PD 176252

Name: PD 176252
Brand: Tocris Bioscience
SKU: 2602

Tocris Bioscience, part of Bio-Techne | Catalog # 2602

Citations (11)

COA / SDS

GRP (BB2) and NMB (BB1) receptor antagonist

Key Product Details

Description:	GRP (BB₂) and NMB (BB₁) receptor antagonist
Chemical Name:	(S)-N-[[1-(5-Methoxy-2-pyridinyl)cyclohexyl]methyl]-α-methyl-α-[[[-(4-nitrophenyl)amino]carbonyl]amino-1H-indole-3-propanamide
Purity:	≥98% (HPLC)
Molecular Weight:	584.67

View Full Technical Details for PD 176252

Technical Data
Citations

Biological Activity for PD 176252

PD 176252 is a non-peptide gastrin-releasing peptide receptor (GRP-R, BB₂) and neuromedin B receptor (NMB-R, BB₁) antagonist (K_i 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).

Technical Data for PD 176252

M. Wt	584.67
Formula	C₃₂H₃₆N₆O₅
Storage	Store at +4°C
Purity	≥98% (HPLC)
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for PD 176252

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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 will 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

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References for PD 176252

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