PK 11195
PK 11195 is a ligand of the peripheral translocator protein (TSPO) which was previously known as the peripheral benzodiazepine receptor. PK 11195 binds to TSPO with selectivity and high affinity (Ki = 3.1 nM in cerebellum, 4.1 nM in spinal cord), capable of blocking binding of typical benzodiazepines to TSPO. TSPO, a protein primarily localized in the outer mitochondrial membrane, is present in many peripheral tissues but highly enriched in steroid-synthesizing tissues including the brain, based on which the binding of labeled PK 11195 to tissues is used to detect the presence of TSPO and discriminate the central benzodiazepine receptor from TSPO.?
References:
1.?Watanabe Y, Shibuya T, Khatami S, et al. Comparison of typical and atypical benzodiazepines on the central and peripheral benzodiazepine receptors. The Japanese Journal of Pharmacology, 1986, 42(2): 189-197.
2.?Olson JM, Junck L, Young AB, et al. Isoquinoline and peripheral-type benzodiazepine binding in gliomas: implications for diagnostic imaging. Cancer Research, 1988, 48(20): 5837-5841.
3.?Pike VW, Halldin C, Crouzel C, et al. Radioligands for PET studies of central benzodiazepine receptors and PK (peripheral benzodiazepine) binding sites--current status. Nuclear Medicine and Biology, 1993, 20(4): 503-525.
4. Rupprecht R, Papadopoulos V, Rammes G, et al. Translocator protein (18 kDa) (TSPO) as a therapeutic target for neurological and psychiatric disorders. Nature Reviews Drug Discovery, 2010, 9: 971-988.
| Physical Appearance | A white to off-white solid |
| Storage | Store at RT |
| M.Wt | 352.86 |
| Cas No. | 85532-75-8 |
| Formula | C21H21ClN2O |
| Solubility | Soluble in DMSO |
| Chemical Name | (R)-N-(sec-butyl)-1-(2-chlorophenyl)-N-methylisoquinoline-3-carboxamide |
| SDF | Download SDF |
| Canonical SMILES | ClC1=CC=CC=C1C2=C(C=CC=C3)C3=CC(C(N(C)[C@H](C)CC)=O)=N2 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment:[2] | |
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Cell lines |
Human glioblastoma line U251 and rat glioma line C6 |
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Reaction Conditions |
15 min incubation |
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Applications |
In human and rat glioma cell cultures, [3H]PK 11195 bound with higher affinity (Kd = 14.0 and 15.8 nM, respectively) than either Ro5-4864 (Ki = 1204 and 84.9 nM, respectively) or flunitrazepam (Ki > 10,000 and = 848 nM, respectively). |
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Note |
The technical data provided above is for reference only. |
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References: 1. Watanabe Y, Shibuya T, Khatami S, et al. Comparison of typical and atypical benzodiazepines on the central and peripheral benzodiazepine receptors. The Japanese Journal of Pharmacology, 1986, 42(2): 189-197. 2. Olson JM, Junck L, Young AB, et al. Isoquinoline and peripheral-type benzodiazepine binding in gliomas: implications for diagnostic imaging. Cancer Research, 1988, 48(20): 5837-5841. 3. Pike VW, Halldin C, Crouzel C, et al. Radioligands for PET studies of central benzodiazepine receptors and PK (peripheral benzodiazepine) binding sites--current status. Nuclear Medicine and Biology, 1993, 20(4): 503-525. 4. Rupprecht R, Papadopoulos V, Rammes G, et al. Translocator protein (18 kDa) (TSPO) as a therapeutic target for neurological and psychiatric disorders. Nature Reviews Drug Discovery, 2010, 9: 971-988. |
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Quality Control & MSDS
- View current batch:
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Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
Chemical structure
