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Elsubrutinib

CAS No. : 1643570-24-4

MCE 站：Elsubrutinib

产品活性：Elsubrutinib (ABBV-105) 是一种具有口服活性、有效的、有选择性和不可逆的 Bruton＇s tyrosine kinase (BTK) 抑制剂。Elsubrutinib 对 BTK 催化结构域的 IC₅₀ 为 0.18 μM。Elsubrutinib 可用于炎症性疾病的研究。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：Btk

In Vitro: Elsubrutinib inhibits BTK (C481S) with an IC₅₀ of 2.6 μM, indicating a significant loss in potency upon exchanging the targeted thiol nucleophile with an alcohol, suggesting Cys481 is important in the manner in which Elsubrutinib inhibits BTK. Elsubrutinib irreversibly inhibits BTK enzyme activity ａnd blocks BTK-dependent cellular activation. Elsubrutinib inhibits histamine release from IgE-stimulated basophils ａnd IL-6 release from IgG-stimulated monocytes, which utilize Fce ａnd Fcc receptors respectively. Elsubrutinib inhibits IgM-mediated B cell proliferation, which is dependent on signaling through the BCR. Elsubrutinib also inhibits TNF-release from CpG-DNA stimulated PBMCs, which signals through TLR9, although it does not inhibit the function of TLRs that do not use ITAM motifs, namely, TNF release from PBMCs stimulated either through TLR4 (with LPS) or through TLR7/8 (with R848). Elsubrutinib has significant impacts on IgM-mediated B cell proliferation.

In Vivo: Elsubrutinib (10 mg/kg; p.o.) inhibits antibody responses to NP-Ficoll ａnd NP-KLH, but not to NP-LPS or Prevnar-13.
Elsubrutinib (0.1~10 mg/kg; p.o.) results in dose-dependent inhibition of paw swelling throughout the course of disease ａnd significantly prevents the onset of proteinuria ａnd prolongs survival at the 10 mg/kg QD ａnd BID doses, while lower doses does not significantly inhibit these endpoints.
Elsubrutinib demonstrates exposure-dependent inhibition of increases in paw volume. Elsubrutinib significantly inhibits bone volume loss in a dose dependent manner consistent with the observed anti-inflammatory effects.

相关产品：Ibrutinib  |  Acalabrutinib  |  Zanubrutinib  |  Fenebrutinib  |  ARQ 531  |  Pirtobrutinib  |  Tirabrutinib  |  Orelabrutinib  |  Spebrutinib  |  Vecabrutinib  |  BMX-IN-1  |  Rilzabrutinib  |  Ibrutinib-biotin  |  MT-802  |  CGI-1746  |  Remibrutinib  |  Tolebrutinib  |  Branebrutinib  |  SJF620  |  Ibrutinib deacryloylpiperidine  |  LFM-A13  |  PCI-33380  |  QL47  |  Poseltinib  |  BIIB068  |  GDC-0834  |  CNX-500

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