Elsubrutinib|T39130|TargetMol

價格	￥4190
包裝	2mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-09-30

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產(chǎn)品詳情

中文名稱:Elsubrutinib	英文名稱:Elsubrutinib
CAS:1643570-24-4	品牌: TargetMol
產(chǎn)地: 美國	保存條件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
產(chǎn)品類別: 抑制劑
貨號: T39130

Product Introduction

Bioactivity

名稱	Elsubrutinib
描述	Elsubrutinib (ABBV-105) is a highly active, potent, and selective orally-administered inhibitor of Bruton's tyrosine kinase (BTK). It irreversibly inhibits the catalytic domain of BTK with an IC50 value of 0.18 μM. Elsubrutinib holds potential for the advancement of research on inflammatory diseases.
體外活性	Elsubrutinib inhibits BTK (C481S) with an IC 50 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[1].
體內(nèi)活性	Elsubrutinib (10 mg/kg; p.o.) inhibits antibody responses to NP-Ficoll and NP-KLH, but not to NP-LPS or Prevnar-13[1]. 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[1]. 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[1]. Animal Model: Female C57/BL6 mice[1]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[1]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[1]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.
存儲條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
關(guān)鍵字	ABBV105 \| Elsubrutinib \| ABBV 105

關(guān)鍵字： ABBV-105|TargetMol

公司簡介

TargetMol Chemicals Inc. 總部位于馬薩諸塞州波士頓，致力于為全球生化領(lǐng)域科學(xué)家的研究提供專業(yè)的產(chǎn)品和服務(wù)。TargetMol?品牌的客戶群分布于40多個國家和地區(qū)，已發(fā)展成為全球知名的化合物庫和小分子化合物研究供應(yīng)商。 TargetMol?可提供160多種滿足不同需求的化合物庫，以及多種類型的生化試劑產(chǎn)品，包括12000多種抑制劑、16000多種天然產(chǎn)物和各類多肽、抗體、生命科學(xué)試劑盒等，此外，我們還建設(shè)有CADD（計算機輔助藥物設(shè)計）研究中心、藥理實驗室、藥化合成平臺三大技術(shù)中心，全方位滿足客戶的定制需求。憑借我們優(yōu)質(zhì)的產(chǎn)品和服務(wù)、快速高效的全球供應(yīng)鏈和專業(yè)的技術(shù)支持，我們將有效幫助您縮短研發(fā)周期，取得更成功的結(jié)果。

成立日期	2013-04-18 （12年）	注冊資本	566.265100萬人民幣
員工人數(shù)	100-500人	年營業(yè)額	￥ 1億以上
主營行業(yè)	天然產(chǎn)物,生化試劑,分子生物學(xué),分子砌塊,生物技術(shù)服務(wù)	經(jīng)營模式	貿(mào)易,工廠,試劑,定制,服務(wù)

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公司成立：12年
注冊資本：566.265100萬人民幣
企業(yè)類型：有限責(zé)任公司(自然人投資或控股)
主營產(chǎn)品：小分子抑制劑、藥物篩選化合物庫、藥物篩選等
公司地址：靜安區(qū)江場三路238號8樓

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