PK11195

Modify Date: 2024-01-03 10:00:33

PK11195 Structure
PK11195 structure
Common Name PK11195
CAS Number 85532-75-8 Molecular Weight 352.857
Density 1.2±0.1 g/cm3 Boiling Point 511.7±45.0 °C at 760 mmHg
Molecular Formula C21H21ClN2O Melting Point 74-75
MSDS Chinese USA Flash Point 263.3±28.7 °C

 Use of PK11195


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.

 Names

Name 1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide
Synonym More Synonyms

 PK11195 Biological Activity

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
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 & Physical Properties

Density 1.2±0.1 g/cm3
Boiling Point 511.7±45.0 °C at 760 mmHg
Melting Point 74-75
Molecular Formula C21H21ClN2O
Molecular Weight 352.857
Flash Point 263.3±28.7 °C
Exact Mass 352.134247
PSA 33.20000
LogP 4.58
Vapour Pressure 0.0±1.3 mmHg at 25°C
Index of Refraction 1.611
Storage condition Store at RT

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
NW6987000
CHEMICAL NAME :
3-Isoquinolinecarboxamide, 1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-
CAS REGISTRY NUMBER :
85532-75-8
LAST UPDATED :
199612
DATA ITEMS CITED :
2
MOLECULAR FORMULA :
C21-H21-Cl-N2-O
MOLECULAR WEIGHT :
352.89

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

TYPE OF TEST :
Unscheduled DNA synthesis
TEST SYSTEM :
Rodent - mouse Fibroblast
DOSE/DURATION :
1 nmol/L
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

 Safety Information

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

 Articles4

More Articles
Inhibitory action of 1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxam ide (PK 11195) on some mononuclear phagocyte functions.

Biochem. Pharmacol. 59 , 1305-1314, (2000)

Peripheral benzodiazepine receptors (PBRs) are widely distributed throughout the body, but their functions are unknown. They are found on mononuclear phagocytes, and they are up-regulated in a number ...

Chronic exposure of rat primary astrocyte cultures to manganese results in increased binding sites for the 'peripheral-type' benzodiazepine receptor ligand 3H-PK 11195.

Neurosci. Lett. 271 , 5, (1999)

Alterations of 'peripheral-type' benzodiazepine receptors (PTBRs) in brain are a feature of hepatic encephalopathy (HE). Although ammonia toxicity has been implicated in the disorder, recent findings ...

Pharmacokinetics of the peripheral benzodiazepine receptor antagonist, PK 11195, in rats. The effect of dose and gender.

Pharmacol. Res. 41 , 461-468, (2000)

In spite of the extensive use of the peripheral benzodiazepine (BZ) receptor antagonist, PK 11195 (PK), in pharmacological studies, there is a lack of information of its pharmacokinetics in the rat. I...

 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
Top Suppliers:I want be here




Get all suppliers and price by the below link:

PK11195 suppliers

PK11195 price