化合物 BMS-066|T14669|TargetMol

價(jià)格	￥17200	￥29500	￥22800
包裝	25mg	100mg	50mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-02

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產(chǎn)品詳情

中文名稱(chēng):化合物 BMS-066	英文名稱(chēng):BMS-066
CAS:914946-88-6	品牌: TargetMol
產(chǎn)地: 美國(guó)	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(lèi)別: 抑制劑
貨號(hào): T14669

Product Introduction

Bioactivity

名稱(chēng)	BMS-066
描述	BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor. With IC50s of 9 nM and 72 nM, respectively.
體外活性	BMS-066 is shown to inhibit IKKβ-catalyzed phosphorylation of IKKβ in vitro with an IC50 of 9 nM and is more than 500-fold selective for IKKβ over the closely related IKKα. For the six kinases showing more than 75% inhibition at 10 μM, IC50 values are determined in dose-response assays and BMS-066 is shown to be more than 30-fold selective against even the next most potently inhibits kinase (Brk). BMS-066 shows IC50 values of 72 and 1020 nM against the Tyk2 pseudokinase domain probe displacement and IL-23-stimulated reporter assays, respectively[2]. To understand the selectivity on a more comprehensive scale, BMS-066 is assayed against 155 additional kinases at 10 μM, and only six of these kinases are inhibited more than 75%. This indicates that BMS-066 is more than 400-fold selective for IKKβ over more than 95% of the kinases tested. BMS-066 inhibits LPS-stimulated cytokine production in human peripheral blood mononuclear cells, both at the protein and message level, with IC50 values of approximately 200 nM against these endpoints and it also inhibits the IKKβ-catalyzed phosphorylation of IkBα in LPS stimulated cells with a similar IC50 value[1].
體內(nèi)活性	Clear reduction of inflammation is also evident in the low dose of BMS-066 (5 mg/kg) and the bone resorption seems to be more focal and less severe compared with the control. The joints from animals receiving 10 mg/kg BMS-066 are normal or show minimal changes in both inflammation and bone resorption. Bone density measurements also show a clear dose-dependent benefit of treatment with BMS-066. Microcomputed tomography of the hind limbs also show that BMS-066 provides a dose-dependent protection against the pitting, loss of bone mass, woven porous bone, and fusion of the small bones evident in the rats. Serum drug level measurements in satellite animals on the first day of dosing show that a single dose provides coverage for approximately 3 h (6 h daily with twice daily dosing) of the mouse whole-blood IC50 value against LPS-induced TNF-α. It is also showed that IKKβ inhibitors suppress TNF-α and IL-1β production within these tissues in experimental arthritis model[1].
存儲(chǔ)條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
關(guān)鍵字	BMS-066 \| BMS 066 \| BMS066
相關(guān)產(chǎn)品	Deucravacitinib \| GSK8612 \| Gefitinib \| Amlexanox \| Ruxolitinib \| Malachite green oxalate \| Resveratrol \| Allicin \| Baricitinib \| GSK 3 Inhibitor IX \| Ibrutinib \| Delgocitinib

關(guān)鍵字： BMS-066|TargetMol

公司簡(jiǎn)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(zhuān)業(yè)的產(chǎn)品和服務(wù)。TargetMol?品牌的客戶群分布于40多個(gè)國(guó)家和地區(qū)，已發(fā)展成為全球知名的化合物庫(kù)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(kù)，以及多種類(lèi)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(lèi)多肽、抗體、生命科學(xué)試劑盒等，此外，我們還建設(shè)有CADD（計(jì)算機(jī)輔助藥物設(shè)計(jì)）研究中心、藥理實(shí)驗(yàn)室、藥化合成平臺(tái)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(zhuān)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(cè)資本	589.8595萬(wàn)人民幣
員工人數(shù)	100-500人	年?duì)I業(yè)額	￥ 1億以上
主營(yíng)行業(yè)	中間體,天然產(chǎn)物,生物化工,化學(xué)試劑,生物技術(shù)服務(wù)	經(jīng)營(yíng)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(cè)資本：589.8595萬(wàn)人民幣
企業(yè)類(lèi)型：有限責(zé)任公司(自然人投資或控股)
主營(yíng)產(chǎn)品：抑制劑&激動(dòng)劑，天然產(chǎn)物，重組蛋白，化合物庫(kù)，技術(shù)服務(wù)
公司地址：上海市靜安區(qū)江場(chǎng)三路238號(hào)8樓

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