| 中文名称 |
Zelnecirnon
|
| 英文名称 |
Zelnecirnon
|
| 英文别名 |
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-;Zelnecirnon
|
| Cas No. |
2366152-15-8
|
| 分子式 |
C27H34Cl3N5O2
|
| 分子量 |
566.95
|
| 包装储存 |
Powder -20°C 3 years;In solvent -80°C 6 months
|
| 详情描述 |
Zelnecirnon (RPT193) 是具有口服活性的 CCR4 抑制剂。Zelnecirnon 抑制 Th2 炎性免疫细胞募集到炎症组织,在特应性皮炎、哮喘等疾病中起着过敏性炎症的具有重要作用。
|
| 产品详情 |
Zelnecirnon (RPT193) 是具有口服活性的 CCR4 抑制剂。Zelnecirnon 抑制 Th2 炎性免疫细胞募集到炎症组织,在特应性皮炎、哮喘等疾病中起着过敏性炎症的具有重要作用。
|
| 生物活性 |
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
|
[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.
1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。
2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。