2. Metabolic Enzyme/Protease PI3K/Akt/mTOR
  3. IPK Superfamily
  4. SC-919

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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SC-919

SC-919 Chemical Structure

CAS No. : 2245949-62-4

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Based on 1 publication(s) in Google Scholar

SC-919 Related Antibodies

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Description

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[1].

IC50 & Target

IP6K1

 

In Vitro

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 Related Antibodies
In Vivo

SC-919 (1-10 mg/kg; p.o.; single dose) dose-dependently decreases plasma phosphate levels in normal male Sprague-Dawley rats[1].
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.

Animal Model: Sprague-Dawley (SD) (8-week-old male)[1]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: p.o.; single dose
Result: Increased plasma SC-919 concentrations in a dose-dependent manner.
Decreased plasma phosphate levels in a dose-dependent manner compared to vehicle control.
Animal Model: cynomolgus monkeys (3-4-year-old male, 2.6-4.7 kg)[1]
Dosage: 0.3 mg/kg; 3 mg/kg
Administration: p.o.; single dose
Result: Lowered plasma phosphate levels significantly compared to vehicle control.
Increased plasma SC-919 concentrations in a dose-dependent manner.
Animal Model: Sprague-Dawley (SD) (8-week-old male)[1]
Dosage: 10 mg/kg
Administration: p.o.; single dose; once daily for 7 days
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.
Animal Model: Sprague-Dawley (SD) (13-week-old male, adenine-induced chronic kidney disease-related hyperphosphataemia)[1]
Dosage: 1 mg/kg; 10 mg/kg
Administration: p.o.; once daily for 7 days
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.
Animal Model: Sprague-Dawley (SD) (9-week-old male, bilateral nephrectomy-induced hyperphosphataemia)[1]
Dosage: 0.3 mg/kg; 1 mg/kg
Administration: p.o.; single dose
Result: Decreased plasma phosphate levels in bilaterally nephrectomized rats with hyperphosphataemia.
Increased plasma SC-919 concentrations in a dose-dependent manner.
Animal Model: Sprague-Dawley (SD) (14-week-old male, adenine-induced chronic kidney disease with hyperphosphataemia)[1]
Dosage: 1 mg/kg; 10 mg/kg
Administration: p.o.; once daily for 5 weeks
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.
Animal Model: Sprague-Dawley (SD) (14-week-old male, adenine-induced chronic kidney disease with hyperphosphataemia)[1]
Dosage: 1 mg/kg; 10 mg/kg
Administration: p.o.; once daily for 8 days
Result: Rescued kidney ATP levels in adenine-treated rats to near-normal levels compared to vehicle control.
Animal Model: Sprague-Dawley (SD) (8-week-old male)[1]
Dosage: 0.3 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: p.o.; single dose
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.
Molecular Weight

407.25

Formula

C19H16Cl2N2O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1[C@@]2(CC[C@@H](CC2)OC3=C(C=C(C=N3)Cl)Cl)C4=CC(C(O)=O)=CC=C4N1
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 : 50 mg/mL (122.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4555 mL 12.2775 mL 24.5549 mL
5 mM 0.4911 mL 2.4555 mL 4.9110 mL
View the 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.

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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Working solution concentration: mg/mL
Purity & Documentation
References

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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SC-919 Related Classifications

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.

Keywords:

SC-9192245949-62-4LI-2124SC919SC 919LI2124LI 2124IPK SuperfamilyInositiol Polyphosphate Kinase (IPK) SuperfamilyIP6K2hyperphosphataemiaXPR1chronic kidney diseasekidney fibrosisIP6K1adenosine triphosphateIP6K3vascular calcificationinositol pyrophosphateInhibitorinhibitorinhibit

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