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GNE-495 is a potent and selective inhibitor of leucine-rich repeat kinase 2 (LRRK2), a protein implicated in the pathogenesis of Parkinson's disease. It has been developed as a potential therapeutic agent for the treatment of Parkinson's disease and other neurodegenerative disorders. GNE-495 has demonstrated the ability to decrease LRRK2 activity and reduce the accumulation of toxic alpha-synuclein aggregates, a characteristic feature of Parkinson's disease. GNE-495 has also shown favorable pharmacokinetic properties and good brain penetration, positioning it as a promising candidate for further development as a disease-modifying therapy for Parkinson's and other neurodegenerative conditions.

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  • 1449277-10-4 Structure
  • Basic information

    1. Product Name: GNE-495
    2. Synonyms: GNE-495;8-Amino-N-[1-(cyclopropylcarbonyl)-3-azetidinyl]-2-(3-fluorophenyl)-1,7-naphthyridine-5-carboxamide
    3. CAS NO:1449277-10-4
    4. Molecular Formula: C22H20FN5O2
    5. Molecular Weight: 405.4249032
    6. EINECS: -0
    7. Product Categories: N/A
    8. Mol File: 1449277-10-4.mol
  • Chemical Properties

    1. Melting Point: N/A
    2. Boiling Point: 734.5±60.0 °C(Predicted)
    3. Flash Point: N/A
    4. Appearance: /
    5. Density: 1.45±0.1 g/cm3(Predicted)
    6. Refractive Index: N/A
    7. Storage Temp.: N/A
    8. Solubility: N/A
    9. PKA: 11.60±0.20(Predicted)
    10. CAS DataBase Reference: GNE-495(CAS DataBase Reference)
    11. NIST Chemistry Reference: GNE-495(1449277-10-4)
    12. EPA Substance Registry System: GNE-495(1449277-10-4)
  • Safety Data

    1. Hazard Codes: N/A
    2. Statements: N/A
    3. Safety Statements: N/A
    4. WGK Germany:
    5. RTECS:
    6. HazardClass: N/A
    7. PackingGroup: N/A
    8. Hazardous Substances Data: 1449277-10-4(Hazardous Substances Data)

1449277-10-4 Usage

Uses

Used in Pharmaceutical Industry:
GNE-495 is used as a therapeutic agent for the treatment of Parkinson's disease and potentially other neurodegenerative disorders due to its ability to inhibit LRRK2 activity and reduce toxic alpha-synuclein aggregates.
Used in Neurodegenerative Research:
GNE-495 is used as a research tool for studying the role of LRRK2 in the pathogenesis of Parkinson's disease and other neurodegenerative conditions, providing insights into the development of novel therapeutic strategies.
Used in Drug Development:
GNE-495 is used as a lead compound in the development of new drugs targeting LRRK2 for the treatment of Parkinson's disease and other neurodegenerative disorders, given its promising pharmacokinetic properties and brain penetration capabilities.

Check Digit Verification of cas no

The CAS Registry Mumber 1449277-10-4 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,4,4,9,2,7 and 7 respectively; the second part has 2 digits, 1 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 1449277-10:
(9*1)+(8*4)+(7*4)+(6*9)+(5*2)+(4*7)+(3*7)+(2*1)+(1*0)=184
184 % 10 = 4
So 1449277-10-4 is a valid CAS Registry Number.

1449277-10-4Downstream Products

1449277-10-4Relevant articles and documents

MAP4K4 regulates integrin-FERM binding to control endothelial cell motility

Vitorino, Philip,Yeung, Stacey,Crow, Ailey,Bakke, Jesse,Smyczek, Tanya,West, Kristina,McNamara, Erin,Eastham-Anderson, Jeffrey,Gould, Stephen,Harris, Seth F.,Ndubaku, Chudi,Ye, Weilan

, p. 425 - 430 (2015/04/14)

Cell migration is a stepwise process that coordinates multiple molecular machineries. Using in vitro angiogenesis screens with short interfering RNA and chemical inhibitors, we define here a MAP4K4-moesin-talin-? 21-integrin molecular pathway that promotes efficient plasma membrane retraction during endothelial cell migration. Loss of MAP4K4 decreased membrane dynamics, slowed endothelial cell migration, and impaired angiogenesis in vitro and in vivo. In migrating endothelial cells, MAP4K4 phosphorylates moesin in retracting membranes at sites of focal adhesion disassembly. Epistasis analyses indicated that moesin functions downstream of MAP4K4 to inactivate integrin by competing with talin for binding to ? 21-integrin intracellular domain. Consequently, loss of moesin (encoded by the MSN gene) or MAP4K4 reduced adhesion disassembly rate in endothelial cells. Additionally, ?± 5? 21-integrin blockade reversed the membrane retraction defects associated with loss of Map4k4 in vitro and in vivo. Our study uncovers a novel aspect of endothelial cell migration. Finally, loss of MAP4K4 function suppressed pathological angiogenesis in disease models, identifying MAP4K4 as a potential therapeutic target.

Structure-Based Design of GNE-495, a Potent and Selective MAP4K4 Inhibitor with Efficacy in Retinal Angiogenesis

Ndubaku, Chudi O.,Crawford, Terry D.,Chen, Huifen,Boggs, Jason W.,Drobnick, Joy,Harris, Seth F.,Jesudason, Rajiv,McNamara, Erin,Nonomiya, Jim,Sambrone, Amy,Schmidt, Stephen,Smyczek, Tanya,Vitorino, Philip,Wang, Lan,Wu, Ping,Yeung, Stacey,Chen, Jinhua,Chen, Kevin,Ding, Charles Z.,Wang, Tao,Xu, Zijin,Gould, Stephen E.,Murray, Lesley J.,Ye, Weilan

, p. 913 - 918 (2015/08/24)

Diverse biological roles for mitogen-activated protein kinase kinase kinase kinase 4 (MAP4K4) have necessitated the identification of potent inhibitors in order to study its function in various disease contexts. In particular, compounds that can be used to carry out such studies in vivo would be critical for elucidating the potential for therapeutic intervention. A structure-based design effort coupled with property-guided optimization directed at minimizing the ability of the inhibitors to cross into the CNS led to an advanced compound 13 (GNE-495) that showed excellent potency and good PK and was used to demonstrate in vivo efficacy in a retinal angiogenesis model recapitulating effects that were observed in the inducible Map4k4 knockout mice.

ISOQUINOLINE AND NAPHTHYRIDINE DERIVATIVES

-

, (2013/08/15)

The invention provides novel compounds having the general formula(I) wherein A, R1 and R2 are as described herein, compositions including the compounds and use of the compounds for inhibiting angiogenesis by inhibition of MAP4K4.

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