PRX-08066 Maleic acid

Catalog No.S8010

PRX-08066 Maleic acid Chemical Structure

Molecular Weight(MW): 517.96

PRX-08066 Maleic acid is a selective 5-HT2B receptor antagonist with IC50 of 3.4 nM, prevents the severity of pulmonary arterial hypertension in the MCT rat model. Phase 2.

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In DMSO USD 560 In stock
USD 270 In stock
USD 370 In stock
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Cited by 1 Publication

1 Customer Review

  • The HTR2B antagonist PRX-08066 reduced the viability of UM metastatic cell lines. MTS cell viability assays were performed 72 h post-treatment with PRX-08066. Increasing concentrations of PRX-08066 (5, 10, 20, 50 and 100 µM) were tested on UM metastatic cell lines T111, T128 and T131 (a). The 20  µM concentration was tested on UM non-metastatic cell lines (T108, T130 and T143) and normal uveal melanocytes (NUM; b). Data are represented as relative percentage of viability using a column bar graph (mean±SEM). The absorbance of untreated cells (black bars) was considered as 100%. Student t test, *P<0.05

    Clinical & Experimental Metastasis, 2018, https://doi.org/10.1007/s10585-018-9894-x. PRX-08066 Maleic acid purchased from Selleck.

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Biological Activity

Description PRX-08066 Maleic acid is a selective 5-HT2B receptor antagonist with IC50 of 3.4 nM, prevents the severity of pulmonary arterial hypertension in the MCT rat model. Phase 2.
Features A selective 5-HT2BR antagonist and high selectivity over the closely related 5-HT2A and 5-HT2C receptors and other receptor targets.
Targets
5-HT2B [1]
3.4 nM
In vitro

PRX-08066 inhibits 5-HT-induced mitogen-activated protein kinase activation with IC50 of 12 nM and markedly reduces thymidine incorporation with IC50 of 3 nM in Chinese hamster ovary cells expressing the human 5-HT2BR, which suggests that PRX-08066 can potentially inhibit the pathologic 5-HT-induced vascular muscularization associated with PAH. [1] PRX-08066 inhibits cell proliferation with IC50 of 0.46 nM and with a maximum inhibition of 20% and 5-HT secretion with IC50 of 6.9 nM with a maximum inhibition of 30% in the 5-HT(2B) expressing SI-NET cell line, KRJ-I. PRX-08066 inhibits isoproterenol-stimulated 5-HT release with IC50 of 1.25 nM and a maximum inhibition of 60% in NCI-H720 cells. PRX-08066 (0.5 nM) significantly inhibits ERK phosphorylation in KRJ-I cells. PRX-08066 inhibits TGFβ1, CTGF and FGF2 transcription and secretion in KRJ-I cells. PRX-08066 decreases level of transcripts for Ki67 (84%) as well as Ki67 protein (36.8%) associated with an increase in caspase 3 transcript levels in KRJ-I cells. PRX-08066 decreases level of transcripts of TGFβ1, FGF2 and TPH1 in KRJ-I cells. PRX-08066 significantly increases the number of dead cells (34%) compared with untreated controls in KRJ-I cells. PRX-08066 causes a significant increase in dead/caspase 3 positive cells (76%) and caspase 3 activity (52%) in HEK293 cells. [2]

In vivo PRX-08066 (100 mg/kg) treated groups demonstrates less right ventricular hypertrophy and septal flattening than the monocrotaline control group in rats. PRX-08066 significantly reduces peak pulmonary artery pressure at 50 mg/kg and 100 mg/kg compared with monocrotaline control rats. PRX-08066 also significantly reduces right ventricle (RV)/body weight and RV/left ventricle + septum, compared with MCT-treated rats. PRX-08066 significantly attenuates the elevation in pulmonary artery pressure and RV hypertrophy and maintains cardiac function. PRX-08066 significantly 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. [1] PRX-08066 (100 mg/kg) significantly inhibits both right ventricular systolic pressure and right ventricular/left ventricular +septum weight elevations in rats. PRX-08066 (30 mg/kg) inhibits right ventricular systolic pressure and monocrotaline-induced ERK phosphorylation in whole lung homogenates in rats. [3]

Protocol

Cell Research: [2]
+ Expand
  • Cell lines: KRJ-I cell lines
  • Concentrations: ~1 μM
  • Incubation Time: 24 hours
  • Method: 5×103 cells/mL, seeds in 96-well plates at 100 μL (4 plates/experimental condition) are stimulated with PRX-08066 (0.1 μM to 100 nM: n = 6 wells/concentration). After 24 hours, mitochondrial activity is measured after adding MTT (3-[4,5-dimethylthiazol-2-ly]-2.5-diphenyltetrazolium bromide: 0.5mg/mL per well) for 3 hours. The optical density is read photospectrometrically at 595 nm using a microplate reader. 29 Results are normalized to control (unstimulated cells) and the effective half-maximal concentrations calculated.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Male Sprague-Dawley rats
  • Formulation: 0.5% methylcellulose (w/v)
  • Dosages: 100 mg/kg
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 104 mg/mL (200.78 mM)
Water 104 mg/mL (200.78 mM)
Ethanol 98 mg/mL (189.2 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 517.96
Formula

C19H17ClFN5S.C4H4O4

CAS No. 866206-55-5
Storage powder
in solvent
Synonyms N/A

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID