PRX-08066

SKU: orb1307842

Description

PRX-08066

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 866206-54-4
• MW: 401.89
• Purity: 98.07%
• Formula: C₁₉H₁₇ClFN₅S
• SMILES: Fc1ccc(CN2CCC(CC2)Nc2ncnc3sc(Cl)cc23)cc1C#N
• Target: 5-HT Receptor
• Solubility: DMSO:7 mg/mL (17.42 mM)

Bioactivity

• Target IC50:
  5-HT2B:3.4 nM
• In Vivo:
  PRX-08066 significantly reduces peak pulmonary artery pressure at 50 mg/kg and 100 mg/kg compared with monocrotaline control rats. PRX-08066 also significantly reduces the right ventricle (RV)/body weight and RV/left ventricle + septum, compared with MCT-treated rats. PRX-08066 significantly attenuates the elevation in pulmonary artery pressure and RV hypertrophy and maintains cardiac function. PRX-08066 significantly reduces the hypoxia-dependent increase in right ventricular systolic pressure in both rats and mice without affecting the systemic mean arterial pressure in the animals. PRX-08066 (30 mg/kg) inhibits right ventricular systolic pressure and monocrotaline-induced ERK phosphorylation in whole lung homogenates in rats. PRX-08066 (100 mg/kg) treated groups show less right ventricular hypertrophy and septal flattening than the monocrotaline control group in rats. PRX-08066 (100 mg/kg) significantly inhibits both right ventricular systolic pressure and right ventricular/left ventricular +septum weight elevations in rats .
• In Vitro:
  PRX-08066 inhibits TGFβ1, CTGF, and FGF2 transcription and secretion in KRJ-I cells. PRX-08066 decreases the level of transcripts for Ki67 (84%) as well as Ki67 protein (36.8%) associated with an increase in caspase 3 transcript levels in KRJ-I cells. PRX-08066 decreases the level of transcripts of TGFβ1, FGF2, and TPH1 in KRJ-I cells. PRX-08066 significantly increases the number of dead cells (34%) compared with untreated controls in KRJ-I cells. PRX-08066 causes a significant increase in dead/caspase 3 positive cells (76%) and caspase 3 activity (52%) in HEK293 cells. PRX-08066 inhibits cell proliferation with IC50 of 0.46 nM and with a maximum inhibition of 20% and 5-HT secretion with IC50 of 6.9 nM with a maximum inhibition of 30% in the 5-HT(2B) expressing SI-NET cell line, KRJ-I. PRX-08066 inhibits isoproterenol-stimulated 5-HT release with IC50 of 1.25 nM and maximum inhibition of 60% in NCI-H720 cells. PRX-08066 inhibits 5-HT-induced mitogen-activated protein kinase activation (IC50: 12 nM) and markedly reduces thymidine incorporation with IC50 of 3 nM in Chinese hamster ovary cells expressing the human 5-HT2BR, which suggests that PRX-08066 can potentially inhibit the pathologic 5-HT-induced vascular muscularization associated with PAH. PRX-08066 (0.5 nM) significantly inhibits ERK phosphorylation in KRJ-I 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

5-HT2B, 5-HT Receptor, 5HT Receptor, 5HTReceptor, 5-hydroxytryptamine Receptor, inhibit, Inhibitor, PRX 08066, PRX08066, PRX-08066, Serotonin Receptor

Compound Identifiers

PubChem CID

11502243