For research use only. Not for therapeutic Use.
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[1].
Zelnecirnon (1 nM-10 μM) inhibits Th2 cells chemotaxis or migration with IC50s of ~370 nM[2].
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[2].
| Catalog Number | I042896 |
| CAS Number | 2366152-15-8 |
| Synonyms | 3-[(3R)-3-[1-[5-chloro-4-[[(1R)-1-(2,4-dichlorophenyl)ethyl]amino]-6-methylpyrimidin-2-yl]azetidin-3-yl]piperidin-1-yl]-1-methylcyclobutane-1-carboxylic acid |
| Molecular Formula | C27H34Cl3N5O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C27H34Cl3N5O2/c1-15(21-7-6-19(28)9-22(21)29)31-24-23(30)16(2)32-26(33-24)35-13-18(14-35)17-5-4-8-34(12-17)20-10-27(3,11-20)25(36)37/h6-7,9,15,17-18,20H,4-5,8,10-14H2,1-3H3,(H,36,37)(H,31,32,33)/t15-,17+,20?,27?/m1/s1 |
| InChIKey | ANPSFQZLPNWKHR-PRZTZBHNSA-N |
| SMILES | CC1=C(C(=NC(=N1)N2CC(C2)C3CCCN(C3)C4CC(C4)(C)C(=O)O)NC(C)C5=C(C=C(C=C5)Cl)Cl)Cl |
| Reference | [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. |
