SC-919
Based on 1 Customer Validation
SC-919 is an orally active IP6K inhibitor, with an IC50 of < 5.2 nM against IP6K1, < 3.8 nM against IP6K2, and 0.65 nM against IP6K3. By inhibiting the activity of IP6K, SC-919 reduces intracellular IP7 levels, thereby suppressing XPR1-mediated cellular phosphate efflux. SC-919 increases intracellular phosphate and ATP levels while reducing phosphate entry into the bloodstream, thus decreasing plasma phosphate levels. SC-919 can be used in research related to chronic kidney disease and hyperphosphatemia.
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- Pureza: 98.68%
- No. CAS: 2245949-62-4
- Fòrmula: C19H16Cl2N2O4
- Peso molecular:407.25
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
Actividad biológica
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IP6K1 |
SC-919 (0.001-1 μM; 4 h) dose-dependently inhibits phosphate efflux and promotes phosphate uptake in HEK293 cells, accompanied by decreased InsP7 levels[1].
SC-919 (0.001-1 μM; 1-4 h) increases intracellular ATP levels in HEK293 cells in a dose-dependent manner within 1-4 h[1].
SC-919 (0.1-1 μM; 4 h) increases the incorporation of 32P-phosphate in HEK293 cells and exogenous 32P-phosphate outside cells into ATP[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
SC-919 (0.3-3 mg/kg; p.o.; single dose) significantly decreases plasma phosphate levels in normal male cynomolgus monkeys[1].
SC-919 (10 mg/kg; p.o.; single dose; once daily for 7 days) does not significantly alter faecal phosphate excretion but reduces urinary phosphate excretion in normal male Sprague-Dawley rats[1].
SC-919 (1-10 mg/kg; p.o.; single dose; once daily for 7 days) effectively and sustainably decreases plasma phosphate levels in adenine-induced hyperphosphataemic male Sprague-Dawley rats[1].
SC-919 (0.3-1 mg/kg; p.o.; single dose) decreases plasma phosphate levels in bilaterally nephrectomized hyperphosphataemic male Sprague-Dawley rats[1].
SC-919 (1-10 mg/kg; p.o.; once daily for 5 weeks) alleviates hyperphosphataemia, improves kidney function, reduces vascular calcification, and reverses weight loss in adenine-induced chronic kidney disease male Sprague-Dawley rats[1].
SC-919 (1-10 mg/kg; p.o.; once daily for 8 days) increases kidney ATP levels in adenine-induced chronic kidney disease male Sprague-Dawley rats[1].
SC-919 (0.3-10 mg/kg; p.o.; single dose) dose-dependently decreases InsP7 levels in liver, skeletal muscle, and kidney tissue of normal male Sprague-Dawley rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (SD) (8-week-old male)[1]
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Dosage:1 mg/kg; 3 mg/kg; 10 mg/kg
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Administration:p.o.; single dose
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Result:Increased plasma SC-919 concentrations in a dose-dependent manner.
Decreased plasma phosphate levels in a dose-dependent manner compared to vehicle control.
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Animal Model:cynomolgus monkeys (3-4-year-old male, 2.6-4.7 kg)[1]
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Dosage:0.3 mg/kg; 3 mg/kg
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Administration:p.o.; single dose
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Result:Lowered plasma phosphate levels significantly compared to vehicle control.
Increased plasma SC-919 concentrations in a dose-dependent manner.
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Animal Model:Sprague-Dawley (SD) (8-week-old male)[1]
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Dosage:10 mg/kg
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Administration:p.o.; single dose; once daily for 7 days
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Result:Showed a non-significant slight increase in cumulative ^32P activity in faeces compared to vehicle control.
Lowered cumulative ^32P activity in urine compared to vehicle control, consistent with decreased plasma phosphate levels.
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Animal Model:Sprague-Dawley (SD) (13-week-old male, adenine-induced chronic kidney disease-related hyperphosphataemia)[1]
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Dosage:1 mg/kg; 10 mg/kg
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Administration:p.o.; once daily for 7 days
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Result:Decreased plasma phosphate levels effectively after a single oral dose.
