PK 11195
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 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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质量控制和MSDS
- View current batch:
-
Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
化学结构
