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PD176252

Catalog No. T16449 CAS 204067-01-6

PD176252 is a potent BB1 and BB2 antagonist with inhibitory effects on BB1 and BB2 receptors.PD176252 acts as a small molecule GRPR inhibitor and FPR1/FPR2 agonist to inhibit the growth and proliferation of a variety of cancer cells.

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PD176252, CAS 204067-01-6

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Purity: 99.18%

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Description	PD176252 is a potent BB1 and BB2 antagonist with inhibitory effects on BB1 and BB2 receptors.PD176252 acts as a small molecule GRPR inhibitor and FPR1/FPR2 agonist to inhibit the growth and proliferation of a variety of cancer cells.
Targets&IC50	FPR1:0.31 μM (EC50), BB2 receptor:16 nM (Rat), BB1 receptor:0.66 nM (Ki, Rat), FPR:0.72±0.21 μM (EC50, human), FPR2:0.66 μM (EC50), BB1 receptor:0.17 nM (Ki, Human), BB2 receptor:1 nM (Ki, Human)
In vitro	PD176252 is a potent antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide-preferring (BB2) receptors with Kis of 0.17 nM and 1 nM for human BB1 and BB2 receptors, and 0.66 nM and 16 nM for Rat BB1 and BB2 receptors, respectively. In CHO cells expressing human BB1 or BB2 receptors, PD176252 inhibits acidification responses to neuromedin-B or neuromedin-C with appKBs of 4.0 nM or 13 nM. It also blocks bombesin-evoked increases in intracellular calcium levels in CHO cells stably expressing human BB1 or BB2 receptors, with appKBs of 2.3 nM and 36 nM, respectively.PD176252 is additionally an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC50s of 0.31 and 0.66 μM in HL-60 cells. It activates Ca2+ mobilization in HL-60 cells transfected with human FPRs (EC50, 0.72 ± 0.21 μM)[2]. PD176252 shows little specific 125I-gastrin releasing peptide binding to NCI-H345 cells at 1 nM, suppressing almost all specific bindings at 1000 nM, with an IC50 of 30 nM. Furthermore, PD176252 (10, 30 μM) significantly inhibits the growth of NCI-H345 or H1299 cells, with IC50s of 7 and 5 μM[1].
In vivo	Orally administered PD176252 (1, 10 μg) potently inhibits the growth and proliferation of NCI-H1299 xenografts in nude mice[1].

Molecular Weight	584.67
Formula	C32H36N6O5
CAS No.	204067-01-6

Storage

store under nitrogen

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL(171.04 mM), Sonication is recommended.

References and Literature

1. Moody TW, et al. Nonpeptide gastrin releasing peptide receptor antagonists inhibit the proliferation of lung cancer cells. Eur J Pharmacol. 2003 Aug 1;474(1):21-9. 2. Schepetkin IA, et al. Gastrin-releasing peptide/neuromedin B receptor antagonists PD176252, PD168368, and related analogs are potent agonists of human formyl-peptide receptors. Mol Pharmacol. 2011 Jan;79(1):77-90. 3. Ashwood V, et al. PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist. Bioorg Med Chem Lett. 1998 Sep 22;8(18):2589-94.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Membrane Protein-targeted Compound Library GPCR Compound Library

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Keywords

PD176252 204067-01-6 GPCR/G Protein Bombesin Receptor PD-176252 PD 176252 inhibitor inhibit

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