85532-75-8

85532-75-8 structure

Name: PK11195
Chemical Name: 1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide
CAS Number: 85532-75-8
Molecular Formula: C₂₁H₂₁ClN₂O
Molecular Weight: 352.857
Catalog: Signaling Pathways Anti-infection Parasite
Create Date: 2018-12-24 16:00:34
Modify Date: 2024-01-03 10:00:33
PK-11195 is a ligand of translocator protein (TSPO), which targets Leishmania chemotherapy, with IC50s of 14.2 μM, 8.2 μM, 3.5 μM for L. amazonensis, L. major and L. braziliensis, respectively.

Name	1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide
Synonyms	N-sec-Butyl-1-(2-chlorophenyl)-N-methyl-3-isoquinolinecarboxamide UNII:YNF83VN1RL MFCD00069334 3-Isoquinolinecarboxamide, 1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)- N-sec-Butyl-1-(2-chlorophenyl)-N-methylisoquinoline-3-carboxamide

Description	PK-11195 is a ligand of translocator protein (TSPO), which targets Leishmania chemotherapy, with IC50s of 14.2 μM, 8.2 μM, 3.5 μM for L. amazonensis, L. major and L. braziliensis, respectively.
Related Catalog	Signaling Pathways >> Anti-infection >> Parasite Research Areas >> Infection
Target	IC50: 14.2 μM (L. amazonensis), 8.2 μM (L. major), 3.5 μM (L. braziliensis)[1].
In Vitro	Median IC50 values for PK-11195 are 14.2 μM for L. amazonensis, 8.2 μM for L. major, and 3.5 μM for L. braziliensis. The selective index value for L. amazonensis is 13.7, indicating the safety of PK-11195 for future testing in mammals. Time-and dose-dependent reductions in the percentage of infected macrophages, the number of parasites per infected macrophage, and the number of viable intracellular parasites are observed. Electron microscopy reveals some morphological alterations suggestive of autophagy. Interestingly, MCP-1 and superoxide levels are reduced in L. amazonensis-infected macrophages treated with PK-11195[1].
References	[1]. Guedes CES, et al. In vitro evaluation of the anti-leishmanial activity and toxicity of PK-11195. Mem Inst Oswaldo Cruz. 2018 Feb 5;113(4):e170345.

CHEMICAL NAME :: 3-Isoquinolinecarboxamide, 1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-

REFERENCE :: CALEDQ Cancer Letters (Shannon, Ireland). (Elsevier Scientific Pub. Ireland Ltd., POB 85, Limerick, Ireland) V.1- 1975- Volume(issue)/page/year: 49,115,1990

RIDADR	NONH for all modes of transport
WGK Germany	3
RTECS	NW6987000

124236-61-9

74-88-4

~84%

85532-75-8

541-41-3

774152-11-3

89242-09-1

85532-75-8

Literature: US4499094 A1, ;