GNE-7915
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 510257

CAS#: 1351761-44-8 (free base)

Description: GNE-7915 is a potent LRRK2 kinase inhibitor, which possess an ideal balance of LRRK2 cellular potency, broad kinase selectivity, metabolic stability, and brain penetration across multiple species. GNE-7915 was reported as a potent (IC50=9 nM) selective (1/187 kinases), brain-penetrant and non-toxic inhibitor of LRRK2.


Chemical Structure

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GNE-7915
CAS# 1351761-44-8 (free base)

Theoretical Analysis

MedKoo Cat#: 510257
Name: GNE-7915
CAS#: 1351761-44-8 (free base)
Chemical Formula: C19H21F4N5O3
Exact Mass: 443.15805
Molecular Weight: 443.39535
Elemental Analysis: C, 51.47; H, 4.77; F, 17.14; N, 15.79; O, 10.83

Size Price Shipping out time Quantity
25mg USD 120 Same day
50mg USD 190 Same day
100mg USD 350 Same day
200mg USD 650 Same day
500mg USD 1350 Same day
1g USD 2250 Same day
2g USD 3850 Same day
Inquire bulk and customized quantity

Pricing updated 2021-02-26. Prices are subject to change without notice.

GNE-7915, purity > 98%, is in stock, the same day shipped after order received.

Related CAS #: 2070015-00-6 (tosylate)   1351761-44-8 (free base)    

Synonym: GNE7915; GNE 7915; GNE-7915.

IUPAC/Chemical Name: (4-((4-(ethylamino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)-2-fluoro-5-methoxyphenyl)(morpholino)methanone

InChi Key: XCFLWTZSJYBCPF-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H21F4N5O3/c1-3-24-16-12(19(21,22)23)10-25-18(27-16)26-14-9-13(20)11(8-15(14)30-2)17(29)28-4-6-31-7-5-28/h8-10H,3-7H2,1-2H3,(H2,24,25,26,27)

SMILES Code: O=C(C1=CC(OC)=C(NC2=NC=C(C(F)(F)F)C(NCC)=N2)C=C1F)N3CCOCC3

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
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 Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001

Biological target: LRRK2 kinase
In vitro activity: LRRK2 IC50: 9 nM (J Med Chem. 2012 Nov 26;55(22):9416-33. doi: 10.1021/jm301020q)

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 10.0 22.55

Preparing Stock Solutions

The following data is based on the product molecular weight 443.39535 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
In vitro protocol: In vitro protocol was reported in below reference: Estrada AA, Liu X, Baker-Glenn C, Beresford A, Burdick DJ, Chambers M, Chan BK, Chen H, Ding X, DiPasquale AG, Dominguez SL, Dotson J, Drummond J, Flagella M, Flynn S, Fuji R, Gill A, Gunzner-Toste J, Harris SF, Heffron TP, Kleinheinz T, Lee DW, Le Pichon CE, Lyssikatos JP, Medhurst AD, Moffat JG, Mukund S, Nash K, Scearce-Levie K, Sheng Z, Shore DG, Tran T, Trivedi N, Wang S, Zhang S, Zhang X, Zhao G, Zhu H, Sweeney ZK.Customer may reference protocol in blow papers: 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. doi: 10.1021/jm301020q. Epub 2012 Oct 15. PMID: 22985112.
In vivo protocol: In vivo protocol was reported in below reference: Howlett EH, Jensen N, Belmonte F, Zafar F, Hu X, Kluss J, Schüle B, Kaufman BA, Greenamyre JT, Sanders LH. LRRK2 G2019S-induced mitochondrial DNA damage is LRRK2 kinase dependent and inhibition restores mtDNA integrity in Parkinson's disease. Hum Mol Genet. 2017 Nov 15;26(22):4340-4351. doi: 10.1093/hmg/ddx320. PMID: 28973664; PMCID: PMC5886254.

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1: Baptista MAS, Merchant K, Barrett T, Bhargava S, Bryce DK, Ellis JM, Estrada AA, Fell MJ, Fiske BK, Fuji RN, Galatsis P, Henry AG, Hill S, Hirst W, Houle C, Kennedy ME, Liu X, Maddess ML, Markgraf C, Mei H, Meier WA, Needle E, Ploch S, Royer C, Rudolph K, Sharma AK, Stepan A, Steyn S, Trost C, Yin Z, Yu H, Wang X, Sherer TB. LRRK2 inhibitors induce reversible changes in nonhuman primate lungs without measurable pulmonary deficits. Sci Transl Med. 2020 Apr 22;12(540):eaav0820. doi: 10.1126/scitranslmed.aav0820. PMID: 32321864.

2: Liu H, Ho PW, Leung CT, Pang SY, Chang EES, Choi ZY, Kung MH, Ramsden DB, Ho SL. Aberrant mitochondrial morphology and function associated with impaired mitophagy and DNM1L-MAPK/ERK signaling are found in aged mutant Parkinsonian LRRK2R1441G mice. Autophagy. 2020 Dec 10:1-25. doi: 10.1080/15548627.2020.1850008. Epub ahead of print. PMID: 33300446.

3: Cao J, Zhuang Y, Zhang J, Zhang Z, Yuan S, Zhang P, Li H, Li X, Shen H, Wang Z, Chen G. Leucine-rich repeat kinase 2 aggravates secondary brain injury induced by intracerebral hemorrhage in rats by regulating the P38 MAPK/Drosha pathway. Neurobiol Dis. 2018 Nov;119:53-64. doi: 10.1016/j.nbd.2018.07.024. Epub 2018 Jul 23. PMID: 30048803.

4: Qin Q, Zhi LT, Li XT, Yue ZY, Li GZ, Zhang H. Effects of LRRK2 Inhibitors on Nigrostriatal Dopaminergic Neurotransmission. CNS Neurosci Ther. 2017 Feb;23(2):162-173. doi: 10.1111/cns.12660. Epub 2016 Dec 9. PMID: 27943591; PMCID: PMC5248597.

5: Kavanagh ME, Doddareddy MR, Kassiou M. The development of CNS-active LRRK2 inhibitors using property-directed optimisation. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3690-6. doi: 10.1016/j.bmcl.2013.04.086. Epub 2013 May 9. PMID: 23721803.

6: Howlett EH, Jensen N, Belmonte F, Zafar F, Hu X, Kluss J, Schüle B, Kaufman BA, Greenamyre JT, Sanders LH. LRRK2 G2019S-induced mitochondrial DNA damage is LRRK2 kinase dependent and inhibition restores mtDNA integrity in Parkinson's disease. Hum Mol Genet. 2017 Nov 15;26(22):4340-4351. doi: 10.1093/hmg/ddx320. PMID: 28973664; PMCID: PMC5886254.

7: Estrada AA, Liu X, Baker-Glenn C, Beresford A, Burdick DJ, Chambers M, Chan BK, Chen H, Ding X, DiPasquale AG, Dominguez SL, Dotson J, Drummond J, Flagella M, Flynn S, Fuji R, Gill A, Gunzner-Toste J, Harris SF, Heffron TP, Kleinheinz T, Lee DW, Le Pichon CE, Lyssikatos JP, Medhurst AD, Moffat JG, Mukund S, Nash K, Scearce-Levie K, Sheng Z, Shore DG, Tran T, Trivedi N, Wang S, Zhang S, Zhang X, Zhao G, Zhu H, Sweeney ZK. 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. doi: 10.1021/jm301020q. Epub 2012 Oct 15. PMID: 22985112.



Additional Information