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2942328-06-3

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2942328-06-3 Structure

Identification	Back Directory
[Name] LRRK2-IN-14
[CAS] 2942328-06-3
[Synonyms] LRRK2-IN-14
[Molecular Formula] C17H18F3N5O2
[MOL File] 2942328-06-3.mol
[Molecular Weight] 381.35

Chemical Properties	Back Directory
[Boiling point ] 484.8±55.0 °C(predicted)
[density ] 1.43±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted)
[pka] 3.30±0.20(predicted)

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[Uses]

LRRK2-IN-14 (Compound 8) is an orally active LRRK2 inhibitor. LRRK2-IN-14 has an IC50 of 6.3 nM for LRRK2(G2019S) cell activity.LRRK2-IN-14 has an inhibitory effect on hERG (IC50=22 μM). LRRK2-IN-14 has blood-brain barrier permeability[1].

[in vivo]

LRRK2-IN-14 (30 mg/kg; p.o.; single dose) inhibits phosphorylation of G2019S mutant LRRK2 in the brain in ICR mice^[1].

Pharmacokinetic Analysis in ICR mice^[1]

Route	Dose (mg/kg)	C₀ (ng/mL)	C_max (ng/mL)	T_max (h)	t_1/2 (h)	Vd_ss (mL/kg)	Cl_obs (mL/min/kg)	AUC_0-last (ng·h/mL)	AUC_0-INF (ng·h/mL)	MRT_0-INF (h)	F (%)
i.v.	5	4101	/	/	0.905	1233	16.3	5122	5181	1.27	/
p.o.	5	/	2803	0.083	0.709	/	/	3657	3672	1.22	70.9
brain	5	/	837	0.292	0.648	/	/	1230	1233	1.14	/

Animal Model:	ICR mice^[1]
Dosage:	30 mg/kg
Administration:	p.o.; single dose
Result:	Reduced phosphorylated LRRK2 levels to 34%.

[References]

[1] Kim K, et al. Concurrent Optimizations of Efficacy and Blood-Brain Barrier Permeability in New Macrocyclic LRRK2 Inhibitors for Potential Parkinson's Disease Therapeutics. J Med Chem. 2024 May 9;67(9):7647-7662. DOI:10.1021/acs.jmedchem.4c00520

2942328-06-3 suppliers list

Company Name:	TargetMol Chemicals Inc.
Tel:	15002134094
Website:	https://www.targetmol.cn/

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