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PK-11195

PK-11195用途

PK-11195 是 TSPO 的一个配体,可靶向治疗利什曼病,其对 L. amazonensis,L. major 和 L. braziliensis 的 IC50 值分别为 14.2 μM, 8.2 μM, 3.5 μM。

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PK-11195名称

[ CAS 号 ]:
85532-75-8

[ 中文名 ]:
1-(2-氯苯基)-n-甲基-n-(1-甲基丙基)-3-异喹啉羧酰胺

[ 英文名 ]:
PK11195

[英文别名 ]:

UNII:YNF83VN1RL
MFCD00069334

PK-11195生物活性

[ 描述 ]:

PK-11195 是 TSPO 的一个配体,可靶向治疗利什曼病,其对 L. amazonensis,L. major 和 L. braziliensis 的 IC50 值分别为 14.2 μM, 8.2 μM, 3.5 μM。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 寄生物

研究领域 >> 感染

[ 靶点 ]

IC50: 14.2 μM (L. amazonensis), 8.2 μM (L. major), 3.5 μM (L. braziliensis)[1].

[体外研究]

对于亚马逊酵母,PK-11195的中位IC50值为14.2μM,对于L. major为8.2μM,对于L.braziliensis为3.5μM。亚马逊酵母的选择性指数值为13.7,表明PK-11195在哺乳动物未来测试中的安全性。观察到感染的巨噬细胞的百分比,每个感染的巨噬细胞的寄生虫数量和活细胞内寄生虫的数量的时间和剂量依赖性降低。电子显微镜显示一些暗示自噬的形态学改变。有趣的是,用PK-11195处理的亚马逊感染巨噬细胞中MCP-1和超氧化物水平降低[1]。

[参考文献]

[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.

[相关活性小分子]

PK-11195物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
511.7±45.0 °C at 760 mmHg

[ 熔点 ]:
74-75

[ 分子式 ]:
C₂₁H₂₁ClN₂O

[ 分子量 ]:
352.857

[ 闪点 ]:
263.3±28.7 °C

[ 精确质量 ]:
352.134247

[ PSA ]:
33.20000

[ LogP ]:
4.58

[ 蒸汽压 ]:
0.0±1.3 mmHg at 25°C

[ 折射率 ]:
1.611

[ 储存条件 ]:
Store at RT

PK-11195MSDS

详细MSDS(安全技术说明书)

PK-11195毒性和生态

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

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PK-11195安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
NW6987000

PK-11195合成路线

详细合成路线

PK-11195上下游产品

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PK-11195文献

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...

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