A brain penetrant inhibitor of wild-type and G2019S mutant LRRK2
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HG-10-102-01

Item No. 20049

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
[4-[[5-chloro-4-(methylamino)-2-pyrimidinyl]amino]-3-methoxyphenyl]-4-morpholinyl-methanone
CAS Number
1351758-81-0
Molecular Formula
C17H20ClN5O3
Formula Weight
377.8
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mLDMSO: 30 mg/mLDMSO:PBS(pH 7.2) (1:4): 0.2 mg/mLEthanol: 0.3 mg/mL
λmax
225, 275, 309 nm
SMILES
O=C(C1=CC(OC)=C(NC2=NC=C(Cl)C(NC)=N2)C=C1)N3CCOCC3
InChi Code
InChI=1S/C17H20ClN5O3/c1-19-15-12(18)10-20-17(22-15)21-13-4-3-11(9-14(13)25-2)16(24)23-5-7-26-8-6-23/h3-4,9-10H,5-8H2,1-2H3,(H2,19,20,21,22)
InChi Key
YEVOZZZLKJKCCD-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    HG-10-102-01 is an inhibitor of leucine-rich repeat kinase 2 (LRRK2; IC50 = 20.3 nM).1 It also inhibits the G2019S, A2016T, and [G2019S+A2016T] mutants of LRRK2 (IC50s = 3.2, 153, and 95.9 nM, respectively).1 HG-10-102-01 substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type and G2019S mutant LRRK2 in cells. When given intraperitoneally, HG-10-102-01 penetrates the blood-brain barrier and inhibits phosphorylation of LRRK2 in the brain as well as the kidney and spleen.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Choi, H.G., Zhang, J., Deng, X., et al. Brain Penetrant LRRK2 Inhibitor. ACS Med. Chem. Lett. 3(8), 658-662 (2012).