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PK 11195
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
PK 11195图片
CAS NO:85532-75-8
包装与价格：
包装价格(元)
10mg电议
50mg电议

产品介绍

化学性质

Physical AppearanceA white to off-white solid
StorageStore at RT
M.Wt352.86
Cas No.85532-75-8
FormulaC21H21ClN2O
SolubilitySoluble in DMSO
Chemical Name(R)-N-(sec-butyl)-1-(2-chlorophenyl)-N-methylisoquinoline-3-carboxamide
Canonical SMILESClC1=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。
一般建议为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。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。

资料参考

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.

试验操作

Cell experiment:[2]

Cell lines

Human glioblastoma line U251 and rat glioma line C6

Reaction Conditions

15 min incubation

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).

Note

The technical data provided above is for reference only.

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.