1. Metabolic Enzyme/Protease
  2. Lactate Dehydrogenase
  3. 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.

Dual GO/LDHA-IN-1

Dual GO/LDHA-IN-1 Chemical Structure

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Description

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[1].

In Vitro

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.

In Vivo

Dual GO/LDHA-IN-1 (20 mg/kg; p.o.; daily; 10 days) reduces hepatic LDHA abundance, urinary oxalate, and renal calcium-oxalate crystal deposition in Agxt−/− mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Agxt-/- mice (male, 12-week-old, C57BL/6J background)[1]
Dosage: 20 mg/kg
Administration: p.o.; daily; 10 days
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.
Molecular Weight

577.71

Formula

C37H39NO5

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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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Dual GO/LDHA-IN-1
Cat. No.:
HY-180992
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