PD 168368

SKU: orb1685361

Description

PD 168368 is a selective, nonpeptide antagonist of the neuromedin B receptor (NMB-R) and an inhibitor of the gastrin-releasing peptide receptor (GRPR). It also acts as a potent mixed agonist for FPR1, FPR2, and FPR3. This compound is a valuable research tool for studying receptor signaling in cancer, inflammation, and neurobiology using both in vitro and in vivo models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 204066-82-0
• MW: 554.64
• Purity: 99.87% (May vary between batches)
• Formula: C₃₁H₃₄N₆O₄
• SMILES: C[C@@](Cc1c[nH]c2ccccc12)(NC(=O)Nc1ccc(cc1)[N+]([O-])=O)C(=O)NCC1(CCCCC1)c1ccccn1
• Target: Bombesin Receptor
• Solubility: DMF:5 mg/mL (9.01 mM);DMSO:20 mg/mL (36.06 mM)

Bioactivity

• In Vivo:
  In mice, PD 168368 potently inhibits the in vivo metastasis of breast cancer. Administered at a dose of 1.2 mg/kg through intraperitoneal injection for 30 days, PD 168368 effectively inhibits breast cancer metastasis.
• In Vitro:
  PD 168368 exhibits high activity and induces [Ca2+]I release in human neutrophils, with EC50 values in the nanomolar range. In the human breast cancer cell line MDA-MB-231, PD 168368 suppresses migration and invasion. It also reduces epithelial-mesenchymal transition (EMT) by upregulating E-cadherin and downregulating vimentin. At a concentration of 5 μM, PD 168368 inhibits migration and invasiveness in breast cancer cells. Furthermore, at a concentration of 10 μM, PD 168368 suppresses the activation of the mTOR/p70S6K/4EBP1 and AKT/GSK-3β pathways in breast cancer cells.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Bombesin Receptor, BombesinReceptor, PD168368, PD-168368, PD 168368

Compound Identifiers

PubChem CID

9937534