Elsubrutinib ABBV-105|cas:1643570-24-4|西域试剂

Elsubrutinib ABBV-105,98.0%

产品编号：Bellancom-109143| CAS NO：1643570-24-4| 分子式：C₁₇H₁₉N₃O₂| 分子量：297.35

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-109143		￥6100.00	杭州北京（现货）
Bellancom-109143		￥9800.00	杭州北京（现货）

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Elsubrutinib ABBV-105

产品介绍

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。

生物活性

Elsubrutinib (ABBV-105) is an orally active, potent, selective and irreversible Bruton's tyrosine kinase (BTK) inhibitor。The IC₅₀ of Elsubrutinib for BTK catalytic domain is 0.18 μM. Elsubrutinib can be used for the research of inflammatory disease.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female C57/BL6 mice
Dosage:	10 mg/kg
Administration:	P.o.
Result:	Inhibited antibody responses to NP-Ficoll and NP-KLH, but not to NP-LPS or Prevnar-13.

Animal Model:	Lewis rats
Dosage:	0.1~10 mg/kg
Administration:	P.o.
Result:	Resulted in dose-dependent inhibition of paw swelling throughout the course of disease.

Animal Model:	NZBWF1 mice
Dosage:	0.1~10 mg/kg
Administration:	P.o.
Result:	Significantly prevented the onset of proteinuria and prolonged survival at the 10 mg/kg QD and BID doses, while lower doses did not significantly inhibit these endpoints.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female C57/BL6 mice
Dosage:	10 mg/kg
Administration:	P.o.
Result:	Inhibited antibody responses to NP-Ficoll and NP-KLH, but not to NP-LPS or Prevnar-13.

Animal Model:	Lewis rats
Dosage:	0.1~10 mg/kg
Administration:	P.o.
Result:	Resulted in dose-dependent inhibition of paw swelling throughout the course of disease.

Animal Model:	NZBWF1 mice
Dosage:	0.1~10 mg/kg
Administration:	P.o.
Result:	Significantly prevented the onset of proteinuria and prolonged survival at the 10 mg/kg QD and BID doses, while lower doses did not significantly inhibit these endpoints.