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首页-小分子抑制剂&激动剂-GPCR-GPR88-RTI-13951-33
RTI-13951-33

Chemical Structure : RTI-13951-33

CAS No.: 2244884-08-8

RTI-13951-33 (GPR88 agonist)

货号: PC-35398Not For Human Use, Lab Use Only.

RTI-13951-33 is a potent, selective, brain-penetrant agonist of the orphan receptor GPR88 with EC50 of 25 nM in in vitro cAMP functional assay.

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2 mg ¥2280 In stock
5 mg ¥3980 In stock
10 mg ¥5980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

RTI-13951-33 is a potent, selective, brain-penetrant agonist of the orphan receptor GPR88 with EC50 of 25 nM in in vitro cAMP functional assay.
RTI-13951-33 displays no significant off-target activity at 38 GPCRs, ion channels, and neurotransmitter transporters.
RTI-13951-33 exhibits enhanced aqueous solubility compared to (1R,2R)-2-PCCA (2) and had favorable pharmacokinetic properties for behavioral assessment.
RTI-13951-33 significantly reduces alcohol self-administration and alcohol intake in a dose-dependent manner without effects on locomotion and sucrose self-administration in rats

物理化学性质&存储条件

分子量 459.59
分子式 C28H33N3O3
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

(1R,2R)-N-((2R,3R)-2-amino-3-methoxybutyl)-N-(4'-(methoxymethyl)-[1,1'-biphenyl]-4-yl)-2-(pyridin-2-yl)cyclopropane-1-carboxamide

参考文献

1. Jin C, et al. J Med Chem. 2018 Jul 16. doi: 10.1021/acs.jmedchem.8b00566.

2. Ye N, et al. ACS Chem Neurosci. 2018 Dec 12. doi: 10.1021/acschemneuro.8b00572.

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