A PDE4B inhibitor
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PDE4B Inhibitor

Item No. 32732

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
[1-(3,4-dichlorophenyl)-1H-pyrrolo[2,3-b]pyridin-2-yl](3,3-difluoro-1-azetidinyl)-methanone
CAS Number
2410550-31-9
Synonyms
  • KVA-D-88
Molecular Formula
C17H11Cl2F2N3O
Formula Weight
382.2
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:5): 0.16 mg/ml
λmax
298 nm
SMILES
O=C(N1CC(F)(C1)F)C2=CC3=C(N2C4=CC=C(C(Cl)=C4)Cl)N=CC=C3
InChi Code
InChI=1S/C17H11Cl2F2N3O/c18-12-4-3-11(7-13(12)19)24-14(6-10-2-1-5-22-15(10)24)16(25)23-8-17(20,21)9-23/h1-7H,8-9H2
InChi Key
JQEUSIGJVMRCOL-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    Cayman Chemical
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    Product Description

    PDE4B inhibitor is an inhibitor of phosphodiesterase 4B (PDE4B; IC50 = 140 nM).1,2 It is selective for PDE4B over a panel of 20 PDE isoforms and a panel of 39 CNS receptors at 10 µM but does inhibit the activity of PDE4C1, PDE3B, the serotonin (5-HT) receptor subtype 5-HT2C, and sigma-2 (σ2) receptors by greater than 50%.1 PDE4B inhibitor (1 µM) decreases LPS- or Pam3Cys-induced production of TNF-α in mouse bone marrow-derived macrophages (BMDMs). It reduces cocaine self-administration and the progressive ratio breakpoint in mice when administered at a dose of 5 mg/kg.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Vadukoot, A.K., Sharma, S., Aretz, C.D., et al. Synthesis and SAR studies of 1H-pyrrolo[2,3-b]pyridine-2-carboxamides as phosphodiesterase 4B (PDE4B) inhibitors. ACS Med. Chem. Lett. 11(10), 1848-1854 (2020).

    2. Burkovetskaya, M.E., Liu, Q., Vadukoot, A.K., et al. KVA-D-88, a novel preferable phosphodiesterase 4B inhibitor, decreases cocaine-mediated reward properties in vivo. ACS Chem. Neurosci. 11(15), 2231-2242 (2020).