2. Immunology/Inflammation
  3. CD38
  4. 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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A-3190

A-3190 Chemical Structure

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A-3190 Related Antibodies

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Description

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[1].

In Vitro

A-3190 (compound 39) (1 μM; 1-2 h) potently inhibits human CD38 with an IC50 of 7.25 nM and mouse CD38 with an IC50 of 1.24 nM in a biochemical etheno-NAD hydrolase inhibition assay[1].

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

A-3190 Related Antibodies
In Vivo

A-3190 (compound 39) (1-30 mg/kg; p.o.; daily; 4 days) dose-dependently boosts NAD+ levels (and reduces NAM/ADPR levels in brain) in mouse skin, lung, liver, and brain, with unbound tissue concentrations reaching up to 1000-fold over the mouse CD38 IC50[1].
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.

Animal Model: C57Bl/6J (female, average 20 g, 11-14 weeks of age)[1]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg; 30 mg/kg
Administration: p.o.; daily; 4 days
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.
Animal Model: CD-1 (male, 25-40 g, 31-44 days old)[1]
Dosage: 30 mg/kg
Administration: p.o.; single dose
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.
Molecular Weight

383.45

Formula

C17H13N5O2S2
SMILES

O=S(N1N=CC(C2=NC3=C(SC=C3C4=CC=NC=C4)C=N2)=C1)(C5CC5)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
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A-3190 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

A-3190A3190A 3190CD38ADPRparkinson’s diseaseCD-1 miceNAMMDCK-MDR1 cellsNAD+strokealzheimer’s diseasemultiple sclerosisInhibitorinhibitorinhibit

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