1. Immunology/Inflammation
  2. CD38
  3. CVN14

CVN14 is a potent, selective and brain-penetrant CD38 inhibitor with human IC50 19 nM, mouse IC50 2.4 nM. CVN14 binds uncompetitively to form a complex with CD38 and ADPR, and inhibits CD38 enzymatic activity. CVN14 can be used for the research of neurodegenerative diseases.

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CVN14

CVN14 Chemical Structure

CAS No. : 2925663-26-7

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Description

CVN14 is a potent, selective and brain-penetrant CD38 inhibitor with human IC50 19 nM, mouse IC50 2.4 nM. CVN14 binds uncompetitively to form a complex with CD38 and ADPR, and inhibits CD38 enzymatic activity. CVN14 can be used for the research of neurodegenerative diseases[1].

In Vitro

CVN14 potently inhibits human CD38 with an IC50 of 19 nM and mouse CD38 with an IC50 of 2.4 nM[1].
CVN14 potently inhibits human CD38 activity in CHO-hCD38 cells with an IC50 of 19 nM[1].
CVN14 binds tightly to human CD38 with a Kd of 3.6 nM and a long dissociation half-life of 143 min[1].
CVN14 has favorable in vitro permeability across MDR1-MDCK cell monolayers with an efflux ratio of 0.90[1].

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

Parmacokinetics
Species Dose Route CLplasma Vdss C0 AUC0-∞ T1/2 Cmax Tmax
Mice[1] 1 mg/kg i.v. 5.5 mL/min/kg 0.84 L/kg 5.77 μM 8.15 μM·h 2.32 h / /
Mice[1] 10 mg/kg p.o. / / / 98.5 μM·h 2.53 h 29.6 μM 0.5 h
In Vivo

CVN14 (10 mg/kg; p.o.; single dose) shows a high distribution to the brain with Kpuu,brain values greater than 0.3[1].

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

Molecular Weight

382.38

Formula

C17H21F3N6O

CAS No.
SMILES

FC(F)(F)CN[C@H](CC1)CC[C@@H]1NC(C2=CC(C)=NC(N3C=NC=C3)=N2)=O

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Storage

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

Purity & Documentation
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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.

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CVN14
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HY-181543
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