TAS-303
TAS-303 is an orally effective selective norepinephrine transporter (NET) inhibitor. TAS-303 inhibits human NET ligand binding with a Ki of 50.9 nM, and suppresses NET-mediated norepinephrine uptake with an IC50 of 38.9 nM. TAS-303 enhances norepinephrine-induced contraction in isolated rat urethral tissues, elevates plasma norepinephrine levels in rats, and increases urethral baseline pressure and leak point pressure. TAS-303 is applicable for research related to stress urinary incontinence, norepinephrine reuptake, and lower urinary tract function.
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- CAS. Nr.: 1449371-87-2
- Formel: C22H20D7NO3
- Molecular Weight:360.50
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
Human NET 50.9 nM (Ki) |
Human NET 38.9 nM (IC50) |
In Vitro
TAS-303 (3-3000 nM; 3 h) inhibits ligand binding to human NET, SERT, and DAT, with Ki values of 50.9, 1560, and 1290 nM, respectively, and exhibits selectivity for NET[1].
TAS-303 (3-3000 nM; preincubated at 25°C for 20 min) potently and selectively inhibits the uptake of [3H]norepinephrine in MDCK cells expressing human NET, with an IC50 of 38.9 nM[1].
TAS-303 (10-1000 nM; rat isolated urethral tissue) shifts the concentration-response curve of noradrenaline-induced urethral contraction to the left[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
TAS-303 (0.3-3 mg/kg; p.o.; single administration) dose-dependently increases the baseline urethral pressure in healthy female Sprague-Dawley rats, with a 38% increase in pressure observed at the dose of 3 mg/kg[1].
TAS-303 (0.3-3 mg/kg; p.o.; single administration) dose-dependently increases the leak point pressure in a rat model of vaginal distension-induced stress urinary incontinence, with a 26% increase observed at the dose of 3 mg/kg [1].
TAS-303 (10-100 mg/kg; p.o.; single administration) has no effect on the immobility time in the forced swimming test of healthy female Sprague-Dawley rats[1].
TAS-303 (1-10 mg/kg; p.o.; single administration) exerts no effects on cardiovascular parameters in conscious healthy dogs[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 (female, 10 weeks of age)[1]
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Dosage:3 mg/kg
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Administration:p.o.; once daily for 7 days
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Result:Increased plasma norepinephrine levels significantly compared to vehicle-treated rats.
Produced no differences in plasma epinephrine, dopamine, or serotonin levels compared to vehicle-treated rats.
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Animal Model:Sprague-Dawley (female, 11 weeks of age)[1]
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Dosage:0.3 mg/kg; 1 mg/kg; 3 mg/kg
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Administration:p.o.; single dose
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Result:Produced a dose-dependent increase in urethral baseline pressure.
Increased urethral pressure significantly at doses of 1 mg/kg and 3 mg/kg compared to vehicle.
Increased urethral baseline pressure by 38% at the 3 mg/kg dose.
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Animal Model:Sprague-Dawley (female, 11 weeks of age, stress urinary incontinence induced by vaginal distention)[1]
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Dosage:0.3 mg/kg; 1 mg/kg; 3 mg/kg
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Administration:p.o.; single dose
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Result:Produced a dose-dependent increase in leak point pressure (LPP).
Increased LPP significantly at doses of 1 mg/kg and 3 mg/kg compared to vehicle.
Increased LPP by 26% at the 3 mg/kg dose.
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Animal Model:Sprague-Dawley (female, 11 weeks of age)[1]
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Dosage:10 mg/kg; 30 mg/kg; 100 mg/kg
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Administration:p.o.; single dose
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Result:Produced no significant change in immobility time compared to vehicle-treated rats at all tested doses.
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Animal Model:Conscious dogs[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:Produced no significant changes in systolic blood pressure, diastolic blood pressure, mean blood pressure, or heart rate compared to vehicle-treated dogs at all tested doses.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Anwendung
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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CAS. Nr. 1449371-87-2
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Unlabeled CAS 108640-65-9
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Molecular Weight 360.50
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Formel C22H20D7NO3
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SMILES
C(C(OC1CCNCC1)=O)(OC(C(C([2H])([2H])[2H])([2H])[2H])([2H])[2H])(C2=CC=CC=C2)C3=CC=CC=C3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
TAS-303 Related Classifications
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