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GNE-0877

GNE-0877 Structure
GNE-0877
  • CAS No.1374828-69-9
  • Chemical Name:GNE-0877
  • CBNumber:CB52703630
  • Molecular Formula:C14H16F3N7
  • Formula Weight:339.32
  • MOL File:1374828-69-9.mol
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
  • FDA UNII ANGHS285FG
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal wordWarning
  • Hazard statements H317-H319
  • Precautionary statements P280-P305+P351+P338

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 (Ki = 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
GNE-0877 Suppliers
Global(96)Suppliers
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    career henan chemical co
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GNE-0877 Spectrum
1374828-69-9, GNE-0877Related Search:
  • API
  • Inhibitors
  • 抑制剂
  • 合成有机化合物配体
  • 小分子抑制剂，天然产物
  • C14H16F3N7
  • 化合物GNE0877,10 MM DMSO 溶液
  • 2-甲基-2-[3-甲基-4-[[4-(甲氨基)-5-(三氟甲基)-2-嘧啶基]氨基]-1-吡唑基]丙腈
  • 2-甲基-2-(3-甲基-4-((4-(甲胺基)-5-(三氟甲基)嘧啶-2-基)氨基)-1H-吡唑-1-基)丙腈
  • 2-甲基-2-(3-甲基-4-(4-(甲基氨基)-5-(三氟甲基)嘧啶-2-基氨基)-1H-吡唑-1-基)丙腈
  • 化合物GNE0877
  • ALPHA,ALPHA,3-三甲基-4-[[4-(甲基氨基)-5-(三氟甲基)-2-嘧啶基]氨基]-1H-吡唑-1-乙腈
  • 1374828-69-9
  • GNE0877, 10 mM in DMSO
  • 2-Methyl-2-[3-methyl-4-[[4-(methylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-1-pyrazolyl]propanenitrile
  • Leucine-rich repeat kinase 2,LRRK2,oral,brain-penetrant,small molecule,GNE0877,liver microsomes,Inhibitor,inhibit
  • GNE-0877 (DNL201)
  • DNL201
  • GNE-0877 USP/EP/BP
  • 1H-Pyrazole-1-acetonitrile, α,α,3-trimethyl-4-[[4-(methylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-
  • CS-1275
  • GNE-0877; GNE 0877; GNE0877.
  • GNE-0877, >=98%
  • alpha,alpha,3-Trimethyl-4-[[4-(methylamino)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-1H-pyrazole-1-acetonitrile GNE-0877
  • 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
  • 2-Methyl-2-(3-methyl-4-((4-(methylamino)-5-(trifluoromethyl)-pyrimidin-2-yl)amino)-1H-pyrazol-

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