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

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CAS:1351758-81-0
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Products Intro: Product Name:[4-[[5-Chloro-4-(MethylaMino)-2-pyriMidinyl]aMino]-3-Methoxyphenyl]-4-MorpholinylMethanone
CAS:1351758-81-0
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CAS:1351758-81-0
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Products Intro: Product Name:[4-[[5-Chloro-4-(MethylaMino)-2-pyriMidinyl]aMino]-3-Methoxyphenyl]-4-MorpholinylMethanone
CAS:1351758-81-0
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Products Intro: Product Name:HG-10-102-01
CAS:1351758-81-0

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

  • HG-10-102-01
  • HG-10-102-01 pictures
  • $53.00 / 5mg
  • 2026-04-21
  • CAS:1351758-81-0
  • Min. Order:
  • Purity: 99.73%
  • Supply Ability: 10g
[4-[[5-Chloro-4-(MethylaMino)-2-pyriMidinyl]aMino]-3-Methoxyphenyl]-4-MorpholinylMethanone Basic information
Product Name:[4-[[5-Chloro-4-(MethylaMino)-2-pyriMidinyl]aMino]-3-Methoxyphenyl]-4-MorpholinylMethanone
Synonyms:[4-[[5-Chloro-4-(MethylaMino)-2-pyriMidinyl]aMino]-3-Methoxyphenyl]-4-MorpholinylMethanone;HG-10-102-01;(4-((5-chloro-4- (methylamino)pyrimidin-2-yl)amino)- 3- methoxyphenyl)(morpholino)methano ne;LRRK2 INHIBITOR 1;CS-949;Methanone, [4-[[5-chloro-4-(methylamino)-2-pyrimidinyl]amino]-3-methoxyphenyl]-4-morpholinyl-;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;HG-10-102-01, 10 mM in DMSO
CAS:1351758-81-0
MF:C17H20ClN5O3
MW:377.83
EINECS:
Product Categories:Amines, Aromatics, Heterocycles, Pharmaceuticals, Intermediates & Fine Chemicals;Amines;Aromatics;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;API
Mol File:1351758-81-0.mol
[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 Chemical Properties
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
pka4.60±0.10(Predicted)
color White to off-white
Safety Information
MSDS Information
[4-[[5-Chloro-4-(MethylaMino)-2-pyriMidinyl]aMino]-3-Methoxyphenyl]-4-MorpholinylMethanone Usage And Synthesis
DescriptionHG-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.
DefinitionChEBI: 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/mLh)74.85502.34
AUCINF (ng/mLh)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 materialsMethanone, (3-methoxy-4-nitrophenyl)-4-morpholinyl--->4-Amino-3-methoxybenzoic acid-->3-Methoxy-4-nitrobenzoic acid-->2,5-dichloro-n-MethylpyriMidin-4-aMine
Tag:[4-[[5-Chloro-4-(MethylaMino)-2-pyriMidinyl]aMino]-3-Methoxyphenyl]-4-MorpholinylMethanone(1351758-81-0) Related Product Information
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