A competitive

PD 168368 – 10 mg

Brand:
Cayman
CAS:
204066-82-0
Storage:
-20
UN-No:
Non-Hazardous - /

PD 168368 is a competitive antagonist of neuromedin B (NMB) receptors (Kis = 15-45 nM for rat and human receptors expressed in various cell lines).{31668,31671} It blocks the elevation of intracellular calcium and release of inositol phosphate induced by NMB in cells expressing NMB receptors.{31668} PD 168368 is selective for NMB receptors over those for related peptide agonists, including bombesin and gastrin-releasing peptide. It is also an agonist of formyl-peptide receptors (FPRs) at higher concentrations (EC50s = 0.57 and 0.24 µM for FPR1 and FPR2, respectively).{31669} PD 168368 induces cell cycle arrest and apoptosis in MDA-MB-231 breast cancer cells and blocks neovascularization and cancer cell growth in breast cancer xenograft tumors in mice.{31667}  

 

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Description

A competitive, selective antagonist of NMB receptors (Kis = 15-45 nM for rat and human receptors expressed in various cell lines); blocks the elevation of intracellular calcium and release of inositol phosphate induced by NMB in cells expressing NMB receptors

Formal name: (αS)-α-methyl-α-[[[(4-nitrophenyl)amino]carbonyl]amino]-N-[[1-(2-pyridinyl)cyclohexyl]methyl]-1H-indole-3-propanamide

Synonyms: 

Molecular weight: 554.6

CAS: 204066-82-0

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Cell Cycle||Research Area|Cancer|Cell Death|Apoptosis

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