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首页-小分子抑制剂&激动剂-GPCR-Neurotensin Receptor-SBI-553
SBI-553

Chemical Structure : SBI-553

CAS No.: 1849603-72-0

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SBI-553 (SBI553)

货号: PC-38142Not For Human Use, Lab Use Only.

SBI-553 (SBI553) is a potent, selective, β-arrestin-biased, brain penetrant neurotensin receptor 1 (NTR1, NTSR1) allosteric modulator with EC50 of 0.34 uM.

规格 价格 库存 数量
5 mg ￥1880 In stock
10 mg ￥2980 In stock
25 mg ￥4980 In stock
50 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

SBI-553 (SBI553) is a potent, selective, β-arrestin-biased, brain penetrant neurotensin receptor 1 (NTR1, NTSR1) allosteric modulator with EC50 of 0.34 uM.
SBI-553 had no effect on the potency of NT in the NTR1 high-content (β-arrestin2-GFP) assay.
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 only showed moderate affinity against a range of related and unrelated GPCRs using the same high-content assay format (NTR2, GPR35, GPR55, K-opioid).
SBI-553 (12 mg/kg, i.p.) attenuated basal hyperlocomotion in dopamine transporter knockout (DAT−/−) mice.
SBI-553 showed efficacy in animal models of psychostimulant abuse, including cocaine self-administration, without the side effects characteristic of balanced NTSR1 agonism.

物理化学性质&存储条件

分子量 450.558
分子式 C26H31FN4O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2-((2-(1-Fluorocyclopropyl)-4-(4-(2-methoxyphenyl)piperidin-1-yl)quinazolin-6-yl)(methyl)amino)ethan-1-ol

参考文献

1. Pinkerton AB, et al. J Med Chem. 2019 Sep 12;62(17):8357-8363.

2. Slosky LM, et al. Cell. 2020 Jun 11;181(6):1364-1379.e14.

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