LSN3353871
Based on 1 Customer Validation
LSN3353871 is an orally active inhibitor of lipoprotein (a) (Lp (a)) formation, with Kd values of 756 nM (apo (a) KIV8), 605 nM (apo (a) KIV7-8), and 423 nM (apo (a) KIV5-8), respectively, and an IC50 of 1.69 μM against apo (a) KIV5-8. LSN3353871 reduces circulating Lp (a) levels in transgenic mice and cynomolgus monkeys. LSN3353871 can be used in the research of atherosclerotic cardiovascular disease and calcific aortic valve disease.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.62%
- No. CAS: 2565657-20-5
- Fòrmula: C13H18ClNO2
- Peso molecular:255.74
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Metabolism/Protease Compound Library
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Anti-Cardiovascular Disease Compound Library
HY-L046
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Orally Active Compound Library
HY-L061
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Metabolic Enzyme Compound Library
HY-L146
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
Actividad biológica
LSN3353871 selectively binds to apo(a) K(IV)8, K(IV)7-8, and K(IV)5-8 domains with Kd values of 756 nM, 605 nM, and 423 nM, respectively, and does not bind to apo(a) K(IV)2[1].
LSN3353871 (0.03-10 µM; 2 hours) inhibits in vitro Lp(a) assembly with an IC50 of 1.69 µM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
LSN3353871 (20-40 mg/kg; p.o.; twice daily/once daily; 14 days) reduces Lp(a) levels from baseline in cynomolgus monkeys, with a maximum median reduction of 40% at 20 mg/kg BID over 14 days[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:B6.SJL-Tg(APOB)1102Sgy Tg(Alb-LPA)32Arte (female, 7-17 months old)[1]
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Dosage:3 mg/kg; 10 mg/kg; 30 mg/kg; 100 mg/kg
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Administration:p.o.; twice daily; 5 days
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Result:Reduced steady-state Lp(a) levels by approximately 30% at 3 mg/kg, 40% at 10 mg/kg, 60% at 30 mg/kg, and 78% at 100 mg/kg.
Achieved a median effective dose (ED50) of 14 mg/kg twice daily.
Showed significant reductions at all doses.
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Animal Model:Macaca fascicularis (female, 2.0-5.0 kg)[1]
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Dosage:20 mg/kg (twice daily); 40 mg/kg (once daily)
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Administration:p.o.; twice daily (20 mg/kg); once daily (40 mg/kg); 14 days
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Result:Reduced median Lp(a) levels by up to 40% from baseline over 14 days at 20 mg/kg twice daily.
Reduced median Lp(a) levels by up to 25% from baseline over 14 days at 40 mg/kg once daily.
Showed significant reductions at day 14 for 20 mg/kg and 40 mg/kg doses.
Chemical Information
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No. CAS 2565657-20-5
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Appearance Solid
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Peso molecular 255.74
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Fòrmula C13H18ClNO2
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Color White to off-white
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SMILES
OC([C@@H](CC1=CC=CC=C1)[C@@H]2CNCC2)=O.Cl
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvente y solubilidad
DMSO : 125 mg/mL (488.78 mM; Need ultrasonic; 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
Pureza y Documentación
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Ficha de datos (274 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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Instrucciones de manejo (2659 KB)
Referencias
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 (sealed storage, away from moisture). 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 | 3.9102 mL | 19.5511 mL | 39.1022 mL | 97.7555 mL |
| 5 mM | 0.7820 mL | 3.9102 mL | 7.8204 mL | 19.5511 mL | |
| 10 mM | 0.3910 mL | 1.9551 mL | 3.9102 mL | 9.7756 mL | |
| 15 mM | 0.2607 mL | 1.3034 mL | 2.6068 mL | 6.5170 mL | |
| 20 mM | 0.1955 mL | 0.9776 mL | 1.9551 mL | 4.8878 mL | |
| 25 mM | 0.1564 mL | 0.7820 mL | 1.5641 mL | 3.9102 mL | |
| 30 mM | 0.1303 mL | 0.6517 mL | 1.3034 mL | 3.2585 mL | |
| 40 mM | 0.0978 mL | 0.4888 mL | 0.9776 mL | 2.4439 mL | |
| 50 mM | 0.0782 mL | 0.3910 mL | 0.7820 mL | 1.9551 mL | |
| 60 mM | 0.0652 mL | 0.3259 mL | 0.6517 mL | 1.6293 mL | |
| 80 mM | 0.0489 mL | 0.2444 mL | 0.4888 mL | 1.2219 mL | |
| 100 mM | 0.0391 mL | 0.1955 mL | 0.3910 mL | 0.9776 mL |
LSN3353871 Related Classifications
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