Dual GO/LDHA-IN-1
Dual GO/LDHA-IN-1 is an orally available dual inhibitor targeting glycolate oxidase (GO) and lactate dehydrogenase A (LDHA), with Ki values of 390 nM and 40 nM, respectively. Dual GO/LDHA-IN-1 reduces hepatic LDHA levels, urinary oxalate excretion, and renal calcium-oxalate crystal deposition. Dual GO/LDHA-IN-1 is applicable for research on primary hyperoxaluria type 1.
For research use only. We do not sell to patients.
- Formula: C37H39NO5
- Molecular Weight:577.71
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Dual GO/LDHA-IN-1 (Compound 2) potently inhibits hGO and hLDHA with selectivity for hLDHA over hLDHB (IC50 for hGO = 1.1 μM, Kᵢ for hGO = 0.39 μM, IC50 for hLDHA = 0.05 μM, Kᵢ for hLDHA = 0.04 μM, Kᵢ for hLDHB = 1.7 μM)[1].
Dual GO/LDHA-IN-1 (10-50 μM; 24 h) reduces intracellular oxalate levels without cytotoxicity[1].
Dual GO/LDHA-IN-1 (2-50 μM; 24 h) induces LDHA degradation via the autophagy-lysosomal pathway[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Agxt-/- mice (male, 12-week-old, C57BL/6J background)[1]
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Dosage:20 mg/kg
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Administration:p.o.; daily; 10 days
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Result:Reduced hepatic LDHA protein abundance, decreased hepatic LDH activity by 40% and GO activity by 25%, lowered urinary oxalate levels by ~50% from day 3 onward, increased urinary glycolate levels, reduced renal calcium-oxalate crystal deposition, and modestly reduced alanine aminotransferase (ALT) levels.
Chemical Information
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Molecular Weight 577.71
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Formula C37H39NO5
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SMILES
O=C(O)C1=CC(C2=CC=C(/C=C/C(C3=CC=C(C#CCCCCNCC45CC6CC(C5)CC(C6)C4)C=C3)=O)O2)=CC=C1O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)