PRX-08066
CAS No. : 866206-54-4
| Size | Price | Stock |
|---|---|---|
| 1mg | $70 | In-stock |
| 5mg | $150 | In-stock |
| 10mg | $220 | In-stock |
| 25mg | $450 | In-stock |
| 50mg | $790 | In-stock |
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| 200 mg | Get quote | |
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| Cat. No. : | HY-15472 |
| M.Wt: | 401.89 |
| Formula: | C19H17ClFN5S |
| Purity: | >98 % |
| Solubility: | DMSO : 7 mg/mL (ultrasonic) |
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].
In Vitro:PRX-08066 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) 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) 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) significantly reduces the phosphorylation level of ERK in KRJ-I cells[2].
PRX-08066 (1-2 h) reduces fibrotic factors (TGFβ1, CTGF, FGF2) in KRJ-I cells[2].
PRX-08066 (1 pM, 24 h) significantly increases the proportion of apoptotic cells by activating Caspase-3 in KRJ-I cells and HEK293 cells established in a coculture system[2].
In Vivo:PRX-08066 (50-100 mg/kg, p.o., twice daily for 5 weeks) improves pulmonary vascular remodeling, right ventricular hypertrophy and cardiac function in Monocrotaline (MCT) (HY-N0750)-induced PAH rats[1].
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