PRX 08066 - CAS 866206-54-4
Catalog number: 866206-54-4
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C19H17ClFN5S
Molecular Weight:
401.89
COA:
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Targets:
5-HT Receptor
Description:
PRX 08066, a selective 5-hydroxytryptamine receptor 2B(5-HT2BR) antagonist, causes selective vasodilation of pulmonary arteries. Its IC50 value is 3.4 nM. It can potentially inhibit the pathologic 5-HT-induced vascular muscularization and is developed to treat for pulmonary arterial hypertension (PAH). It reduces monocrotaline-induced pulmonary arterial hypertension and right ventricular hypertrophy in rats. It shows effects on the vascular muscularization induced by 5-HT in the in vitro studies. It inhibits 5-HT-induced mitogen-activated protein kinase activation and markedly reduces thymidine incorporation in Chinese hamster ovary cells expressing the human 5-HT2BR in vitro. It decreases level of transcripts of TGFβ1, FGF2 and TPH1 in KRJ-I cells. It significantly reduces peak pulmonary artery pressure at 50 mg/kg and 100 mg/kg compared with monocrotaline control rats. It also significantly attenuates the elevation in pulmonary artery pressure and RV hypertrophy and maintains cardiac function. It 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. It is also found to have anti-proliferative and anti-fibrotic effects. It was developed by Allergan company and is in clinical phase 2 with no progression.
Purity:
>98%
Appearance:
Solid powder
Synonyms:
PRX-08066; PRX 08066; PRX08066. 5-[[4-[(6-chlorothieno[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]methyl]-2-fluorobenzonitrile
Solubility:
DMSO: ≤ 7 mg/mL (Need ultrasonic)
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
PRX 08066 can potentially inhibit the pathologic 5-HT-induced vascular muscularization and is developed to treat for pulmonary arterial hypertension (PAH). It is also found to have anti-proliferative and anti-fibrotic effects.
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Grams to Kilograms
Boiling Point:
579.9±50.0 °C | Condition: Press: 760 Torr
Density:
1.44±0.1 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr
InChIKey:
IENZFHBNCRQMNP-UHFFFAOYSA-N
InChI:
InChI=1S/C19H17ClFN5S/c20-17-8-15-18(23-11-24-19(15)27-17)25-14-3-5-26(6-4-14)10-12-1-2-16(21)13(7-12)9-22/h1-2,7-8,11,14H,3-6,10H2,(H,23,24,25)
Canonical SMILES:
C1CN(CCC1NC2=C3C=C(SC3=NC=N2)Cl)CC4=CC(=C(C=C4)F)C#N
Current Developer:
PRX 08066 was developed by Allergan company and is in clinical phase 2 with no progression.
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CAS 866206-54-4 PRX 08066

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