Delgocitinib（JTE-052）
Delgocitinib，也称为 LEO-124249 和 JTE052，是一种有效的选择性 JAK 抑制剂。 在啮齿动物模型中，Delgocitinib（JTE-052）与传统治疗剂比较，可以更有效的减少皮肤炎症并逐步改善慢性皮炎； Delgocitinib（JTE-052）还可通过下调 T 细胞活化和分化来调节接触性超敏反应。
仅供研究使用。 我们不向患者出售。
化学信息
| 名称 | Delgocitinib（JTE-052） |
|---|---|
| Iupac 化学名称 | 3-[(3S,4R)-3-methyl-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1,6-diazaspiro[3.4]octan-1-yl]-3-oxopropanenitrile |
| 同义词 | Delgocitinib ; LEO-124249 ; LEO124249 ; LEO 124249 ; JTE-052 ; JTE 052 ; JTE052 ; |
| 英文同义词 | Delgocitinib ; LEO-124249 ; LEO124249 ; LEO 124249 ; JTE-052 ; JTE 052 ; JTE052 ; |
| 分子式 | C16H18N6O |
| 分子量 | 310.35 |
| Smile | N#CCC(N1C[C@H](C)[C@]12CN(C3=C4C(NC=C4)=NC=N3)CC2)=O |
| InChiKey | LOWWYYZBZNSPDT-ZBEGNZNMSA-N |
| InChi | InChI=1S/C16H18N6O/c1-11-8-22(13(23)2-5-17)16(11)4-7-21(9-16)15-12-3-6-18-14(12)19-10-20-15/h3,6,10-11H,2,4,7-9H2,1H3,(H,18,19,20)/t11-,16-/m0/s1 |
| Cas号 | 1263774-59-9 |
| 相关CAS号 | 2064338-33-4 (EtOH) 1263774-59-9 (free) 2064338-35-6 (CHCl3) |
订购信息
| 包装 | 价格 | 库存 | 纯度 | 备货期 |
|---|---|---|---|---|
| 大货 | 询价 | 询价 | 询价 |
| 外观性状 | 类白色固体粉末 |
|---|---|
| 纯度 | ≧98.0% |
| 存储 | 0-4 ℃ 可短期保存（两周）；- 20 ℃ 可长期保存。 |
| 可溶性 | 溶于DMSO |
| 处理方式 | Refer to MSDS operation |
| 运输条件 | 可在室温下运输。 |
| 海关编码 | 2934200090 |
| Targets | JAK |
|---|---|
| Mechanism | Janus Kinase (Jak) Inhibitors |
| Cell study | Signal Transduction Modulators |
| Animal study | |
| Clinical study | Launched - 2020 |
1: Nakagawa H, Nemoto O, Yamada H, Nagata T, Ninomiya N. Phase 1 studies to assess the safety, tolerability and pharmacokinetics of JTE-052 (a novel Janus kinase inhibitor) ointment in Japanese healthy volunteers and patients with atopic dermatitis. J Dermatol. 2018 Jun;45(6):701-709. doi: 10.1111/1346-8138.14322. Epub 2018 Apr 17. PubMed PMID: 29665062; PubMed Central PMCID: PMC6001687.
2: Nakagawa H, Nemoto O, Igarashi A, Nagata T. Efficacy and safety of topical JTE-052, a Janus kinase inhibitor, in Japanese adult patients with moderate-to-severe atopic dermatitis: a phase II, multicentre, randomized, vehicle-controlled clinical study. Br J Dermatol. 2018 Feb;178(2):424-432. doi: 10.1111/bjd.16014. Epub 2018 Jan 15. PubMed PMID: 28960254.
3: Tanimoto A, Shinozaki Y, Yamamoto Y, Katsuda Y, Taniai-Riya E, Toyoda K, Kakimoto K, Kimoto Y, Amano W, Konishi N, Hayashi M. A novel JAK inhibitor JTE-052 reduces skin inflammation and ameliorates chronic dermatitis in rodent models: Comparison with conventional therapeutic agents. Exp Dermatol. 2018 Jan;27(1):22-29. doi: 10.1111/exd.13370. Epub 2017 Jul 3. PubMed PMID: 28423239.
4: Nomura T, Kabashima K. Advances in atopic dermatitis in 2015. J Allergy Clin Immunol. 2016 Dec;138(6):1548-1555. doi: 10.1016/j.jaci.2016.10.004. Review. PubMed PMID: 27931536.
5: Amano W, Nakajima S, Yamamoto Y, Tanimoto A, Matsushita M, Miyachi Y, Kabashima K. JAK inhibitor JTE-052 regulates contact hypersensitivity by downmodulating T cell activation and differentiation. J Dermatol Sci. 2016 Dec;84(3):258-265. doi: 10.1016/j.jdermsci.2016.09.007. Epub 2016 Sep 13. PubMed PMID: 27665390.
6: Tanimoto A, Shinozaki Y, Nozawa K, Kimoto Y, Amano W, Matsuo A, Yamaguchi T, Matsushita M. Improvement of spontaneous locomotor activity with JAK inhibition by JTE-052 in rat adjuvant-induced arthritis. BMC Musculoskelet Disord. 2015 Nov 6;16:339. doi: 10.1186/s12891-015-0802-0. PubMed PMID: 26546348; PubMed Central PMCID: PMC4636776.
7: Amano W, Nakajima S, Kunugi H, Numata Y, Kitoh A, Egawa G, Dainichi T, Honda T, Otsuka A, Kimoto Y, Yamamoto Y, Tanimoto A, Matsushita M, Miyachi Y, Kabashima K. The Janus kinase inhibitor JTE-052 improves skin barrier function through suppressing signal transducer and activator of transcription 3 signaling. J Allergy Clin Immunol. 2015 Sep;136(3):667-677.e7. doi: 10.1016/j.jaci.2015.03.051. Epub 2015 Jun 24. PubMed PMID: 26115905.
8: Tanimoto A, Ogawa Y, Oki C, Kimoto Y, Nozawa K, Amano W, Noji S, Shiozaki M, Matsuo A, Shinozaki Y, Matsushita M. Pharmacological properties of JTE-052: a novel potent JAK inhibitor that suppresses various inflammatory responses in vitro and in vivo. Inflamm Res. 2015 Jan;64(1):41-51. doi: 10.1007/s00011-014-0782-9. Epub 2014 Nov 12. PubMed PMID: 25387665; PubMed Central PMCID: PMC4286029.
