GNE-7915 free base · Synonyms: GNE 7915 · GNE7915

GNE-7915 is a potent, selective and brain-penetrant inhibitor of LRRK2.

For research use only. Not for human or veterinary use.

Target LRRK2

Research area Neurological Disease

Purity >98% Stock Inquire

Data Sheet SDS COA

GNE-7915 structure

CAS No.: 1351761-44-8

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
500 mg	USD 450.00	BP-02129-500mg	In stock	Get quote
1 g	USD 710.00	BP-02129-1g	In stock	Get quote
2 g	USD 1,120.00	BP-02129-2g	In stock	Get quote
5 g	USD 2,200.00	BP-02129-5g	In stock	Get quote
10 g	USD 3,800.00	BP-02129-10g	In stock	Get quote

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Description

GNE-7915 is a potent, selective and brain-penetrant inhibitor of LRRK2 with an IC50 of 9 nM.

Biological activity

In Vitro Maintaining the methoxy/fluoro arrangement at C-2′/C-5′ and varying aminoalkyl R1 substitution resultes in single-digit nanomolar LRRK2 cellular activities for GNE-7915 and compound 19. Expanded Invitrogen kinase profiling (187 kinases) at 0.1 μM for both GNE-7915 (100-fold over LRRK2 Ki) and 19 (250-fold over LRRK2 Ki) resultes in only TTK showing greater than 50% inhibition. Selectivity profiling using the DiscoverX KinomeScan55 competitive binding assay panel, which includes 392 unique kinases, is also performed for GNE-7915 at 0.1 μM. Binding of >50% probe displacement is detected for 10 kinases and of >65% for only LRRK2, TTK, and ALK, further supporting the excellent LRRK2 selectivity for GNE-7915. Cerep receptor profiling, including expanded brain panels, suggestes that GNE-7915 and 19 only inhibite 5-HT2B with >70% inhibition at 10 μM. GNE-7915 and 19 are confirmed to be moderately potent 5-HT2B antagonists in vitro functional assays.

Identifiers

SMILES: CCNC1=NC(NC2=C(OC)C=C(C(=O)N3CCOCC3)C(F)=C2)=NC=C1C(F)(F)F
InChIKey: XCFLWTZSJYBCPF-UHFFFAOYSA-N

Specifications

MW (average): 443.3954
Formula: C₁₉H₂₁F₄N₅O₃
CAS No.: 1351761-44-8
Physical state: Solid
Color: off-white to light yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Kavanagh ME, et al. The development of CNS-active LRRK2 inhibitors using property-directed optimisation. Bioorg Med Chem Lett.?2013 Jul 1;23(13):3690-6.

[2]. Estrada AA, et al. Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. J Med Chem. 2012 Nov 26;55(22):9416-33.

Same research area

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