8-Aminoinosine
8-Aminoinosine is a purine nucleoside phosphorylase (PNPase) inhibitor with a Ki value of 35 μM for the human target. 8-Aminoinosine exerts indirect competitive inhibition through two mechanisms: competitive substrate occupancy and metabolic conversion to the PNPase inhibitor (8-Aminohypoxanthine). 8-Aminoinosine induces increased urine output, sodium excretion, and glucose excretion, without altering potassium excretion. 8-Aminoinosine can be used in research related to hypertension, heart failure, and chronic kidney disease.
For research use only. We do not sell to patients.
- CAS No.: 13389-16-7
- Formula: C10H13N5O5
- Molecular Weight:283.24
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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- References
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Biological Activity
Description
IC50 & Target
[1]|
PNPase 35 μM (Ki) |
In Vitro
8-Aminoinosine (25-100 μM; 10 min) competitively inhibits recombinant human purine nucleoside phosphorylase with a Ki value of 35 μM and mediates direct and indirect PNPase inhibition through conversion to 8-aminohypoxanthine[1][2].
8-Aminoinosine (100-2000 μM; 10 min) serves as a competitive substrate for recombinant human purine nucleoside phosphorylase, with a Km value of 143 μM and a Vmax value of 58 μM/L per 10 minutes[1].
8-Aminoinosine (25-100 μM; 10 min) is a competitive substrate of recombinant human PNPase, and inosine competitively occupies the enzyme active site in a concentration-dependent manner, inhibiting its metabolic conversion to 8-aminohypoxanthine[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, ~16 weeks old, anesthetized, instrumented)[1]
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Dosage:33.5 mmol/kg
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Administration:i.v.; single bolus injection
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Result:Suppressed the urinary guanine-to-guanosine ratio to 0.19 during Period 3.
Suppressed the urinary hypoxanthine-to-inosine ratio to 0.56 during Period 3.
Increased urine volume to 274 mL per 30 minutes during Period 2 and 371 mL per 30 minutes during Period 3, up from a basal 69 mL per 30 minutes.
Increased sodium excretion to 12.8 mmoles per 30 minutes during Period 2 and 24.2 mmoles per 30 minutes during Period 3, up from a basal 2.7 mmoles per 30 minutes.
Increased glucose excretion to 11.7 mg per 30 minutes during Period 2 and 8.1 mg per 30 minutes during Period 3, up from a basal 3.6 mg per 30 minutes.
Did not alter potassium excretion (basal: 25.0 mmoles per 30 minutes; Period 2: 24.8 mmoles per 30 minutes; Period 3: 26.9 mmoles per 30 minutes).
Did not affect mean arterial blood pressure, heart rate, renal blood flow, or mesenteric blood flow across all periods.
Increased urinary excretion of this compound to 60 nmol per 30 minutes during Period 2 and 20 nmol per 30 minutes during Period 3.
Increased urinary excretion of 8-aminohypoxanthine to measurable levels during Periods 2 and 3.
Chemical Information
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CAS No. 13389-16-7
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Molecular Weight 283.24
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Formula C10H13N5O5
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SMILES
O=C1C2=C(N([C@H]3[C@H](O)[C@H](O)[C@@H](CO)O3)C(N)=N2)NC=N1
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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)
8-Aminoinosine Related Classifications
HY-W743023 Related Classifications
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