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JH-II-127

Cat. No. M5204
JH-II-127 Structure
Size Price Availability Quantity
5mg USD 150  USD150 In stock
10mg USD 240  USD240 In stock
50mg USD 720  USD720 In stock
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Quality Control & Documentation
Biological Activity

JH-II-127 is a highly selective LRRK2 inhibitor with an IC50 = 6.5 nM.

In vitro: At a concentration of 1 μM, JH-II-127 only inhibited the kinase activities of SmMLCK and CHK2 to greater than 90% of the DMSO control (complete results presented in the Supporting Information). Dose–response analysis revealed inhibition of SmMLCK with an IC50 = 81.3 nM and CHK2 with an IC50 = 27.6 nM.

In vivo: JH-II-127 can inhibit phosphorylation of Ser935 of LRRK2 in brain and peripheral tissues following intraperitoneal doses of 30 mg/kg.

Chemical Information
Molecular Weight 416.86
Formula C19H21ClN6O3
CAS Number 1700693-08-8
Solubility (25°C) DMSO 30 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Hatcher JM, et al. ACS Med Chem Lett. Discovery of a Pyrrolopyrimidine (JH-II-127), a Highly Potent, Selective, and Brain Penetrant LRRK2 Inhibitor.

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  Catalog
Abmole Inhibitor Catalog




Keywords: JH-II-127 supplier, LRRK2, inhibitors, activators


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