A potent LRRK2 inhibitor
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GNE-9605

Item No. 23446

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
rel-N2-[5-chloro-1-[(3R,4R)-3-fluoro-1-(3-oxetanyl)-4-piperidinyl]-1H-pyrazol-4-yl]-N4-methyl-5-(trifluoromethyl)-2,4-pyrimidinediamine
CAS Number
1536200-31-3
Molecular Formula
C17H20ClF4N7O
Formula Weight
449.8
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 20 mg/mlMethanol: 1 mg/ml
λmax
230 nm
SMILES
CNC1=C(C(F)(F)F)C=NC(NC2=C(Cl)N([C@H]3CCN(C4COC4)C[C@@H]3F)N=C2)=N1
InChi Code
InChI=1S/C17H20ClF4N7O/c1-23-15-10(17(20,21)22)4-24-16(27-15)26-12-5-25-29(14(12)18)13-2-3-28(6-11(13)19)9-7-30-8-9/h4-5,9,11,13H,2-3,6-8H2,1H3,(H2,23,24,26,27)/t11-,13-/m0/s1
InChi Key
PUXPEQJKNAWNQA-AAEUAGOBSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $44

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    5 mg

    $195

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    10 mg

    $344

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    25 mg

    $642

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    Product Description

    GNE-9065 is an orally bioavailable and potent inhibitor of leucine-rich repeat kinase 2 (LRRK2; IC50 = 18.7 nM).1 It is selective for LRRK2 over 178 kinases, inhibiting only TAK1-TAB1 >50% at a concentration of 0.1 μM. GNE-9065 (10 and 50 mg/kg) inhibits LRRK2 Ser1292 autophosphorylation in BAC transgenic mice expressing human LRRK2 protein with the G2019S mutation found in families with autosomal Parkinson’s disease.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Estrada, A.A., Chan, B.K., Baker-Glenn, C., et al. Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. J. Med. Chem. 57(3), 921-936 (2014).