A-3190
A-3190 is an orally active, blood-brain barrier permeable CD38 inhibitor, with an IC50 of 7.25 nM against human CD38 and 1.24 nM against mouse CD38. A-3190 is a derivative of A-8531 (HY-184021), and it forms covalent adducts with NAD+ in the presence of CD38. A-3190 acts as an inducer of NAD+ levels and an inhibitor of NAM and ADPR levels. A-3190 increases NAD+ levels in the skin, lung, liver and brain of rodents, while reducing NAM and ADPR levels in brain tissues. A-3190 can be used in research related to multiple sclerosis, Parkinson's disease and Alzheimer's disease.
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- 화학식: C17H13N5O2S2
- 분자량:383.45
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보관:
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
- 순도&문서
- References
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Help & FAQs
Biological Activity
A-3190 (30 mg/kg; p.o.; single dose) maintains unbound plasma concentrations above the mouse CD38 IC50 for over 24 hours and achieves moderate brain penetration[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57Bl/6J (female, average 20 g, 11-14 weeks of age)[1]
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Dosage:1 mg/kg; 3 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:p.o.; daily; 4 days
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Result:Increased NAD+ levels in a dose-dependent manner in skin, lung, liver, and brain.
Significantly increased NAD+ levels relative to vehicle at 3, 10, and 30 mg/kg in skin, lung; at 1, 3, 10, and 30 mg/kg in liver and brain.
Reached unbound tissue concentrations up to ~1000-fold over the mouse CD38 IC50 at 30 mg/kg in skin, lung, and liver.
Decreased nicotinamide (NAM) and adenosine diphosphate ribose (ADPR) levels in a dose-dependent manner in brain, with significant reductions relative to vehicle seen at 1, 3, 10, and 30 mg/kg.
Reached unbound brain concentrations up to ~80-fold over the mouse CD38 IC50 at 30 mg/kg.
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Animal Model:CD-1 (male, 25-40 g, 31-44 days old)[1]
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Dosage:30 mg/kg
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Administration:p.o.; single dose
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Result:Maintained unbound plasma concentrations above the mouse CD38 IC50 for more than 24 hours post-dose.
Achieved an unbound brain-to-plasma ratio of 0.12 at 3 hours post-dose and 0.11 at 24 hours post-dose.
Chemical Information
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분자량 383.45
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화학식 C17H13N5O2S2
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SMILES
O=S(N1N=CC(C2=NC3=C(SC=C3C4=CC=NC=C4)C=N2)=C1)(C5CC5)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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