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SBI-553 {[allProObj[0].p_purity_real_show]}

货号:A1216662

SBI-553是一种有效且可穿透大脑的 NTR1 的变构调节剂,EC50 为 0.34 μM。

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
SBI-553 化学结构 CAS号:1849603-72-0
SBI-553 化学结构
CAS号:1849603-72-0
SBI-553 3D分子结构
CAS号:1849603-72-0
SBI-553 化学结构 CAS号:1849603-72-0
SBI-553 3D分子结构 CAS号:1849603-72-0
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SBI-553 纯度/质量文件 产品仅供科研

货号:A1216662 标准纯度: {[allProObj[0].p_purity_real_show]}
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SBI-553 生物活性

描述 Neurotensin receptor 1 (NTSR1) is a G-protein-coupled receptor (GPCR) that engages multiple subtypes of G protein, and is involved in the regulation of blood pressure, body temperature, weight and the response to pain[1].SBI-553 not only acts as a β-arrestin-biased agonist but also extends profound β-arrestin bias to the endogenous ligand by selectively antagonizing G protein signaling. SBI-553 shows efficacy in animal models of psychostimulant abuse, including cocaine self-administration, without the side effects characteristic of balanced NTSR1 agonism. SBI-553 administration (12 mg/kg, i.p.) to attenuate cocaine-induced hyperlocomotion relative to the vehicle control (saline, 5 ml/kg, i.p.) (Fig 5A,B). By contrast, responses to the vehicle and SBI-553 were comparable in non-stimulant exposed animals. This SBI-553 dose also reduced methamphetamine (2 mg/kg) -induced hyperlocomotion and blocked the expression of methamphetamine conditioned place preference.[2]. SBI-553 increases NTS binding affinity and Bmax,, and its binding affinity is reciprocally increased by NTS. These behaviors are characteristic of positive allosteric modulation and are concordant with the Monod-Wyman-Changeux model of allosteric transitions[3].

SBI-553 参考文献

[1] Hideaki E Kato, Yan Zhangi,et al. Conformational transitions of a neurotensin receptor 1-G i1 complex. Nature. 2019 Aug;572(7767):80-85.

[2] Lauren M Slosky, Yushi Bai,et al. β-Arrestin-Biased Allosteric Modulator of NTSR1 Selectively Attenuates Addictive Behaviors. Cell. 2020 Jun 11;181(6):1364-1379.e14.

[3] Canals M, Lane JR, Wen A, Scammells PJ, Sexton PM, and Christopoulos A (2012). A MonodWyman-Changeux Mechanism Can Explain G Protein-coupled Receptor (GPCR) AllostericModulation. J Biol Chem 287, 650–659.

SBI-553 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.22mL

0.44mL

0.22mL

11.10mL

2.22mL

1.11mL

22.20mL

4.44mL

2.22mL

SBI-553 技术信息

CAS号1849603-72-0
分子式C26H31FN4O2
分子量 450.548
别名
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,2-8°C

溶解方案

DMSO: 16 mg/mL(35.51 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
动物实验配方
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