目录:MedChemExpress LLC>>生化试剂>> XL01126 | MCE
| 纯度 | 99.81% | 分子量 | 1019.69 |
|---|---|---|---|
| 分子式 | C₅₀H₆₄ClFN₁₀O₆S₂ | 供货周期 | 现货 |
| 货号 | HY-148030 | 应用领域 | 医疗卫生,化工,生物产业,制药/生物制药 |
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CAS No. :
产品活性：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.
研究领域：PROTAC | Autophagy
作用靶点：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 |
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