis, asthma, and other diseases research.
性状
Solid
IC50 & Target[1][2]
CCR4
体外研究(In Vitro)
Zelnecirnon (1 nM-10 μM) inhibits Th2 cells chemotaxis or migration with IC50s of ~370 nM. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Zelnecirnon (100 mg/kg; p.o.; once daily; 2 d, 1 d before OVA-challenge) reduces skin inflammation in an acute ovalbumin (OVA)-induced atopic dermatitis model in mice. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
ClinicalTrial
参考文献
[1]. Bissonnette R, et al. RPT193, an oral CCR4 inhibitor: Efficacy results from a randomized, placebo-controlled Phase 1b monotherapy trial in patients with moderate-to-severe atopic dermatitis[C]//EXPERIMENTAL DERMATOLOGY. 111 RIVER ST, HOBOKEN 07030-5774, NJ USA: WILEY, 2021, 30: 40-41.[2]. Cheng L, et al. Development and first-in-human characterization of a potent oral CCR4 antagonist for the treatment of atopic dermatitis[C]//Journal of Investigative Dermatology. STE 800, 230 PARK AVE, NEW YORK, NY 10169 USA: ELSEVIER SCIENCE INC, 2020, 140(7): S77-S77.
溶解度数据
In Vitro: DMSO : 100 mg/mL (176.38 mM; Need ultrasonic)配制储备液