C0424
PK 11195
peripheral benzodiazepine antagonist, powder
别名:
1-（2-氯苯基）-N-甲基-N-（1-甲基丙基）-3-异喹啉羧
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关于此项目
经验公式（希尔记法）:
C21H21ClN2O
CAS Number:
分子量:
352.86
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
Product Name
PK 11195,
表单
powder
质量水平
SMILES字符串
CCC(C)N(C)C(=O)c1cc2ccccc2c(n1)-c3ccccc3Cl
InChI
1S/C21H21ClN2O/c1-4-14(2)24(3)21(25)19-13-15-9-5-6-10-16(15)20(23-19)17-11-7-8-12-18(17)22/h5-14H,4H2,1-3H3
InChI key
RAVIZVQZGXBOQO-UHFFFAOYSA-N
基因信息
human ... BZRAP1(9256), TSPO(706)
rat ... Gabra2(29706), Tspo(24230)
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相关类别
应用
PK 11195 已被用作胚胎原始红细胞和骨肉瘤细胞质杂交体中外周苯二氮卓受体（PBR）类似物的抑制剂。它还被用作心脏组织切片体外放射自显影实验中的未标记竞争性结合剂。
生化/生理作用
PK 11195是一种外周苯二氮卓拮抗剂。它还是人组成型雄烷受体（hCAR）和人孕烷 X 受体（PXR）的拮抗剂。在人原代肝细胞中，PK 11195通过反甲基化诱导对受体hCAR的激动剂功能。PK 11195还是B细胞淋巴瘤2（Bcl-2）的拮抗剂，有望成为线粒体靶向治疗和肝胆管型肝癌治疗的化合物。
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Eryn L Werry et al.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 96, 186-192 (2016-10-28)
The 18kDa translocator protein (TSPO) is a target for novel glioblastoma therapies due to its upregulation in this cancer and relatively low levels of expression in the healthy cortex. The pyrazolo[1,5-a]pyrimidine acetamides, exemplified by DPA-713 and DPA-714, are a class
Soria Iatmanen-Harbi et al.
International journal of molecular sciences, 20(6) (2019-03-25)
The optimization of translocator protein (TSPO) ligands for Positron Emission Tomography as well as for the modulation of neurosteroids is a critical necessity for the development of TSPO-based diagnostics and therapeutics of neuropsychiatrics and neurodegenerative disorders. Structural hints on the
PBRL, a putative peripheral benzodiazepine receptor, in primitive erythropoiesis
Nakazawa F, et al.
Gene Expression Patterns, 9(2), 114-121 (2009)
Justin V Louis et al.
Neuropharmacology, 118, 167-174 (2017-03-21)
Adaptor-associated kinase 1 (AAK1), a member of the Ark1/Prk1 family of serine/threonine kinases, plays a role in modulating clatherin coated endocytosis of specific surface receptors. We have demonstrated that AAK1 inhibitors are efficacious in rodent models of neuropathic pain (Kostich
A Klegeris et al.
Biochemical pharmacology, 59(10), 1305-1314 (2000-03-29)
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 of neurological and other disease states. We explored the functional consequences of
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