1. PROTAC
    Autophagy
  2. PROTACs
    LRRK2
  3. XL01126

XL01126 

Cat. No.: HY-148030 Purity: 99.81%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

XL01126 Chemical Structure

XL01126 Chemical Structure

Size Price Stock Quantity
1 mg USD 850 In-stock
Estimated Time of Arrival: December 31
5 mg USD 1850 In-stock
Estimated Time of Arrival: December 31
10 mg USD 2950 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

IC50 & Target

DC50: 15-72 nM (LRRK2)[1]

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[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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: G2019S LRRK2 MEFs (mouse embryonic fibroblasts)
Concentration: 300 nM
Incubation Time: 4 hours
Result: Resulted LRRK2 pSer935, Rab10 pThr73 decrease.
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[1].
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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

1019.69

Formula

C50H64ClFN10O6S2

SMILES

O=C([[email protected]]1N(C([[email protected]@H](NC(C2(F)CC2)=O)C(C)(SC[[email protected]@H]3CC[[email protected]@H](CN4CCN(C(C5=CC=C(NC6=NC=C(Cl)C(NC)=N6)C(OC)=C5)=O)CC4)CC3)C)=O)C[[email protected]](O)C1)NCC7=CC=C(C8=C(C)N=CS8)C=C7

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (98.07 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9807 mL 4.9035 mL 9.8069 mL
5 mM 0.1961 mL 0.9807 mL 1.9614 mL
10 mM 0.0981 mL 0.4903 mL 0.9807 mL
*Please refer to the solubility information to select the appropriate solvent.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
XL01126
Cat. No.:
HY-148030
Quantity:
MCE Japan Authorized Agent: