| Identification | Back Directory | [Name]
Cyclobutanecarboxylic acid, 3-[(3R)-3-[1-[5-chloro-4-[[(1R)-1-(2,4-dichlorophenyl)ethyl]amino]-6-methyl-2-pyrimidinyl]-3-azetidinyl]-1-piperidinyl]-1-methyl-, trans- | [CAS]
2366152-15-8 | [Synonyms]
Cyclobutanecarboxylic acid, 3-[(3R)-3-[1-[5-chloro-4-[[(1R)-1-(2,4-dichlorophenyl)ethyl]amino]-6-methyl-2-pyrimidinyl]-3-azetidinyl]-1-piperidinyl]-1-methyl-, trans- | [Molecular Formula]
C27H34Cl3N5O2 | [MOL File]
2366152-15-8.mol | [Molecular Weight]
566.95 |
| Chemical Properties | Back Directory | [Boiling point ]
706.9±70.0 °C(Predicted) | [density ]
1.387±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [form ]
Solid | [pka]
4.09±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
Zelnecirnon, also known as RPT193, is a CCR4 antagonist that blocks the recruitment of Th2 cells in order to treat inflammatory diseases (taken orally). The Phase 1b trial, which was conducted in patients with atopic dermatitis, found that markable improvement occurred after 4 weeks with little side effects. A Phase 2 clinical trial is currently being conducted to evaluate the efficacy and safety of Zelnecirnon, with an expected end date of September 2023. | [Uses]
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]. | [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[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. |
| [IC 50]
CCR4 | [storage]
Store at -20°C | [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. |
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