GNE-0877

ChemicalBook > CAS DataBase List > GNE-0877

Product Name: GNE-0877
CAS No.: 1374828-69-9
Chemical Name: GNE-0877
Synonyms: DNL201;CS-1275;GNE-0877;GNE-0877, >=98%;GNE-0877 (DNL201);GNE-0877 USP/EP/BP;GNE-0877; GNE 0877; GNE0877.;2-Methyl-2-(3-methyl-4-((4-(methylamino)-5-(trifluoromethyl)-pyrimidin-2-yl)amino)-1H-pyrazol-;1H-Pyrazole-1-acetonitrile, α,α,3-trimethyl-4-[[4-(methylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-;2-Methyl-2-[3-methyl-4-[[4-(methylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-1-pyrazolyl]propanenitrile
CBNumber: CB52703630
Molecular Formula: C14H16F3N7
Formula Weight: 339.32
MOL File: 1374828-69-9.mol

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GNE-0877 Property

Melting point:: 121 - 122°C
Boiling point:: 506.3±60.0 °C(Predicted)
Density: 1.36±0.1 g/cm3(Predicted)
storage temp.: -20°C, Inert atmosphere
solubility: DMSO (Slightly), Methanol (Slightly)
form: Solid
pka: 3.87±0.10(Predicted)
color: White to Off-White

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H317May cause an allergic skin reaction

H319Causes serious eye irritation

Precautionary statements

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 16251
Product name: GNE-0877
Purity: ≥98%
Packaging: 500μg
Price: $57
Updated: 2024/03/01

Cayman Chemical

Product number: 16251
Product name: GNE-0877
Purity: ≥98%
Packaging: 1mg
Price: $100
Updated: 2024/03/01

Cayman Chemical

Product number: 16251
Product name: GNE-0877
Purity: ≥98%
Packaging: 5mg
Price: $275
Updated: 2024/03/01

TRC

Product number: G766000
Product name: GNE-0877
Packaging: 5mg
Price: $205
Updated: 2021/12/16

ApexBio Technology

Product number: B4633
Product name: GNE0877
Packaging: 2mg
Price: $173
Updated: 2021/12/16

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GNE-0877 Chemical Properties,Usage,Production

Description

Leucine-rich repeat kinase 2 (LRRK2) is an enzyme that interacts with parkin, a ligase that is part of the ubiquitin-proteasome system that mediates the targeting of proteins for degradation. Loss of function of the parkin protein leads to dopaminergic cell death. The development of Parkinson''s disease has been strongly associated with mutations in the LRRK2 gene that lead to increased kinase activity. GNE 0877 is a selective, brain-penetrable LRRK2 inhibitor (K_i = 0.7 nM). It inhibits LRRK2 Ser¹²⁹² autophosphorylation in BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation with an IC₅₀ value of 3 nM in vivo.

Uses

GNE-0877 is a highly potent and selective leucine-rich repeat kinase 2 (LRRK2) inhibitor.

in vitro

gne-0877 showed significantly enhanced lrrk2 cellular potency (3 nm) and low turnover in human liver microsomes and hepatocytes with no evidence of glucuronidation. invitrogen kinase-selectivity profiling (188 kinases) of gne-0877 at 0.1 μm resulted in only four kinases showing greater than 50% inhibition and suggested that gne-0877 is a highly selective lrrk2 inhibitor. furthermore, gne-0877 possessed a 212-fold biochemical-selectivity index over ttk (ki = 150 nm) [1].

in vivo

gne-0877 was evaluated for its ability to inhibit in vivo lrrk2 ser1292 autophosphorylation using bac transgenic mice expressing human lrrk2 protein with the g2019s parkinson’s disease mutation. using free-drug concentrations, robust concentration-dependent inhibition of ser1292 autophosphorylation was observed for gne-0877 [1].

target

LRRK2

References

[1] estrada aa, chan bk, baker-glenn c, beresford a, burdick dj, chambers m, chen h, dominguez sl, dotson j, drummond j, flagella m, fuji r, gill a, halladay j, harris sf, heffron tp, kleinheinz t, lee dw, le pichon ce, liu x, lyssikatos jp, medhurst ad, moffat jg, nash k, scearce-levie k, sheng z, shore dg, wong s, zhang s, zhang x, zhu h, sweeney zk. discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (lrrk2) small molecule inhibitors. j med chem. 2014 feb 13;57(3):921-36.

GNE-0877 Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from GNE-0877 manufacturers

Career Henan Chemical Co

Product: GNE0877 1374828-69-9
Price: US $1.00/KG
Min. Order: 1KG
Purity: Min98% HPLC
Supply Ability: g/kg/ton
Release date: 2020-01-29

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2-Methyl-2-(3-methyl-4-((4-(methylamino)-5-(trifluoromethyl)-pyrimidin-2-yl)amino)-1H-pyrazol-

GNE-0877

alpha,alpha,3-Trimethyl-4-[[4-(methylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-1H-pyrazole-1-acetonitrile

2-methyl-2-(3-methyl-4-(4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-ylamino)-1H-pyrazol-1-yl)propanenitrile

alpha,alpha,3-Trimethyl-4-[[4-(methylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-1H-pyrazole-1-acetonitrile GNE-0877

GNE-0877, >=98%

GNE-0877; GNE 0877; GNE0877.

CS-1275

1H-Pyrazole-1-acetonitrile, α,α,3-trimethyl-4-[[4-(methylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-

GNE-0877 USP/EP/BP

DNL201

GNE-0877 (DNL201)

Leucine-rich repeat kinase 2,LRRK2,oral,brain-penetrant,small molecule,GNE0877,liver microsomes,Inhibitor,inhibit

2-Methyl-2-[3-methyl-4-[[4-(methylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-1-pyrazolyl]propanenitrile

1374828-69-9

C14H16F3N7

Inhibitors

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