PRX-08066

PRX-08066 is a selective and orally active 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist with a Ki of 3.4 nM. PRX-08066 inhibits the MAPK pathway, 5-HT release and fibrotic factor (TGFβ1, CTGF and FGF2) expression. PRX-08066 inhibits the proliferation of KRJ-I cells and induces apoptosis (caspase-3 activation) . PRX-08066 inhibits pulmonary vascular remodeling. PRX-08066 can be used of pulmonary Arterial Hypertension (PAH) and neuroendocrine tumor (NET) [1][2].

Product Specifications

CAS Number

[866206-54-4]

UNSPSC

12352005

Hazard Statement

H302

Target

5-HT Receptor; Apoptosis; Caspase; FGFR; p38 MAPK; TGF-β Receptor

Type

Reference compound

Related Pathways

Apoptosis; GPCR/G Protein; MAPK/ERK Pathway; Neuronal Signaling; Protein Tyrosine Kinase/RTK; TGF-beta/Smad

Applications

COVID-19-immunoregulation

Field of Research

Cancer; Neurological Disease; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/PRX-08066.html

Purity

97.46

Solubility

DMSO : 7 mg/mL (ultrasonic)

Smiles

N#CC1=CC(CN2CCC(NC3=C(C=C(Cl)S4)C4=NC=N3)CC2)=CC=C1F

Molecular Formula

C19H17ClFN5S

Molecular Weight

401.89

Precautions

H302

References & Citations

[1]Porvasnik SL, et al. PRX-08066, a novel 5-hydroxytryptamine receptor 2B antagonist, reduces monocrotaline-induced pulmonary arterial hypertension and right ventricular hypertrophy in rats. J Pharmacol Exp Ther. 2010 Aug;334 (2) :364-72.|[2]Svejda B, et al. The 5-HT (2B) receptor plays a key regulatory role in both neuroendocrine tumor cell proliferation and the modulation of the fibroblast component of the neoplastic microenvironment. Cancer. 2010 Jun 15;116 (12) :2902-12.