A high affinity ligand for peripheral benzodiazepine receptor, TSPO
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Product Type

Small Molecule Modulators
Receptor Pharmacology

Research Area

Neuroscience

PK11195

Item No. 10525

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide
CAS Number
85532-75-8
Synonyms
  • RP 52028
Molecular Formula
C21H21ClN2O
Formula Weight
352.9
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: 10 mg/mlChloroform: 33 mg/mlMethanol: 16 mg/ml
λmax
224 nm
SMILES
ClC1=CC=CC=C1C2=NC(C(N(C)C(C)CC)=O)=CC3=CC=CC=C32
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    10 mg

    $90

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    50 mg

    $306

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    Product Description

    Benzodiazepines bind two types of receptors, the central γ-aminobutyric acid A receptor and the peripheral translocator protein (TSPO). PK11195 binds the peripheral benzodiazepine receptor, TSPO, with selectivity and high affinity (Ki = 3.1 nM in cerebellum, 4.1 nM in spinal cord).1,2 PK11195, which lacks the 7-member heterocycle of diazepines, blocks binding of typical benzodiazepines to TSPO.1 In addition, the binding of labeled PK11195 to tissues is used to detect the presence of TSPO by various methods.2,3 PK11195 has been used to study the ligand binding site of the B. cereus TSPO.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Watanabe, Y., Shibuya, T., Khatami, S., et al. Comparison of typical and atypical benzodiazepines on the central and peripheral benzodiazepine receptors. Jpn. J. Pharmacol. 42(2), 189-197 (1986).

    2. Pike, V.W., Halldin, C., Crouzel, C., et al. Radioligands for PET studies of central benzodiazepine receptors and PK (peripheral benzodiazepine) binding sites-current status. Nucl. Med. Biol. 20(4), 503-525 (1993).

    3. Olson, J.M.M., Junck, L., Young, A.B., et al. Isoquinoline and peripheral-type benzodiazepine binding in gliomas: Implications for diagnostic imaging. Cancer Res. 48(20), 5837-5841 (1988).

    4. Guo, Y., Kalathur, R.C., Liu, Q., et al. Protein structure. Structure and activity of tryptophan-rich TSPO proteins. Science 347(6221), 551-555 (2015).