tBPC是一种具有选择性的Y4受体正向变构调节剂。
Cas No.:1942-71-8
Sample solution is provided at 25 µL, 10mM.
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tBPC is a selective positive allosteric modulator of the Y4 receptor. tBPC enhances the activation of the Y4 receptor in G protein signaling and arrestin3 recruitment, thereby potentiating the Y4R responses to pancreatic polypeptide, neuropeptide Y, and peptide YY, while maintaining specificity by selectively modulating the Y4 receptor without affecting the Y1, Y2, or Y5 receptors[1].
In vitro, treatment of COS7 cells and HEK293 cells with tBPC (5.1μM-30μM) for 30 minutes enhances the activation effect of Polypeptide and other peptides (NPY, PYY) on Y4R, as well as the rate of arrestin3 recruitment[1].
References:
[1] Schubert M, Stichel J, Du Y, et al. Identification and Characterization of the First Selective Y4 Receptor Positive Allosteric Modulator. J Med Chem. 2017 Sep 14;60(17):7605-7612.
tBPC是一种具有选择性的Y4受体正向变构调节剂。tBPC可增强Y4受体在G蛋白信号传导和arrestin3招募中的激活作用来增强胰腺多肽、神经肽Y和肽YY的Y4R反应，同时通过选择性调节Y4受体而不影响Y1、Y2或Y5受体以维持特异性[1]。
在体外，tBPC（5.1μM-30μM）处理COS7细胞和HEK293细胞30分钟。tBPC处理能增强Polypeptide和其它肽段（NPY，PYY）对Y4R的激活效应，和arrestin3招募速率[1]。
| Cell experiment [1]: | |
Cell lines | COS7 cells stably transfected with human Y4R-eYFP and chimeric △6Gαqi4-myr G-protein; HEK293 cells transiently expressing Y4R-Rluc8 and venus-arrestin3 fusion proteins; Mouse descending colon mucosa endogenously expressing Y4R. |
Preparation Method | For Ca²⁺ flux assays, transfected COS7 cells were seeded in plates and loaded with Fluo2-AM dye. For arrestin3 recruitment BRET assays, transfected HEK293 cells were seeded in plates and incubated with coelenterazine H. Cells tBPC (5.1μM-30μM) for 30 minutes. |
Reaction Conditions | 5.1-30µM; incubation for 30 min. |
Applications | tBPC potentiated Y4R activation by its native ligand Pancreatic Polypeptide (PP) and other peptide ligands (NPY, PYY) in both G-protein-mediated Ca²⁺ signaling and arrestin3 recruitment pathways. tBPC acted as a positive allosteric modulator (PAM) and displayed weak agonistic activity in overexpressing systems. |
References: | |
| Cas No. | 1942-71-8 | SDF | |
| 别名 | 2-(4-叔丁基苯氧基)环己醇 | ||
| 化学名 | 2-[4-(1,1-Dimethylethyl)phenoxy]cyclohexanol | ||
| Canonical SMILES | CC(C)(C1=CC=C(C=C1)OC2CCCCC2O)C | ||
| 分子式 | C16H24O2 | 分子量 | 248.36 |
| 溶解度 | 24.84mg/ml in DMSO, 24.84mg/ml in Ethanol | 储存条件 | Store at 4℃ |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.0264 mL | 20.1321 mL | 40.2641 mL |
| 5 mM | 805.3 μL | 4.0264 mL | 8.0528 mL |
| 10 mM | 402.6 μL | 2.0132 mL | 4.0264 mL |
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动物数量 | 只 |
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2.
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- Purity: >98.00% Appearance: A solid
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