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首页-小分子抑制剂&激动剂-GPCR-Cholecystokinin Receptor-CCKBR Gi-biased agonist 3qr
CCKBR Gi-biased agonist 3qr

Chemical Structure : CCKBR Gi-biased agonist 3qr

CAS No.: 2923120-30-1

CCKBR Gi-biased agonist 3qr

货号: PC-25772Not For Human Use, Lab Use Only.

CCKBR Gi-biased agonist 3qr is a potent, selective Gq-biased agonist of cholecystokinin (CCK) B receptor (CCKBR) with EC50 of 0.035 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

CCKBR Gi-biased agonist 3qr is a potent, selective Gq-biased agonist of cholecystokinin (CCK) B receptor (CCKBR) with EC50 of 0.035 nM.
3r1 effectively increased the viability of primary cortical neurons in a concentration-dependent manner (EC50 = 0.037 nM), but not CCKBR Gi-biased agonist z-44.
3r1 (0.01 or 0.05 mg/kg) through intraperitoneal injection every day for 3 months significantly rescued neuronal apoptosis in 5×FAD mice, increases number of secondary branches and the axon length of neurons.
3r1 (0.01 or 0.05 mg/kg) significantly reduced the p-Tau (phosphorylated tau protein) level alleviated cognitive decline in AD mouse model.
3r1 reduces the number of plaques by increasing α-secretase activity and PLCB4 expression in 5×FAD mice.

物理化学性质&存储条件

分子量 699.60
分子式 C32H39BrN6O7
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

(S)-3-((S)-2-((S)-2-acetamido-3-(1H-indol-3-yl)propanamido)hexanamido)-4-(((S)-1-amino-3-(3-bromophenyl)-1-oxopropan-2-yl)amino)-4-oxobutanoic acid

参考文献

1. Wang JL, et al. Cell. 2025 Nov 20:S0092-8674(25)01238-3.

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