PRX-08066

• Description:

  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].

• 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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Phase 2

• Isoform:

  α-1 microglobulin

• CAS Number:

  866206-54-4