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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
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 416.86
Formula C19H21ClN6O3
CAS Number 1700693-08-8
Purity >98%
Solubility DMSO 30 mg/mL
Storage at -20°C
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 2017




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

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