PD 176252
Tocris Bioscience, part of Bio-Techne | Catalog # 2602
GRP (BB2) and NMB (BB1) receptor antagonist
Key Product Details
Description
GRP (BB2) and NMB (BB1) receptor antagonist
Product Description
PD 176252 is a non-peptide gastrin-releasing peptide receptor (GRP-R, BB2) and neuromedin B receptor (NMB-R, BB1) antagonist (Ki values are 0.17 and 1.0 nM for BB1 and BB2 respectively). Inhibits proliferation of rat C6 glioma cells (IC50 = 2 μM) and inhibits NCI-H1299 xenograft proliferation in nude mice (IC50 = 5 μM).Product Specifications
Molecular Weight
584.67
Formula
C32H36N6O5
Storage
Store at +4°C
Purity
≥98% (HPLC)
Chemical Name
(S)-N-[[1-(5-Methoxy-2-pyridinyl)cyclohexyl]methyl]-α-methyl-α-[[[-(4-nitrophenyl)amino]carbonyl]amino-1H-indole-3-propanamide
CAS Number
204067-01-6
PubChem ID
9829828
InChI Key
NNFUWNLENRUDHR-HKBQPEDESA-N
SMILES
O=C(NC3=CC=C([N+]([O-])=O)C=C3)N[C@@](C)(CC5=CNC4=CC=CC=C45)C(NCC1(C2=CC=C(OC)C=N2)CCCCC1)=O
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 58.47 | 100 |
Preparing Stock Solutions
for PD 176252
The following data is based on the product molecular weight 584.67
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.71 mL | 8.55 mL | 17.10 mL |
| 5 mM | 0.34 mL | 1.71 mL | 3.42 mL |
| 10 mM | 0.17 mL | 0.86 mL | 1.71 mL |
| 50 mM | 0.03 mL | 0.17 mL | 0.34 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Schepetkin Gastrin-releasing peptide/neuromedin B receptor antagonists pD176252, PD168368, and related analogs are potent agonists of human formyl-peptide receptors. Mol.Pharmacol. 2011 PMID: 20943772
- Moody Nonpeptide neuromedin B receptor antagonists inhibit the proliferation of C6 cells Eur.J.Pharmacol. 2000 PMID: 11104826
- Moody Nonpeptide gastrin releasing peptide receptor antagonists inhibit the proliferation of lung cancer cells Eur.J.Pharmacol. 2003 PMID: 12909192
- Ashwood PD 176252 - the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist Bioorg.Med.Chem.Lett. 1998 PMID: 9873586
Product Specific Notices for PD 176252
For research use only
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