2. GPCR/G Protein Neuronal Signaling MAPK/ERK Pathway TGF-beta/Smad Protein Tyrosine Kinase/RTK Apoptosis
  3. 5-HT Receptor p38 MAPK TGF-β Receptor FGFR Apoptosis Caspase
  4. PRX-08066 maleate

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

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PRX-08066 maleate

PRX-08066 maleate Chemical Structure

CAS No. : 866206-55-5

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PRX-08066 maleate Related Antibodies

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Description

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

IC50 & Target[1]

5-HT2B Receptor

3.4 nM (Ki)

In Vitro

PRX-08066 maleate inhibits 5-HT induced mitogen-activated protein kinase activation (IC50 = 12 nM) and markedly reduced thymidine incorporation (IC50 = 3 nM) in hamster ovary cells expressing the human 5-HT2BR[1].
. PRX-08066 (0.01 pM-100 pM, 24 h) maleate significantly inhibits the proliferation of KRJ-I cells with an IC50 of 4.6 pM and has no significant effect on NCI-H720 cells (with no expression of 5-HT2B receptors)[2].
PRX-08066 (0.01 pM-100 pM) maleate inhibits basal and Isoproterenol (HY-B0468)-stimulated 5-HT secretion with IC50s of 6.9 pM and 1.25 pM in KRJ-I cells[2].
PRX-08066 (0.5 pM) maleate significantly reduces the phosphorylation level of ERK in KRJ-I cells[2].
PRX-08066 (1-2 h) maleate reduces fibrotic factors (TGFβ1, CTGF, FGF2) in KRJ-I cells[2].
PRX-08066 (1 pM, 24 h) maleate significantly increases the proportion of apoptotic cells by activating Caspase-3 in KRJ-I cells and HEK293 cells established in a coculture system[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PRX-08066 maleate Related Antibodies

Cell Viability Assay[2]

Cell Line: KRJ-I cells and HEK293 cells established in a coculture system
Concentration: 1 pM
Incubation Time: 24 h
Result: Significantly increased the proportion of dead cells in KRJ-I, and the proportion of Caspase-3 positive cells among the dead cells also rose.
Significantly increased the proportion of positive cells for Caspase-3 in HEK293 cells.
In Vivo

PRX-08066 (50-100 mg/kg, p.o., twice daily for 5 weeks) maleate improves pulmonary vascular remodeling, right ventricular hypertrophy and cardiac function in Monocrotaline (MCT) (HY-N0750)-induced PAH rats[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MCT induced PAH model established in male Sprague-Dawley rats (200-225 g)[1]
Dosage: 50 and 100 mg/kg
Administration: Oral administration (p.o.), once daily for 5 weeks
Result: Selectively reduced pulmonary artery pressure without affecting systemic blood pressure.
Reversed right ventricular hypertrophy.
Reduced the thickness of the media layer of pulmonary small arteries, improves the closure of the lumen, and reduces tissue pathological damage.
Inhibited the proliferation and contraction of vascular smooth muscle mediated by 5-HT.
No significant gastrointestinal side effects or systemic toxicity.
Clinical Trial
Molecular Weight

517.96

Formula

C23H21ClFN5O4S
CAS No.
SMILES

O=C(O)/C=C\C(O)=O.N#CC1=CC(CN2CCC(NC3=C(C=C(Cl)S4)C4=NC=N3)CC2)=CC=C1F
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Room temperature in continental US; may vary elsewhere.
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Purity & Documentation
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PRX-08066 maleate Related Classifications

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Keywords:

PRX-08066866206-55-5PRX08066PRX 080665-HT Receptorp38 MAPKTGF-β ReceptorFGFRApoptosisCaspaseSerotonin Receptor5-hydroxytryptamine ReceptorTransforming growth factor beta receptorsFibroblast growth factor receptorcarcinoidcoculturefibrosisgastrointestinalHEK293KRJ-Ineuroendocrine tumorproliferationserotonintumor microenvironmentInhibitorinhibitorinhibit

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