MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)。

GIBH-130

CAS No. : 1252608-59-5

產(chǎn)品活性：GIBH-130 is an effective inhibitor of neuroinflammation. GIBH-130 significantly suppresses the IL-1β secretion by activated microglia (IC₅₀=3.4 nM).

研究領(lǐng)域：Immunology/Inflammation

作用靶點(diǎn)：Interleukin Related

In Vitro: GIBH-130 is a novel antineuroinflammatory agent that is identified through microglia-based phenotypic screenings. GIBH-130 (IC₅₀ 3.4 nM) is identified in screenings as one of the most effective inhibitors with an acceptable half-life. Pretreatment of microglia with GIBH-130 significantly reduces the production of these factors in response to Lipopolysaccharides (LPS) stimulation, and the extent of the reduction is dependent on the concentrations of GIBH-130. The IC₅₀ values of GIBH-130 for NO and TNF-α inhibition are 46.24 and 40.82 μM, respectively. Notably, pretreatment with GIBH-130 significantly suppresses the IL-1β secretion by activated microglia (IC₅₀=3.4 nM). The inhibitory efficiency of GIBH-130 at 20 nM is comparable to 20 μM minocycline against IL-1β release. IL-1β is one of the major cytokines during neuroinflammatory progression of AD. So, it is meaningful to explain the selectivity of GIBH-130 against IL-1β (IC₅₀ value 3.4 nM) over NO and TNF-α (IC₅₀ value 46.24 and 40.82 μM, respectively) .

In Vivo: GIBH-130 exhibits comparable in vivo efficacy of cognitive impairment relief to donepezil and memantine respectively in both β amyloid-induced and APP/PS1 double transgenic Alzheimer’s murine models at a substantially lower dose (0.25 mg/kg). The pharmacokinetic properties of GIBH-130 are assessed in Sprague-Dawley rats. As a potential drug candidate targeting in CNS, GIBH-130 is found to be orally bioavailable in rats, with 74.91% bioavailability and 4.32 h half-life. In addition, GIBH-130 displays good penetration ability across blood-brain barrier (AUCBrain/Plasma=0.21).

相關(guān)產(chǎn)品：Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  Differentiation Inducing Compound Library  |  Pyroptosis Compound Library  |  Anti-Alzheimer's Disease Compound Library  |  Angiogenesis-Related Compound Library  |  Targeted Diversity Library  |  Antidepressant Compound Library  |  Heterocyclic Compound Library  |  Pain-Related Compound Library  |  RCGD423  |  Vunakizumab  |  Tagraxofusp  |  Dupilumab  |  IL-17A modulator-2  |  Daclizumab  |  PNRI-299  |  Izokibep  |  Ginsenoside F3  |  Broussonin E  |  Clerodendrin  |  Vudalimab  |  1,4-Dicaffeoylquinic acid  |  Cetrelimab  |  Hydrangenol  |  Mulberroside A  |  Oxelumab  |  Sirukumab  |  Y13g  |  Ginsenoside Rc  |  BIRT 377  |  Ixekizumab  |  IL-17 modulator 3  |  Ligufalimab  |  IL-17A modulator-3  |  Armillarisin A  |  Ustekinumab  |  Kansuinine B  |  VGX-1027  |  RO2959 hydrochloride

熱門產(chǎn)品線：重組蛋白  |  化合物庫(kù)  |  天然產(chǎn)物  |  熒光染料  |  PROTAC  |  同位素標(biāo)記物  |  寡核苷酸  |  抗體  |  點(diǎn)擊化學(xué)

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry

品牌介紹:
•   MCE (MedChemExpress) 擁有200 多種全球僅有化合物庫(kù)，我們致力于為全球科研客戶提供前沿的高品質(zhì)小分子活性化合物；
•   50,000 多種高選擇性抑制劑、激動(dòng)劑涉及各熱門信號(hào)通路及疾病領(lǐng)；
•   產(chǎn)品種類涵蓋各種重組蛋白，多肽，常用試劑盒 ，更有 PROTAC、ADC 等特色產(chǎn)品，廣泛應(yīng)用于新藥研發(fā)、生命科學(xué)等科研項(xiàng)目；
•   提供虛擬篩選，離子通道篩選，代謝組學(xué)分析檢測(cè)分析，藥物篩選等專業(yè)技術(shù)服務(wù)；
•   設(shè)有專業(yè)的實(shí)驗(yàn)中心和嚴(yán)格的質(zhì)控、驗(yàn)證體系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各項(xiàng)質(zhì)檢報(bào)告，確保產(chǎn)品的高純度、高品質(zhì)；
•   產(chǎn)品的生物活性多經(jīng)各國(guó)客戶實(shí)驗(yàn)驗(yàn)證；
•   Nature, Cell, Science 等多種頂級(jí)期刊及制藥 Patent 收錄了MCE客戶的科研成果；
•   專業(yè)團(tuán)隊(duì)跟蹤最新的制藥及生命科學(xué)研究進(jìn)展，為您提供全球新的活性化合物；
•   與世界各大制藥公司及著名科研機(jī)構(gòu)建立了長(zhǎng)期的合作。