Chemical Structure : CCKBR agonist MF-8
CAS No.:
2923123-00-4
CCKBR agonist MF-8
(Glu-(N-Me-W)-Nle-D-F(3-Br)-NH2)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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800.71
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Formula
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C36H46BrN7O9
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(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
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References
1. Shi H, et al. Nat Commun. 2025 Dec 8;16(1):10938.
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