Tyk2-IN-4 (BMS-986165) (Synonyms: BMS-986165) |
| رقم الكتالوجGC31659 |
Tyk2-IN-4 (BMS-986165) (BMS-986165) هو مثبط TYK2 انتقائي للغاية ومتوفر بيولوجيًا عن طريق الفم لعلاج أمراض المناعة الذاتية ، والذي يرتبط بشكل انتقائي بمجال TYK2 pseudokinase (JH2) (IC50 = 1.0 نانومتر) والكتل تنشيط Tyk2 بوساطة مستقبلات عن طريق تثبيت مجال JH2 التنظيمي.
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Cas No.: 1609392-27-9
Sample solution is provided at 25 µL, 10mM.
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Tyk2-IN-4 is a selective, potent, allosteric inhibitor of tyrosine kinase 2 (Tyk2).
Tyk2-IN-4 blocks receptor-mediated Tyk2 activation by stabilizing the regulatory pseudokinase domain of the protein[1].
Lupus-like disease is strongly inhibited in NZB/W mice treated with Tyk2-IN-4. Tyk2-IN-4 is safe and overall well-tolerated. There are no serious adverse events and the frequency of non-serious adverse events are similar in the active (75%) and placebo (76%) groups. After oral administration, Tyk2-IN-4 is rapidly absorbed and exhibits an apparent elimination half-life of 8-15 hours[1].
[1]. I Catlett, et al. SAT0226 A first-in-human, study of BMS-986165, a selective, potent, allosteric small molecule inhibitor of tyrosine kinase 2.
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