An orally bioavailable, potent, and selective MAP4K4 inhibitor
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GNE-495

Item No. 21808

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
8-amino-N-[1-(cyclopropylcarbonyl)-3-azetidinyl]-2-(3-fluorophenyl)-1,7-naphthyridine-5-carboxamide
CAS Number
1449277-10-4
Molecular Formula
C22H20FN5O2
Formula Weight
405.4
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMSO: 5 mg/mlDMSO:PBS (pH 7.2) (1:7): 0.125 mg/mlEthanol: slightly soluble
λmax
277, 343 nm
SMILES
FC1=CC=CC(C2=NC3=C(N)N=CC(C(NC4CN(C(C5CC5)=O)C4)=O)=C3C=C2)=C1
InChi Code
InChI=1S/C22H20FN5O2/c23-14-3-1-2-13(8-14)18-7-6-16-17(9-25-20(24)19(16)27-18)21(29)26-15-10-28(11-15)22(30)12-4-5-12/h1-3,6-9,12,15H,4-5,10-11H2,(H2,24,25)(H,26,29)
InChi Key
FYXCIBJXJYBWPX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

    $213

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    10 mg

    $354

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    25 mg

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    Product Description

    GNE-495 is an orally bioavailable, potent, and selective MAP4K4 inhibitor (IC50 = 3.7 nM).1 In cell sprouting assays, it increases the number of protrusions.2 In a mouse model of oxygen-induced retinopathy, GNE-495 normalizes the percentage of pathological vessels and hemorrhagic areas.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ndubako, C.O., Crawford, T.D., Chen, H., et al. Structure-based design of GNE-495, a potent and selective MAP4K4 inhibitor with efficacy in retinal angiogenesis. ACS Med. Chem. Lett. 6(8), 913-918 (2015).

    2. Vitorino, O., Yeung, S., Crow, A., et al. MAP4K4 regulates integrin-FERM binding to control endothelial cell motility. Nature 519(7544), 425-430 (2015).

    Product Citations

    Nam, G.S., Kim, S., Kwon, Y.-S., et al. A new function for MAP4K4 inhibitors during platelet aggregation and platelet-mediated clot retraction. Biochem. Pharmacol. 188, 114519 (2021).