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제품정보 (DICE 배송 시 비용 별도)
실험식(Hill 표기법):
C21H21ClN2O
CAS 번호:
Molecular Weight:
352.86
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
Form:
powder
Quality level:
제품 이름
PK 11195,
form
powder
Quality Level
SMILES string
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
Gene Information
human ... BZRAP1(9256), TSPO(706)
rat ... Gabra2(29706), Tspo(24230)
Application
PK 11195 has been used as an inhibitor of peripheral benzodiazepine receptor (PBR) homologs in primitive erythrocytes of embryos and in osteosarcoma cytoplasmic hydrids. It has also been used as an unlabelled competitive binder in in vitro autoradiography experiments in cardiac tissue sections.
Biochem/physiol Actions
PK 11195 is a peripheral benzodiazepine antagonist. It is also an antagonist for human constitutive androstane receptor (hCAR) and human pregnane X receptor (PXR). In human primary hepatocytes, PK 11195 upon demethylation elicits agonist functionality towards the receptor hCAR. PK 11195 also antagonise B-cell lymphoma 2 (Bcl-2) and may serve as a potential compound for mitochondrial targeting therapies and in the treatment of cholangiocarcinoma.
저장 등급
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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
Molecular basis of metabolism-mediated conversion of PK11195 from an antagonist to an agonist of the constitutive androstane receptor
Mackowiak B, et al.
Molecular Pharmacology, 92(1), 75-87 (2017)
Ségolène Hescot et al.
Oncotarget, 8(66), 109924-109940 (2018-01-05)
Mitotane (o,p'DDD), the most effective drug in adrenocortical carcinoma, concentrates into the mitochondria and impacts mitochondrial functions. To address the molecular mechanisms of mitotane action and to identify its potential target, metabolomic and lipidomic approaches as well as imaging analyses
국제 무역 품목 번호
| SKU | GTIN |
|---|---|
| C0424-10MG | 04061832556116 |
| C0424-50MG | 04061832556123 |