GRPR antagonist-1
GRPR antagonist-1 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 4.97, 4.36 and 3.40 μM in PC3, Pan02 and HGC-27 cells, respectively) . GRPR antagonist-1 inhibits HGC-27 cell viability by decreasing the Bcl-2 level and increasing the Bax level, causing apoptosis, with anticancer activity[1].
Product Specifications
CAS Number
3052544-28-9
UNSPSC
12352005
Target
Bombesin Receptor
Type
Reference compound
Related Pathways
GPCR/G Protein
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/grpr-antagonist-1.html
Solubility
10 mM in DMSO
Smiles
CC(C)(OC(N1CCN(CC1)C([C@H](CC2=CNC3=C2C=CC=C3)NC(CC4=CC=C(C=C4)C(F)(F)F)=O)=O)=O)C
Molecular Formula
C29H33F3N4O4
Molecular Weight
558.59
References & Citations
[1]Yu, Mj., et al. Structure–activity relationship studies on Pd176252 derivatives leading to discovery of novel GRP receptor antagonist with potent anticancer activity. Med Chem Res 30, 2069–2089 (2021) .
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Frequently Asked Questions
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