Art. -Nr.: HY-171099

SC-919

(Synonyms: LI-2124)

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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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Reinheit: 98.68%
CAS. Nr.: 2245949-62-4
Formel: C₁₉H₁₆Cl₂N₂O₄
Molecular Weight:407.25

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

SC-919 Chemical Structure

CAS. Nr.: 2245949-62-4

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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.

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.

Chemical Information

CAS. Nr. 2245949-62-4
Appearance Solid
Molecular Weight 407.25
Formel C₁₉H₁₆Cl₂N₂O₄
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
Synonyms

LI-2124
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4555 mL

12.2775 mL

24.5549 mL

5 mM

0.4911 mL

2.4555 mL

4.9110 mL

10 mM

0.2455 mL

1.2277 mL

2.4555 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Moritoh Y, et al. The enzymatic activity of inositol hexakisphosphate kinase controls circulating phosphate in mammals. Nat Commun. 2021;12(1):4847. Published 2021 Aug 11. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

MCE Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SC-919 Related Classifications

HY-171099 Related Classifications