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AB120378

PK11195, benzodiazepine receptor antagonist

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(2 Publications)

MW 352.9 Da, Purity >99%. Antagonist at the mitochondrial (peripheral) benzodiazepine receptor (translocator protein, TSPO). Acts as a chemosensitizer of tumor cells to a wide range of chemotherapeutic agents.

View Alternative Names

BPBS, BZRP, Benzodiazapine receptor (peripheral), Benzodiazepine peripheral binding site, IBP, Isoquinoline carboxamide-binding protein, MBR, Mitochondrial benzodiazepine receptor, PKBS, PTBR, PTBZR02, Peripheral benzodiazepine receptor, Peripheral benzodiazepine receptor-related protein, Peripheral-type benzodiazepine receptor, Ptbzr, RATPTBZR02, TSPOA_HUMAN, Translocator protein, Tspo1, mDRC, pk18, translocator protein (18kDa)

1 Images
Chemical Structure - PK11195, benzodiazepine receptor antagonist (AB120378)
  • Chemical Structure

Lab

Chemical Structure - PK11195, benzodiazepine receptor antagonist (AB120378)

2D chemical structure image of ab120378, PK11195, benzodiazepine receptor antagonist

Key facts

CAS number

85532-75-8

Purity

>99%

Form

Solid

form

Molecular weight

352.9 Da

Molecular formula

C<sub>2</sub><sub>1</sub>H<sub>2</sub><sub>1</sub>ClN<sub>2</sub>O

PubChem

1345

Nature

Synthetic

Solubility

Soluble in DMSO to 100 mM

Soluble in ethanol to 50 mM

Biochemical name

1-(2-Chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide

Biological description

Antagonist at the mitochondrial (peripheral) benzodiazepine receptor (translocator protein, TSPO). Acts as a chemosensitizer of tumor cells to a wide range of chemotherapeutic agents.

Canonical smiles

CCC(C)N(C)C(=O)C1=CC2=CC=CC=C2C(=N1)C3=CC=CC=C3Cl

InChi

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

InChiKey

RAVIZVQZGXBOQO-UHFFFAOYSA-N

IUPAC Name

N-butan-2-yl-1-(2-chlorophenyl)-N-methylisoquinoline-3-carboxamide

Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
Ambient
Appropriate long-term storage conditions
Ambient
Storage information
The product can be stored for up to 12 months
Handling instructions

Need more advice on solubility, usage and handling? Please visit our our product support page for more details.

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Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

PBR also known as the Peripheral Benzodiazepine Receptor is a protein predominantly found in the outer mitochondrial membrane. It has alternate names like Translocator Protein (TSPO) and the mass of this protein is approximately 18 kDa. PBR is expressed in various tissues but shows high levels in steroidogenic tissues like adrenal glands as well as in the brain heart liver and kidneys. The abundant presence in these tissues highlights its importance in a variety of physiological functions.
Biological function summary

PBR interacts with cholesterol for the synthesis of steroid hormones making it important for steroidogenesis. PBR is a part of the Mitochondrial Permeability Transition Pore complex (MPTP) involved in regulating the transport of molecules across the mitochondrial membrane. Through its association with the MPTP PBR plays a significant role in mitochondrial functions such as apoptosis and energy metabolism. The interaction with other molecules also includes the binding with benzodiazepines impacting processes like immune response and cell proliferation.

Pathways

PBR plays a role in the steroid biosynthesis and apoptosis pathways. It interfaces with the StAR (Steroidogenic Acute Regulatory) protein to facilitate cholesterol transport into mitochondria the initial step in steroid hormone production. PBR is also involved in pathways that regulate apoptosis and mitochondrial function linking it to different cellular processes through interactions with proteins like VDAC (Voltage-Dependent Anion Channel).

PBR has relevance to conditions such as neurodegenerative diseases and cancer. PBR expression changes in disorders like Alzheimer's disease where it might reflect mitochondrial dysfunctions. It has also been associated with certain cancers where aberrant PBR activity might contribute to altered cell proliferation and apoptosis. Proteins like caspases are involved in the apoptotic pathways connected with PBR highlighting its involvement in disease processes.

Product protocols

Publications (2)

Recent publications for all applications. Explore the full list and refine your search

Journal of translational medicine 21:71 PubMed36732752

2023

The soluble epoxide hydrolase inhibitor TPPU improves comorbidity of chronic pain and depression via the AHR and TSPO signaling.

Applications

Unspecified application

Species

Unspecified reactive species

Ailin Luo,Zifeng Wu,Shan Li,Cindy B McReynolds,Di Wang,Hanyu Liu,Chaoli Huang,Teng He,Xinying Zhang,Yuanyuan Wang,Cunming Liu,Bruce D Hammock,Kenji Hashimoto,Chun Yang

Journal of cerebral blood flow and metabolism : of 35:1331-8 PubMed25833342

2015

[11C]PBR28 PET imaging is sensitive to neuroinflammation in the aged rat.

Applications

Unspecified application

Species

Unspecified reactive species

Matthew D Walker,Katherine Dinelle,Rick Kornelsen,Nathan V Lee,Qing Miao,Mike Adam,Christine Takhar,Edwin Mak,Michael Schulzer,Matthew J Farrer,Vesna Sossi
View all publications

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