目錄:MedChemExpress LLC>>生化試劑>> XL01126 | MCE
| 純度 | 99.81% | 分子量 | 1019.69 |
|---|---|---|---|
| 分子式 | C??H??ClFN??O?S? | 供貨周期 | 現(xiàn)貨 |
| 貨號 | HY-148030 | 應(yīng)用領(lǐng)域 | 醫(yī)療衛(wèi)生,化工,生物產(chǎn)業(yè),制藥/生物制藥 |
MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報，我們不為任何個人用途提供產(chǎn)品和服務(wù)。
CAS No. :
產(chǎn)品活性：XL01126 is a potent degrader of LRRK2 with DC50s of 14 nM (G2019S LRRK2) and 32 nM (WT LRRK2), respectively. XL01126 can cross blood-brain barrier and be used as a degrader probe in Parkinson’s disease research. XL01126 exerts function of study of non-catalytic and scaffolding functions of LRRK2.
研究領(lǐng)域：PROTAC | Autophagy
作用靶點：PROTACs | LRRK2
In Vitro: XL01126 (300 nM; 4 h) exhibits strong degradation performance by forming a positively cooperative ternary complex with E3 ubiquitin ligase ligand VHL and target protein LRRK2.
XL01126 (10, 30, 100 nM; 24 h) increases mitophagy in immortalized mouse embryonic fibroblasts cells.
XL01126 (10 μM; 90 min) displays high permeability in Caco-2 cells.
XL01126 (10 μM; 0-60 min; every 15 min interval gradient) exhibits high stability in mouse plasma, liver microsome and hepatocyte.
Pharmacokinetic of XL01126 in vitro
| Parameter | Properties |
| T1/2 in mouse plasma | 108.29 min |
| T1/2 in mouse liver microsome | 3.65 min |
| Clint in mouse liver microsome | 1494.62 mL/min/kg |
| T1/2 in mose hepatocytes | 314.33 min |
| Clint in mose hepatocytes | 26.04 mL/min/kg |
In Vivo: XL01126 (30 mg/kg; p.o.; single dose) shows oral activity with bioavailable value (F) of 15% and can penetrate the blood brain barrier after either oral or parenteral dosing in mice.
Pharmacokinetic property of XL01126 in mice
| Route | Dose (mg/kg) | CL (L/h/kg) | Vss (L/kg) | Tmax (h) | Cmax (ng/mL) | T1/2 (h) | AUClast (h·ng/mL) | AUCinf (h·ng/mL) | MRT (h) | F (%) |
| p.o. | 30 | 2 | 3620 | 21.9 | 21337 | 109271 | 15 | |||
| i.v. | 5 | 0.208 | 0.511 | 1.52 | 23663 | 23981 | 2.45 | |||
| i.p. | 30 | 0.25 | 7700 | 5.2 | 41434 | 64068 | 29.2 |
相關(guān)產(chǎn)品：Bioactive Compound Library Plus | LC-2 | ACBI2 | iRucaparib-AP6 | BSJ-04-132 | PROTAC VEGFR-2 degrader-1 | CZC-54252 hydrochloride | SR-1114 | PROTAC CRABP-II Degrader-3 | PROTAC Sirt2 Degrader-1 | CRBN-6-5-5-VHL | PROTAC BRD2/BRD4 degrader-1 | BSJ-03-204 | JPS016 | KB02-JQ1 | TD-802 | BSJ-03-123 | PROTAC RIPK degrader-6 | VZ185 | PROTAC BRD9 Degrader-4 | MS5033 | PZ703b TFA | PROTAC FKBP Degrader-3 | MS9449 | SB1-G-187 | PFE-360 | PROTAC CDK2/9 Degrader-1 | MD-224 | di-Ellipticine-RIBOTAC | PROTAC CRABP-II Degrader-2 | CCT367766
熱門產(chǎn)品線：重組蛋白 | 化合物庫 | 天然產(chǎn)物 | 熒光染料 | PROTAC | 同位素標記物 | 寡核苷酸 | 抗體 | 點擊化學(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*僅有化合物庫，我們致力于為*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、激動劑涉及各熱門信號通路及疾病領(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)等科研項目；
• 提供虛擬篩選，離子通道篩選，代謝組學(xué)分析檢測分析，藥物篩選等專業(yè)技術(shù)服務(wù)；
• 設(shè)有專業(yè)的實驗中心和嚴格的質(zhì)控、驗證體系；
• 提供 LC/MS、NMR、HPLC、手性分析、元素分析等各項質(zhì)檢報告，確保產(chǎn)品的高純度、高品質(zhì)；
• 產(chǎn)品的生物活性多經(jīng)各國客戶實驗驗證；
• Nature, Cell, Science 等多種頂級期刊及制藥 Patent 收錄了MCE客戶的科研成果；
• 專業(yè)團隊跟蹤新的制藥及生命科學(xué)研究進展，為您提供*新的活性化合物；
• 與世界各大制藥公司及*科研機構(gòu)建立了長期的合作。
4
化工儀器網(wǎng)