JTP-59557
JTP-59557 is an orally active, stereospecific noncompetitive inhibitor of type IIb sodium/phosphate cotransporter (NaPi-IIb). JTP-59557 selectively inhibits type IIb-mediated inorganic phosphate uptake, without affecting Na+-independent inorganic phosphate transport or Na+-dependent D-glucose (HY-B0389) transport. JTP-59557 also suppresses Na+-dependent inorganic phosphate transport in intestinal brush border membrane vesicles. JTP-59557 is applicable to research related to hyperphosphatemia and hyperphosphatemia associated with chronic kidney disease.
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- CAS No.: 540733-03-7
- Formule: C18H15Cl2F3N4OS
- Masse moléculaire:463.30
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
0.12 μM
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Inhibition of human type IIb Na/Pi cotransporter-mediated inorganic phosphate (Pi) uptake in Chinese hamster ovary (CHO) cells stably expressing human type IIb Na/Pi cotransporter via rapid filtration assay with [33P]orthophosphate as substrate, incubated for 10 minutes at room temperature.
Inhibition of human type IIb Na/Pi cotransporter-mediated inorganic phosphate (Pi) uptake in Chinese hamster ovary (CHO) cells stably expressing human type IIb Na/Pi cotransporter via rapid filtration assay with [33P]orthophosphate as substrate, incubated for 10 minutes at room temperature.
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15961073 |
In Vitro
JTP-59557 (0.01-10 μM; 2 min) potently and selectively inhibits Na+-dependent Pi transport in rabbit intestinal brush border membrane vesicles as a noncompetitive inhibitor with an IC50 of 0.40 μM, with no effect on Na+-independent Pi or Na+-dependent d-glucose transport[1].
JTP-59557 (0.01-10 μM) potently and selectively inhibits Na+-dependent Pi transport in rat intestinal brush border membrane vesicles with an IC50 of 0.19 μM, with no effect on Na+-independent Pi or Na+-dependent d-glucose transport[1].
JTP-59557 (0.01-10 μM; 10 min) potently inhibits IIb Na/Pi cotransporter-mediated Pi uptake in stably transfected CHO cells with an IC50 of 0.12 μM, with no effect on Pi uptake in wild-type CHO cells[1].
JTP-59557 potently and selectively inhibits NaPi transport in rabbit and rat intestinal BBMVs with IC50 values of 0.40 μM and 0.19 μM, respectively, and acts as a noncompetitive inhibitor relative to Pi[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
JTP-59557 (30 mg/kg; p.o.; single dose) increases residual luminal phosphorus concentration in the small intestine and cecum of chow-fed normal rats, indicating reduced intestinal phosphate absorption[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 (IGS) (male, 180-270 g, ligated intestinal model)[1]
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Dosage:3 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:i.d.; single dose
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Result:Reduced peripheral vein serum radioactivity to ~65% of vehicle levels at 3 mg/kg.
Reduced peripheral vein serum radioactivity to ~40% of vehicle levels at 10 mg/kg.
Reduced peripheral vein serum radioactivity to ~30% of vehicle levels at 30 mg/kg.
Reduced portal vein serum radioactivity to ~55% of vehicle levels at 10 mg/kg.
Reduced portal vein serum radioactivity to ~30% of vehicle levels at 30 mg/kg.
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Animal Model:Sprague-Dawley (IGS) (male, 280-350 g, chow-fed model)[1]
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Dosage:30 mg/kg
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Administration:p.o.; single dose
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Result:Did not alter the dry weight of residual luminal contents in the stomach, small intestine, or cecum compared to vehicle.
Increased residual phosphorus concentration in the small intestine to ~6 mg/g (vs ~4.5 mg/g in vehicle).
Increased residual phosphorus concentration in the cecum to ~17 mg/g (vs ~13 mg/g in vehicle).
Showed no change in stomach phosphorus concentration.
Chemical Information
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CAS No. 540733-03-7
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Masse moléculaire 463.30
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Formule C18H15Cl2F3N4OS
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SMILES
O=C1NN=C(SC2=NC=C(C=C2)C(F)(F)F)N1C3=CC(Cl)=C(Cl)C=C3C(C)(C)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Matsuo A, et al. Inhibitory effect of JTP-59557, a new triazole derivative, on intestinal phosphate transport in vitro and in vivo. European journal of pharmacology. 2005 Jul 04;517(1-2):111-9. [Content Brief]
[2]. Miyamoto K, et al. Sodium-dependent phosphate cotransporters: lessons from gene knockout and mutation studies. Journal of pharmaceutical sciences. 2011 Sep;100(9):3719-30. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
JTP-59557 Related Classifications
HY-157066 Related Classifications
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