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| Targets |
EB-42486 targets G2019S-LRRK2, a mutant form of leucine-rich repeat kinase 2 that is associated with Parkinson's disease and other disorders. LRRK2 is a large multidomain protein kinase involved in various cellular processes including vesicle trafficking, autophagy, and mitochondrial function. The G2019S mutation increases LRRK2 kinase activity and is the most common genetic cause of familial Parkinson's disease. Inhibition of G2019S-LRRK2 by EB-42486 holds therapeutic potential for Parkinson's disease and other conditions.
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| ln Vitro |
EB-42486 demonstrates potent in vitro activity as a G2019S-LRRK2 inhibitor with an IC50 < 0.2 nM. The compound is a novel, potent, and highly selective inhibitor. Its activity is typically assessed in kinase inhibition assays using purified LRRK2 enzyme or cellular assays measuring LRRK2 autophosphorylation and downstream substrate phosphorylation. The compound's high potency and selectivity make it a valuable tool for studying LRRK2 biology and Parkinson's disease mechanisms.
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| ln Vivo |
In vivo studies for EB-42486 have not been extensively documented in the available literature. As a potent and selective G2019S-LRRK2 inhibitor, it has potential for in vivo applications in Parkinson's disease and other disorders. Studies in appropriate animal models of LRRK2-related diseases would be needed to evaluate its in vivo efficacy, pharmacokinetics, and safety profile. The compound's small molecule properties suggest potential for oral bioavailability and brain penetration.
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| Enzyme Assay |
For kinase inhibition assays, EB-42486 is tested against G2019S-LRRK2 and wild-type LRRK2 at various concentrations. Kinase activity is measured using radiometric (33P-ATP incorporation) or fluorescence-based (TR-FRET) methods with appropriate peptide substrates. IC50 values are calculated from dose-response curves. Selectivity profiling is conducted by screening the compound against a panel of related kinases to assess specificity for G2019S-LRRK2.
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| Cell Assay |
For cellular studies, appropriate cell lines or primary neurons expressing G2019S-LRRK2 are cultured and treated with EB-42486 at various concentrations. LRRK2 kinase activity is assessed by measuring phosphorylation of LRRK2 substrates (e.g., Rab10, Rab12) by Western blot using phospho-specific antibodies. Cell viability and cytotoxicity are assessed using MTT or similar assays. Neuronal health and morphology may be evaluated in neuronal cultures.
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| Animal Protocol |
For in vivo efficacy studies, appropriate animal models of LRRK2-related diseases would be used. EB-42486 would be administered via oral or intraperitoneal routes at various doses. LRRK2 kinase activity in brain tissues would be assessed by measuring substrate phosphorylation. Behavioral and motor function tests would be conducted in Parkinson's disease models. Pharmacokinetic parameters including half-life, clearance, and brain penetration would be determined.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of EB-42486 have not been fully characterized in the available literature. The compound has a molecular formula of C22H22N8O and a molecular weight of 414.46. Purity is 99%. It is soluble in DMSO at ≥100 mg/mL. Powder should be stored at -20°C for 3 years or 4°C for 2 years. In solvent, it is stable for 6 months at -80°C or 1 month at -20°C.
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| Toxicity/Toxicokinetics |
EB-42486 is a research compound intended for laboratory use only and is not approved for human therapeutic use. As a potent and selective G2019S-LRRK2 inhibitor with IC50 < 0.2 nM, it holds therapeutic potential for Parkinson's disease and other conditions. Standard laboratory safety precautions should be followed when handling this compound. Storage at -20°C or 4°C is recommended.
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| References | |
| Additional Infomation |
EB-42486 is a novel, potent, and highly selective inhibitor of G2019S-LRRK2 with IC50 < 0.2 nM, molecular formula C22H22N8O, and molecular weight 414.46. The compound holds therapeutic potential for Parkinson's disease and other conditions driven by LRRK2 dysregulation. It is for research use only and has not been approved for clinical applications. Purity 99% and storage at -20°C or 4°C is recommended.
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| Molecular Formula |
C22H22N8O
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| Molecular Weight |
414.46
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| Exact Mass |
414.191
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| CAS # |
2390475-81-5
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| PubChem CID |
155925851
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
2.9
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
31
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| Complexity |
733
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C12=NN=NN1C(C)(C)C(C(NC1C=CC3=C(C=1)C(C1=CC=CC=C1)=NN3)=O)=C(C)N2C
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| InChi Key |
KHSAHYKLUPESPP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H22N8O/c1-13-18(22(2,3)30-21(29(13)4)26-27-28-30)20(31)23-15-10-11-17-16(12-15)19(25-24-17)14-8-6-5-7-9-14/h5-12H,1-4H3,(H,23,31)(H,24,25)
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| Chemical Name |
4,5,7,7-tetramethyl-N-(3-phenyl-1H-indazol-5-yl)tetrazolo[1,5-a]pyrimidine-6-carboxamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 125 mg/mL (301.60 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.02 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (5.02 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.02 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4128 mL | 12.0639 mL | 24.1278 mL | |
| 5 mM | 0.4826 mL | 2.4128 mL | 4.8256 mL | |
| 10 mM | 0.2413 mL | 1.2064 mL | 2.4128 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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