MK-1468
Based on 1 Customer Validation
MK-1468 is an orally active, selective, and BBB-permeable LRRK2 inhibitor. MK-1468 can be used for the research of Parkinson's disease.
For research use only. We do not sell to patients.
- Purity: 99.69%
- CAS No.: 2769107-89-1
- Formula: C26H33ClN4O4
- Molecular Weight:501.02
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Storage:Powder -20°C, 3 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
Biological Activity
MK-1468 has oral bioavailability in rats and dogs of 56% and 100%, respectively, and it is relatively low in rhesus monkeys of 9%[1].
MK-1468 (30-800 mg/kg; oral administration; 7-30 days) shows good tolerance in rhesus monkeys[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rhesus monkeys[2]
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Dosage:100, 200 and 800 mg/kg for 7 days;
30, 100 and 500 mg/kg b.i.d. for 30 days -
Administration:Oral administration (p.o.)
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Result:Caused sporadic emesis in male animals and led to increased hypertrophy of type 2 pneumocytes as well as an increase in intra-alveolar macrophages in the lungs at doses of 200 or 800 mg/kg/day in the 7-day administration experiment.
Caused no relevant clinical signs in the 30-day administration experiment. At doses of 100 or 500 mg/kg b.i.d., hypertrophy and hyperplasia of type 2 pneumocytes occurred, with thickening and deformation of alveolar walls and an increase in collagen. Some changes still persisted 12 weeks after drug withdrawal.
Chemical Information
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CAS No. 2769107-89-1
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Appearance Solid
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Molecular Weight 501.02
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Formula C26H33ClN4O4
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Color White to off-white
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SMILES
ClC(C(N1CCN([C@]2([C@H](COC2)O)C)CC1)=C3)=CC(C=N4)=C3C=C4NC([C@@H]5C6(CCOCC6)C5)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (199.59 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (272 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)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Kattar SD, et al. Discovery of MK-1468: A Potent, Kinome-Selective, Brain-Penetrant Amidoisoquinoline LRRK2 Inhibitor for the Potential Treatment of Parkinson's Disease. J Med Chem. 2023 Oct 20. [Content Brief]
[2]. Miller GK, et al. Effects of LRRK2 Inhibitors in Nonhuman Primates. Toxicol Pathol. 2023 Jul;51(5):232-245. [Content Brief]
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 | 1.9959 mL | 9.9796 mL | 19.9593 mL | 49.8982 mL |
| 5 mM | 0.3992 mL | 1.9959 mL | 3.9919 mL | 9.9796 mL | |
| 10 mM | 0.1996 mL | 0.9980 mL | 1.9959 mL | 4.9898 mL | |
| 15 mM | 0.1331 mL | 0.6653 mL | 1.3306 mL | 3.3265 mL | |
| 20 mM | 0.0998 mL | 0.4990 mL | 0.9980 mL | 2.4949 mL | |
| 25 mM | 0.0798 mL | 0.3992 mL | 0.7984 mL | 1.9959 mL | |
| 30 mM | 0.0665 mL | 0.3327 mL | 0.6653 mL | 1.6633 mL | |
| 40 mM | 0.0499 mL | 0.2495 mL | 0.4990 mL | 1.2475 mL | |
| 50 mM | 0.0399 mL | 0.1996 mL | 0.3992 mL | 0.9980 mL | |
| 60 mM | 0.0333 mL | 0.1663 mL | 0.3327 mL | 0.8316 mL | |
| 80 mM | 0.0249 mL | 0.1247 mL | 0.2495 mL | 0.6237 mL | |
| 100 mM | 0.0200 mL | 0.0998 mL | 0.1996 mL | 0.4990 mL |
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