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).
For research use only. We do not sell to patients.
- CAS No.: 866206-55-5
- Formula: C23H21ClFN5O4S
- Molecular Weight:517.96
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
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Help & FAQs
Biological Activity
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5-HT2B Receptor 3.4 nM (Ki) |
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].
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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.
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Cell Line:KRJ-I cells and HEK293 cells established in a coculture system
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Concentration:1 pM
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Incubation Time:24 h
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MCT induced PAH model established in male Sprague-Dawley rats (200-225 g)[1]
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Dosage:50 and 100 mg/kg
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Administration:Oral administration (p.o.), once daily for 5 weeks
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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.
Chemical Information
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CAS No. 866206-55-5
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Molecular Weight 517.96
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Formula C23H21ClFN5O4S
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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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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