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RPT193

Names

[ CAS No. ]:
2366152-15-8

[ Name ]:
RPT193

Biological Activity

[Description]:

RPT193 is an orally active inhibitor of CCR4, blocks the recruitment of Th2 inflammatory immune cells into inflamed tissues. RPT193 can be used for allergic inflammation in atopic dermatitis, asthma, and other diseases research[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> CCR
Signaling Pathways >> Immunology/Inflammation >> CCR
Research Areas >> Inflammation/Immunology

[Target]

CCR4


[In Vitro]

RPT193 (1 nM-10 μM) inhibits Th2 cells chemotaxis or migration with IC50s of ~370 nM[2].

[In Vivo]

RPT193 (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[2]. Animal Model: Acute ovalbumin (OVA)-induced atopic dermatitis model in mouse[2] Dosage: 100 mg/kg Administration: Oral gavage; once daily; for 2 days, started 1 day before OVA-challenge (in mouse ear) Result: Decreased the ear thickness significantly.

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C27H34Cl3N5O2

[ Molecular Weight ]:
566.95

Related Compounds