A GRK2 inhibitor
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Takeda-103A

Item No. 41027

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(2,6-difluorophenyl)methyl]-3-[[[4-propyl-5-(4-pyrimidinyl)-4H-1,2,4-triazol-3-yl]methyl]amino]-benzamide
CAS Number
865609-72-9
Molecular Formula
C24H23F2N7O
Formula Weight
463.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/mlEthanol: Soluble: ≥10 mg/ml
SMILES
O=C(C1=CC(NCC2=NN=C(C3=NC=NC=C3)N2CCC)=CC=C1)NCC4=C(F)C=CC=C4F
InChi Code
InChI=1S/C24H23F2N7O/c1-2-11-33-22(31-32-23(33)21-9-10-27-15-30-21)14-28-17-6-3-5-16(12-17)24(34)29-13-18-19(25)7-4-8-20(18)26/h3-10,12,15,28H,2,11,13-14H2,1H3,(H,29,34)
InChi Key
VWBSMGFTNCQOMB-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

    Takeda-103A is an inhibitor of G protein-coupled receptor kinase 2 (GRK2).1 It selectively inhibits phosphorylation of bovine rod outer segments by GRK2 (IC50 = 54 nM) over phosphorylation by GRK1 and GRK5 at concentrations up to 125 µM. Takeda-103A also inhibits phosphorylation of bovine rod outer segments by GRK2 containing various mutations, including GRK2L271M, GRK2Y206S, GRK2I197L, and GRK2L235G (IC50s = 24, 55, 106, and 180 nM, respectively).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Thal, D.M., Yeow, R., Schoenau, C., et al. Molecular mechanism of selectivity among G protein-coupled receptor kinase 2 inhibitors. Mol. Pharmacol. 80(2), 294-303 (2011).