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PD 168368

Catalog No. T8691 CAS 204066-82-0

Synonyms: PD168368

PD 168368 is a novel, potent, competitive and selective nonpeptide neuromodulin B receptor (NMB-R) antagonist with inhibitory effects on the gastrin-releasing peptide receptor (GRPR).PD 168368 is a potent mixed agonist of FPR1/FPR2/FPR3.

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PD 168368, CAS 204066-82-0

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Purity: 98.44%

Biological Description

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Storage & Solubility Information

Description	PD 168368 is a novel, potent, competitive and selective nonpeptide neuromodulin B receptor (NMB-R) antagonist with inhibitory effects on the gastrin-releasing peptide receptor (GRPR).PD 168368 is a potent mixed agonist of FPR1/FPR2/FPR3.
In vitro	PD 168368 exhibits high activity and induces [Ca2+]I release in human neutrophils, with EC50 values in the nanomolar range[3]. 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[4]. 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[4].
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[4].

Synonyms	PD168368
Molecular Weight	554.64
Formula	C31H34N6O4
CAS No.	204066-82-0

Storage

store at low temperature

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

Solubility Information

DMSO: 20 mg/mL(36.06 mM), Sonication is recommended.

DMF: 5 mg/mL(9.01 mM), Sonication is recommended.

References and Literature

1. R R Ryan, et al. Comparative pharmacology of the nonpeptide neuromedin B receptor antagonist PD 168368. J Pharmacol Exp Ther. 1999 Sep;290(3):1202-11.

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Keywords

PD 168368 204066-82-0 GPCR/G Protein Bombesin Receptor PD-168368 PD168368 inhibitor inhibit

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