生物活性：Deuruxolitinib, a deuterated Ruxolitinib (HY-50856), is an orally active JAK1 and JAK2 inhibitor. Deuruxolitinib demonstrates significant hair regrowth effects. Deuruxolitinib can be used for the research of alopecia areata[1].
IC50 & Target[1]：JAK1
JAK2
体外研究(In Vitro)："氢、碳和其他元素的稳定重同位素已被纳入药物分子中，主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注，因为它可能影响药物的药代动力学和代谢谱[2]。氘代化合物的潜在优势：
（1）延长体内半衰期。氘代化合物或能够延长化合物的药代动力学特征，即延长体内半衰期。由此可提高化合物安全性、有效性和耐受性，并增加给药的便捷性。
（2）提高口服生物利用度。氘代化合物或能够减少肠壁和肝脏中不需要的代谢 (首过代谢) 程度，使得更大比例的未代谢药物到达作用的目标位置。生物利用度高决定其在低剂量下具有活性以及更好的耐受性。
（3）改善代谢特征。氘代化合物或能够减少有毒或反应性代谢物的形成，改善药物代谢状况。
（4）改进药品安全性。氘代化合物或能够减少或消除药物化合物的不良副作用，具有安全性。
（5）保留治疗特性。氘代化合物有望保留和此前研究中氢类似物相似的生化效力和选择性。"
瑞禧生物 has not independently confirmed the accuracy of these methods. They are for reference only.
Deuruxolitinib 相关抗体:
Phospho-JAK2 (Tyr1007/1008) Antibody
JAK1 Antibody (YA722)
JAK1 Antibody
JAK2 Antibody (YA721)
Phospho-JAK2 (Tyr1007+Tyr1008) Antibody
JAK2 Antibody (YA330)
Phospho-JNK (Thr183) Antibody
JAK3 Antibody (YA2466)
Clinical Trial
NCT NumberSponsorConditionStart DatePhaseNCT03811912Concert PharmaceuticalsAlopecia AreataMarch 21, 2019Phase 2NCT05041803Concert PharmaceuticalsAlopecia AreataOctober 19, 2021Phase 3NCT05467696Concert PharmaceuticalsHealth VolunteersJune 14, 2022Phase 1 NCT03898479Concert PharmaceuticalsAlopecia AreataApril 4, 2019Phase 2|Phase 3NCT04797650Concert PharmaceuticalsAlopecia AreataJune 10, 2021Phase 3NCT04843540Concert PharmaceuticalsHealthy VolunteersMay 19, 2021Phase 1NCT03137381Concert PharmaceuticalsAlopecia AreataAugust 9, 2017Phase 2NCT05478772Concert PharmaceuticalsHealth VolunteersJuly 11, 2022Phase 1NCT05468749Concert PharmaceuticalsRenal ImpairmentJune 6, 2022Phase 1NCT03880136Concert PharmaceuticalsHealthyMarch 25, 2019Phase 1NCT02777008Concert PharmaceuticalsHealthyMay 2016Phase 1NCT05467722Concert PharmaceuticalsHepatic ImpairmentJune 1, 2022Phase 1NCT05467709Concert PharmaceuticalsHealth VolunteersJune 21, 2022Phase 1NCT04309643Concert Pharmaceuticals|CelerionHealthy VolunteersJune 9, 2020Phase 1NCT04518995Concert PharmaceuticalsAlopecia AreataNovember 23, 2020Phase 3NCT03941548Concert PharmaceuticalsAlopecia AreataMay 24, 2019Phase 2NCT04784533Concert PharmaceuticalsAlopecia AreataFebruary 26, 2021Phase 2NCT04743414Concert PharmaceuticalsHealthy VolunteersMarch 2, 2021Phase 1NCT05192369Concert PharmaceuticalsHealthy VolunteersJanuary 4, 2022Phase 1
分子量：314.41
Formula：C17H10D8N6
CAS 号：1513883-39-0
非标记 CAS：941678-49-5
性状：固体
颜色：White to off-white
中文名称：鲁索利替尼 d8
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，-20°C：1 month