PRX-08066 Inhibitor CAS No. 866206-55-5

Cat. No.	Name	Size	Price
KI2408	PRX-08066	5 mg	$526
	PRX-08066	10 mg	$722
	PRX-08066	50 mg	$2090
	PRX-08066	200 mg	$4828

Chemical Characteristic

Product Name	PRX-08066
CAS No.	866206-55-5
Molecular Weight	517.96
Formula	C₂₃H₂₁ClFN₅O₄S
Chemical Name	Benzonitrile, 5-[[4-[(6-chlorothieno[2,3-d]pyrimidin-4-yl)amino]-1-piperidinyl]methyl]-2-fluoro-, (2Z)-2-butenedioate (1:1)
Smiles	C(#N)c1c(ccc(c1)CN1CCC(CC1)Nc1c2c(ncn1)sc(c2)Cl)F O=C(/C=C\C(=O)O)O
Chemical Structure

Biological activities

PRX-08066 is a highly potent and selective 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist with a Ki value of 3.4 nM. In vitro, PRX-08066 inhibits 5-HT induced mitogen-activated protein kinase (MAPK) activation with an IC50 of 12 nM and markedly reduces thymidine incorporation with an IC50 of 3 nM in Chinese hamster ovary cells expressing the human 5-HT2BR.^[1] In the 5-HT2B expressing small intestinal neuroendocrine tumors (SI-NETs) cell line KRJ-I, PRX-08066 inhibits the cell proliferation with an IC50 of 4.6 nM and prevents 5-HT secretion with an IC50 of 6.9 nM. PRX-08066 also decreases ERK1/2 phosphorylation and profibrotic growth factor (including TGFβ1, CTGF, and FGF2) synthesis and secretion in KRJ-I cell line. In the KRJ-I:HEK293 coculture system, PRX-08066 significantly decreases 5-HT release, Ki67, TGFβ1, CTGF, and FGF2 transcription in the KRJ-I cell line.^[2] In vivo, PRX-08066 administration (100 mg/kg) significantly reduces monocrotaline-induced pulmonary arterial hypertension and right ventricular hypertrophy in rats.^[1]

Protocols

In vivo, PRX-08066 is suspended in water, and the pH is adjusted to between 6.5 and 7.5 by the slow addition of 1 N NaOH (sodium hydroxide). Methylcellulose in water (1% w/v) and 10? phosphate-buffered saline (PBS) are added to achieve a final concentration of 20 mg/mL PRX-08066 in 0.5% cellulose (w/v) and 1 ? PBS.^[1]

References

[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, 334(2): 364-372. [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, 116(12): 2902-2912.

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