Product Name :
HG-10-102-01 — LRRK2 Inhibitor
Description:
HG-10-102-01 is a brain penetrant, potent and selective inhibitor of wild-type LRRK2 and the G2019S mutant (IC50 for LRRK2-wild-type ~20.3 nM and LRRK2-[G2019S] ~3.2 nM). It significantly inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant at a concentration of 0.1−0.3 μM in cells. HG-10-102-01 is the first compound reported to be capable of inhibiting Ser910 and Ser935 phosphorylation in mouse brain following intraperitoneal delivery of doses as low as 50 mg/kg. It may represent a good lead compound for a subset of Parkinson’s disease.
CAS:
1351758-81-0
Molecular Weight:
377.83
Formula:
C17H20ClN5O3
Chemical Name:
(4-((5-chloro-4-(methylamino)pyrimidin-2-yl)amino)-3-methoxyphenyl)(morpholino)methanone
Smiles :
COC1=CC(=CC=C1NC1=NC(NC)=C(Cl)C=N1)C(=O)N1CCOCC1
InChiKey:
YEVOZZZLKJKCCD-UHFFFAOYSA-N
InChi :
InChI=1S/C17H20ClN5O3/c1-19-15-12(18)10-20-17(22-15)21-13-4-3-11(9-14(13)25-2)16(24)23-5-7-26-8-6-23/h3-4,9-10H,5-8H2,1-2H3,(H2,19,20,21,22)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
HG-10-102-01 is a brain penetrant, potent and selective inhibitor of wild-type LRRK2 and the G2019S mutant (IC50 for LRRK2-wild-type ~20.3 nM and LRRK2-[G2019S] ~3.2 nM). It significantly inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant at a concentration of 0.1−0.3 μM in cells. HG-10-102-01 is the first compound reported to be capable of inhibiting Ser910 and Ser935 phosphorylation in mouse brain following intraperitoneal delivery of doses as low as 50 mg/kg. It may represent a good lead compound for a subset of Parkinson’s disease.|Product information|CAS Number: 1351758-81-0|Molecular Weight: 377.83|Formula: C17H20ClN5O3|Chemical Name: (4-((5-chloro-4-(methylamino)pyrimidin-2-yl)amino)-3-methoxyphenyl)(morpholino)methanone|Smiles: COC1=CC(=CC=C1NC1=NC(NC)=C(Cl)C=N1)C(=O)N1CCOCC1|InChiKey: YEVOZZZLKJKCCD-UHFFFAOYSA-N|InChi: InChI=1S/C17H20ClN5O3/c1-19-15-12(18)10-20-17(22-15)21-13-4-3-11(9-14(13)25-2)16(24)23-5-7-26-8-6-23/h3-4,9-10H,5-8H2,1-2H3,(H2,19,20,21,22)|Technical Data|Appearance: Solid Power.{{Dabigatran etexilate} site|{Dabigatran etexilate} Thrombin|{Dabigatran etexilate} Technical Information|{Dabigatran etexilate} Formula|{Dabigatran etexilate} supplier|{Dabigatran etexilate} Epigenetics} |Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO up to 100 mM|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{DREADD agonist 21} web|{DREADD agonist 21} GPCR/G Protein|{DREADD agonist 21} Immunology/Inflammation|{DREADD agonist 21} Technical Information|{DREADD agonist 21} Description|{DREADD agonist 21} custom synthesis} |Shelf Life: ≥12 months if stored properly.PMID:29844565 |Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined.|HS Tariff Code: 382200|How to use|In Vitro:|HG-10-102-01was used at 0.3-1.0 µM final concentration in vitro and in cellular assays.|In Vivo:|HG-10-102-01 was intraperitoneally (IP) dosed to mice at 50 mg/kg once per day.|References:|Choi HG, et al. Brain Penetrant LRRK2 Inhibitorn (2012) ACS Med. Chem. Lett., 2012, 3 (8), 658–662.Chen H, et al. Discovery of Selective LRRK2 Inhibitors Guided by Computational Analysis and Molecular Modeling. (2012) Journal of Medicinal Chemistry. 55(11), 5536-5545.Products are for research use only. Not for human use.|Documents||