Reduced plasma phosphate levels sustainably after 7 days of daily dosing.
Increased plasma SC-919 concentrations in a dose-dependent manner.
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Animal Model:Sprague-Dawley (SD) (9-week-old male, bilateral nephrectomy-induced hyperphosphataemia)[1]
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Dosage:0.3 mg/kg; 1 mg/kg
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Administration:p.o.; single dose
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Result:Decreased plasma phosphate levels in bilaterally nephrectomized rats with hyperphosphataemia.
Increased plasma SC-919 concentrations in a dose-dependent manner.
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Animal Model:Sprague-Dawley (SD) (14-week-old male, adenine-induced chronic kidney disease with hyperphosphataemia)[1]
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Dosage:1 mg/kg; 10 mg/kg
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Administration:p.o.; once daily for 5 weeks
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Result:Increased daily food intake and body weight compared to vehicle control.
Decreased plasma levels of GDF15, FGF23, and intact PTH significantly compared to vehicle control.
Increased plasma 1,25(OH)2-D levels significantly compared to vehicle control.
Reduced plasma phosphate levels and calcium-phosphate product compared to vehicle control.
Decreased plasma creatinine levels compared to vehicle control.
Reduced aortic calcium content compared to vehicle control.
Increased renal Nphs2 and Cyp27b1 mRNA expression compared to vehicle control.
Decreased renal fibrotic area and collagen content compared to vehicle control.
Increased renal non-fibrotic area compared to vehicle control.
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Animal Model:Sprague-Dawley (SD) (14-week-old male, adenine-induced chronic kidney disease with hyperphosphataemia)[1]
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Dosage:1 mg/kg; 10 mg/kg
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Administration:p.o.; once daily for 8 days
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Result:Rescued kidney ATP levels in adenine-treated rats to near-normal levels compared to vehicle control.
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Animal Model:Sprague-Dawley (SD) (8-week-old male)[1]
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Dosage:0.3 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
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Administration:p.o.; single dose
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Result:Decreased InsP7 levels in liver, skeletal muscle, and kidney tissue in a dose-dependent manner compared to vehicle control.
Reduced InsP7 levels significantly at all tested doses compared to vehicle control.
Chemical Information
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No. CAS 2245949-62-4
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Appearance Solid
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Peso molecular 407.25
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Fòrmula C19H16Cl2N2O4
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Color White to off-white
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SMILES
O=C1[C@@]2(CC[C@@H](CC2)OC3=C(C=C(C=N3)Cl)Cl)C4=CC(C(O)=O)=CC=C4N1
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Synonyms
LI-2124
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 50 mg/mL (122.77 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. 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)
Pureza y Documentación
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Ficha de datos (283 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. 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 | 2.4555 mL | 12.2775 mL | 24.5549 mL | 61.3874 mL |
| 5 mM | 0.4911 mL | 2.4555 mL | 4.9110 mL | 12.2775 mL | |
| 10 mM | 0.2455 mL | 1.2277 mL | 2.4555 mL | 6.1387 mL | |
| 15 mM | 0.1637 mL | 0.8185 mL | 1.6370 mL | 4.0925 mL | |
| 20 mM | 0.1228 mL | 0.6139 mL | 1.2277 mL | 3.0694 mL | |
| 25 mM | 0.0982 mL | 0.4911 mL | 0.9822 mL | 2.4555 mL | |
| 30 mM | 0.0818 mL | 0.4092 mL | 0.8185 mL | 2.0462 mL | |
| 40 mM | 0.0614 mL | 0.3069 mL | 0.6139 mL | 1.5347 mL | |
| 50 mM | 0.0491 mL | 0.2455 mL | 0.4911 mL | 1.2277 mL | |
| 60 mM | 0.0409 mL | 0.2046 mL | 0.4092 mL | 1.0231 mL | |
| 80 mM | 0.0307 mL | 0.1535 mL | 0.3069 mL | 0.7673 mL | |
| 100 mM | 0.0246 mL | 0.1228 mL | 0.2455 mL | 0.6139 mL |
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