JH-II-127

Modify Date: 2024-01-27 00:18:22

JH-II-127 Structure
JH-II-127 structure
Common Name JH-II-127
CAS Number 1700693-08-8 Molecular Weight 416.861
Density 1.5±0.1 g/cm3 Boiling Point 581.4±60.0 °C at 760 mmHg
Molecular Formula C19H21ClN6O3 Melting Point N/A
MSDS N/A Flash Point 305.4±32.9 °C

 Use of JH-II-127


JH-II-127 is a highly potent, selective, and brain penetrant LRRK2 inhibitor, with IC50 of 6.6 nM, 2.2 nM ,47.7 nM for LRRK2-wild-type, LRRK2-G2019S, LRRK2-A2016T.IC50 value: 2.2 n(LRRK2-G2019S), 6.6 nM(LRRK2-wild-type), 47.7 nM (LRRK2-A2016T)Target: LRRK2JH-II-127 is a potent and selective inhibitor of both wild-type and G2019S mutant LRRK2. JH-II-127 substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant at a concentration of 0.1-0.3 μM in a variety of cell types and is capable of inhibiting Ser935 phosphorylation in mouse brain following oral delivery of doses as low as 30 mg/kg.

 Names

Name (4-{[5-Chloro-4-(methylamino)-3H-pyrrolo[2,3-d]pyrimidin-2-yl]amino}-3-methoxyphenyl)(4-morpholinyl)methanone
Synonym More Synonyms

 JH-II-127 Biological Activity

Description JH-II-127 is a highly potent, selective, and brain penetrant LRRK2 inhibitor, with IC50 of 6.6 nM, 2.2 nM ,47.7 nM for LRRK2-wild-type, LRRK2-G2019S, LRRK2-A2016T.IC50 value: 2.2 n(LRRK2-G2019S), 6.6 nM(LRRK2-wild-type), 47.7 nM (LRRK2-A2016T)Target: LRRK2JH-II-127 is a potent and selective inhibitor of both wild-type and G2019S mutant LRRK2. JH-II-127 substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant at a concentration of 0.1-0.3 μM in a variety of cell types and is capable of inhibiting Ser935 phosphorylation in mouse brain following oral delivery of doses as low as 30 mg/kg.
Related Catalog
References

[1]. Hatcher JM, et al. Discovery of a Pyrrolopyrimidine (JH-II-127), a Highly Potent, Selective, and Brain Penetrant LRRK2 Inhibitor. ACS Med Chem Lett. 2015 Apr 7;6(5):584-589.

 Chemical & Physical Properties

Density 1.5±0.1 g/cm3
Boiling Point 581.4±60.0 °C at 760 mmHg
Molecular Formula C19H21ClN6O3
Molecular Weight 416.861
Flash Point 305.4±32.9 °C
Exact Mass 416.136353
LogP -0.68
Vapour Pressure 0.0±1.6 mmHg at 25°C
Index of Refraction 1.701
Storage condition 2-8℃

 Synonyms

Methanone, [4-[[5-chloro-4-(methylamino)-3H-pyrrolo[2,3-d]pyrimidin-2-yl]amino]-3-methoxyphenyl]-4-morpholinyl-
(4-{[5-Chloro-4-(methylamino)-3H-pyrrolo[2,3-d]pyrimidin-2-yl]amino}-3-methoxyphenyl)(4-morpholinyl)methanone
JH-II-127
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