ChemicalBook > CAS DataBase List > [4-[[5-Chloro-4-(MethylaMino)-2-pyriMidinyl]aMino]-3-Methoxyphenyl]-4-MorpholinylMethanone

[4-[[5-Chloro-4-(MethylaMino)-2-pyriMidinyl]aMino]-3-Methoxyphenyl]-4-MorpholinylMethanone

[4-[[5-Chloro-4-(MethylaMino)-2-pyriMidinyl]aMino]-3-Methoxyphenyl]-4-MorpholinylMethanone Structure
[4-[[5-Chloro-4-(MethylaMino)-2-pyriMidinyl]aMino]-3-Methoxyphenyl]-4-MorpholinylMethanone
  • CAS No.1351758-81-0
  • Chemical Name:[4-[[5-Chloro-4-(MethylaMino)-2-pyriMidinyl]aMino]-3-Methoxyphenyl]-4-MorpholinylMethanone
  • CBNumber:CB42653826
  • Molecular Formula:C17H20ClN5O3
  • Formula Weight:377.83
  • MOL File:1351758-81-0.mol
[4-[[5-Chloro-4-(MethylaMino)-2-pyriMidinyl]aMino]-3-Methoxyphenyl]-4-MorpholinylMethanone Property
  • Boiling point 641.1±65.0 °C(Predicted)
  • Density 1.381±0.06 g/cm3(Predicted)
  • storage temp. Store at -20°C
  • solubility insoluble in H2O; ≥18.9 mg/mL in DMSO; ≥7.64 mg/mL in EtOH with ultrasonic
  • form solid
  • pka 4.60±0.10(Predicted)
  • color White to off-white
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal wordWarning
  • Hazard statements H302-H315-H319-H335
  • Precautionary statements P261-P305+P351+P338

[4-[[5-Chloro-4-(MethylaMino)-2-pyriMidinyl]aMino]-3-Methoxyphenyl]-4-MorpholinylMethanone Chemical Properties,Usage,Production

  • Description HG-10-102-01 is an inhibitor of leucine-rich repeat kinase 2 (LRRK2; IC50 = 20.3 nM). It also inhibits the G2019S, A2016T, and [G2019S+A2016T] mutants of LRRK2 (IC50s = 3.2, 153, and 95.9 nM, respectively). HG-10-102-01 substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type and G2019S mutant LRRK2 in cells. When given intraperitoneally, HG-10-102-01 penetrates the blood-brain barrier and inhibits phosphorylation of LRRK2 in the brain as well as the kidney and spleen.
  • Uses [4-[[5-Chloro-4-(methylamino)-2-pyrimidinyl]amino]-3-methoxyphenyl]-4-morpholinylmethanone is an aminopyrimidine derivative as LRRK2 modulators used for the treatment of Parkinson''s disease.
  • Definition ChEBI: HG-10-102-01 is a monocarboxylic acid amide resulting from the formal condensation of the carboxy group of 4-{[5-chloro-4-(methylamino)pyrimidin-2-yl]amino}-3-methoxybenzoic acid with the amino group of morpholine. It is an inhibitor of leucine-rich repeat kinase 2 (LRRK2). It has a role as an EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor. It is an aminopyrimidine, a member of morpholines, a monocarboxylic acid amide, an organochlorine compound, a secondary amino compound and an aromatic ether.
  • in vivo

    HG-10-102-01 (0-100 mg/kg, IP, once) shows inhibition of LRRK2 Ser910/Ser935 phosphorylation in kidney, spleen, and brain of mice[1].
    HG-10-102-01 (1 mg/kg, IV; 10 mg/kg, PO; once) shows good oral bioavailability (%F = 67), a short half-life of 0.13 h, and low plasma exposure[1].

    Animal Model:Wild type male C57BL/6 mice[1]
    Dosage:0, 3, 10, 30, 50, and 100 mg/kg
    Administration:IP, once
    Result:Showed near complete dephosphorylation of Ser910 and Ser935 of LRRK2 in all tissues including brain at 100 mg/kg and 50 mg/kg, but only partial inhibition in brain at the 30 and 10 mg/kg doses.
    Animal Model:Wild type male C57BL/6 mice[1]
    Dosage:1 mg/kg (IV); 10 mg/kg (PO)
    Administration:IV, PO; once (Pharmacokinetic Analysis)
    Result:Pharmacokinetic Parameters of HG-10-102-01 in male C57BL/6 mice[1].
    IV (1 mg/kg)PO (10 mg/kg)
    Tmax (h)0.25
    Cmax (ng/mL)13301241
    AUClast (ng/mL?h)74.85502.34
    AUCINF (ng/mL?h)75.06503.41
    T1/2 (h)0.13
    CL (mL/min/kg)222.04
    Vss (L/kg)1.68
    F (%)67
  • References [1] choi hg1, zhang j, deng x, hatcher jm, patricelli mp, zhao z, alessi dr, gray ns. brain penetrant lrrk2 inhibitor. acs med chem lett. 2012 aug 9;3(8):658-662. epub 2012 jun 18.
[4-[[5-Chloro-4-(MethylaMino)-2-pyriMidinyl]aMino]-3-Methoxyphenyl]-4-MorpholinylMethanone Preparation Products And Raw materials
Raw materials
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[4-[[5-Chloro-4-(MethylaMino)-2-pyriMidinyl]aMino]-3-Methoxyphenyl]-4-MorpholinylMethanone Suppliers
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[4-[[5-Chloro-4-(MethylaMino)-2-pyriMidinyl]aMino]-3-Methoxyphenyl]-4-MorpholinylMethanone Spectrum
1351758-81-0, [4-[[5-Chloro-4-(MethylaMino)-2-pyriMidinyl]aMino]-3-Methoxyphenyl]-4-MorpholinylMethanoneRelated Search:
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  • 抑制剂
  • 合成有机化合物配体
  • 化合物HG-10-102-01,10 MM DMSO 溶液
  • (4-((5-氯-4-(甲氨基)嘧啶-2-基)氨基)-3-甲氧基苯基)(吗啉代)甲酮
  • 化合物HG-10-102-01
  • (4-((5-氯-4-(甲氨基)嘧啶-2-基)氨基)-3-甲氧基苯基)(吗啉)甲酮
  • [4-[[5-氯-4-(甲基氨基)-2-嘧啶基]氨基]-3-甲氧基苯基]-4-吗啉基甲酮
  • 1351758-81-0
  • HG-10-102-01, 10 mM in DMSO
  • Parkinson’s disease,Leucine-rich repeat kinase 2,inhibit,Ser910,BBB,HG 10 102 01,Radiosynthesis,Mouse embryonic fibroblast cells,Mouse Swiss 3T3 cells,MAP kinase interacting kinase,Ser935,MNK,Mitogen activated protein kinase interacting kinase,HG1010201,PET,Inhibitor,MAPK interacting kinase,HEK293 cells,LRRK2,Positron emission tomography
  • LRRK2 INHIBITOR 1
  • CS-949
  • Methanone, [4-[[5-chloro-4-(methylamino)-2-pyrimidinyl]amino]-3-methoxyphenyl]-4-morpholinyl-
  • (4-((5-chloro-4- (methylamino)pyrimidin-2-yl)amino)- 3- methoxyphenyl)(morpholino)methano ne
  • HG-10-102-01
  • [4-[[5-Chloro-4-(MethylaMino)-2-pyriMidinyl]aMino]-3-Methoxyphenyl]-4-MorpholinylMethanone

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