XL01126
Based on 1 Customer Validation
XL01126 is a potent LRRK2 PROTAC (DC50: 14 nM (G2019S LRRK2) and 32 nM (WT LRRK2)). XL01126 crosses the blood-brain barrier and is used as a degradation probe in Parkinson's disease research. XL01126 can be used to study the non-catalytic and framework functions of LRRK2.
For research use only. We do not sell to patients.
- Purity: 98.90%
- CAS No.: 3011029-58-3
- Formula: C50H64ClFN10O6S2
- Molecular Weight:1019.69
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
DC50: 15-72 nM (LRRK2)[1]
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[1].
XL01126 (10, 30, 100 nM; 24 h) increases mitophagy in immortalized mouse embryonic fibroblasts cells[1].
XL01126 (10 μM; 90 min) displays high permeability in Caco-2 cells[1].
XL01126 (10 μM; 0-60 min; every 15 min interval gradient) exhibits high stability in mouse plasma, liver microsome and hepatocyte[1].
Pharmacokinetic of XL01126 in vitro[1]
| 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 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:G2019S LRRK2 MEFs (mouse embryonic fibroblasts)
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Concentration:300 nM
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Incubation Time:4 hours
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Result:Resulted LRRK2 pSer935, Rab10 pThr73 decrease.
Pharmacokinetic property of XL01126 in mice[1]
| 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 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3011029-58-3
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Appearance Solid
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Molecular Weight 1019.69
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Formula C50H64ClFN10O6S2
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Color White to off-white
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SMILES
O=C([C@H]1N(C([C@@H](NC(C2(F)CC2)=O)C(C)(SC[C@@H]3CC[C@@H](CN4CCN(C(C5=CC=C(NC6=NC=C(Cl)C(NC)=N6)C(OC)=C5)=O)CC4)CC3)C)=O)C[C@H](O)C1)NCC7=CC=C(C8=C(C)N=CS8)C=C7
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : ≥ 100 mg/mL (98.07 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.9807 mL | 4.9035 mL | 9.8069 mL | 24.5173 mL |
| 5 mM | 0.1961 mL | 0.9807 mL | 1.9614 mL | 4.9035 mL | |
| 10 mM | 0.0981 mL | 0.4903 mL | 0.9807 mL | 2.4517 mL | |
| 15 mM | 0.0654 mL | 0.3269 mL | 0.6538 mL | 1.6345 mL | |
| 20 mM | 0.0490 mL | 0.2452 mL | 0.4903 mL | 1.2259 mL | |
| 25 mM | 0.0392 mL | 0.1961 mL | 0.3923 mL | 0.9807 mL | |
| 30 mM | 0.0327 mL | 0.1634 mL | 0.3269 mL | 0.8172 mL | |
| 40 mM | 0.0245 mL | 0.1226 mL | 0.2452 mL | 0.6129 mL | |
| 50 mM | 0.0196 mL | 0.0981 mL | 0.1961 mL | 0.4903 mL | |
| 60 mM | 0.0163 mL | 0.0817 mL | 0.1634 mL | 0.4086 mL | |
| 80 mM | 0.0123 mL | 0.0613 mL | 0.1226 mL | 0.3065 mL |
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