INSP-0154
INSP-0154 is a potent creatine kinase B (CKB)/creatine transporter (SLC6A8) inhibitor. INSP-0154 binds to the SLC6A8 occluded pocket, prevents creatine transport into cells, and protects SLC6A8 cysteine residue C144 from irreversible inactivation. INSP-0154 inhibits creatine uptake in mouse heart tissue. INSP-0154 can be used for the research of cancer.
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- Formule: C6H10N4O2
- Masse moléculaire:170.17
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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
- Pureté et documentation
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
SLC6A8 |
In Vitro
INSP-0154 (Compound 46) (0.46-1000 μM; 1 h) potently inhibits SLC6A8-mediated creatine uptake in HCT-116 cells with an IC50 of 8.2 μM[1].
INSP-0154 (0.46-1000 μM) inhibits GAT-2, GAT-3, BGT-1, and TAUT-mediated creatine uptake with IC50 of 22.7, 150, 116 and 11.9 μM, while showing no activity against GAT-1 at concentrations up to 1000 μM[1].
INSP-0154 shows strong in vitro plasma and metabolic stability, low Caco-2 permeability, and is not a P-gp efflux substrate[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, 6−9 weeks old)[1]
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Dosage:100 mg/kg
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Administration:i.p.; single dose
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Result:Achieved inhibition of creatine-d3 uptake in heart tissue, with greater potency than β-GPA under the tested conditions.
Chemical Information
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Masse moléculaire 170.17
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Formule C6H10N4O2
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SMILES
[H][C@]12CN(C[C@]1(C(NO2)=O)[H])C(N)=N
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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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
INSP-0154 Related Classifications
HY-181753 Related Classifications
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