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首页-小分子抑制剂&激动剂-GPCR-Cholecystokinin Receptor-CCKBR agonist MF-8
CCKBR agonist MF-8

Chemical Structure : CCKBR agonist MF-8

CAS No.: 2923123-00-4

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CCKBR agonist MF-8 (Glu-(N-Me-W)-Nle-D-F(3-Br)-NH2)

货号: PC-26142Not For Human Use, Lab Use Only.

CCKBR agonist MF-8 is a potent, highly β-arrestin biased CCKBR (Cholecystokinin B Receptor, CCK2) agonist with binding IC50 of 0.9 nM and EC50 of 516 nM in calcium signaling assays, performs poorly in activating Gαq/11-Ca2+ signaling but is highly potent in inducing β-arrestin2 signaling.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

CCKBR agonist MF-8 is a potent, highly β-arrestin biased CCKBR (Cholecystokinin B Receptor, CCK2) agonist with binding IC50 of 0.9 nM and EC50 of 516 nM in calcium signaling assays, performs poorly in activating Gαq/11-Ca2+ signaling but is highly potent in inducing β-arrestin2 signaling.
MF-8 binds to CCKBR with high affinity (IC50=0.9 nM), shows IC50 of 4.54 nM in PRESTO-Tango assays.
MF-8 does not exhibit any agonistic effect on the Gαq/11 signaling of CCKAR and β-arrestin1/2 downstream of GPR173.
MF-8 can effectively induce endocytosis of CCKBR. MF-8 inhibited the key signaling pathway of CCKBR-mediated calcium, cAMP accumulation, and LTP.
MF-8 inhibits the increase in calcium flux and cAMP accumulation induced by CCK8s with IC50 of 22.7 nM and 16 nM in 293T-CCKBR cells.
MF-8 inhibits the CCKBR-LTP mediated cue-to-cue fear memory.

物理化学性质&存储条件

分子量 800.71
分子式 C36H46BrN7O9
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

(2R,5R,8R,11R,14R)-11-((1H-indol-3-yl)methyl)-1,14-diamino-2-(3-bromobenzyl)-8-butyl-5-(carboxymethyl)-12-methyl-1,4,7,10,13-pentaoxo-3,6,9,12-tetraazaheptadecan-17-oic acid

参考文献

1. Shi H, et al. Nat Commun. 2025 Dec 8;16(1):10938.

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