PRX-08066 Maleic acid

Alias: PRX-08066; MT500; MT-500; PRX 08066; PRX08066; MT 500
Cat No.:V0969 Purity: ≥98%
PRX-08066 maleic acid (MT500; MT-500; PRX 08066; PRX08066), the maleic acid salt of PRX08066, is a novel, potent and selective 5-HT2B receptor antagonist with important biological activity.
PRX-08066 Maleic acid Chemical Structure CAS No.: 866206-55-5
Product category: 5-HT Receptor
This product is for research use only, not for human use. We do not sell to patients.
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Other Forms of PRX-08066 Maleic acid:

  • PRX-08066
Official Supplier of:
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Product Description

PRX-08066 maleic acid (MT500; MT-500; PRX 08066; PRX08066), the maleic acid salt of PRX08066, is a novel, potent and selective 5-HT2B receptor antagonist with important biological activity. It inhibits 5-HT2B with an IC50 of 3.4 nM. It inhibits 5-HT2B with an IC50 of 3.4 nM. In the MCT rat model, PRX-08066 reduces the severity of pulmonary arterial hypertension. In rats, PRX-08066 decreases right ventricular hypertrophy and pulmonary arterial hypertension brought on by monocrotaline. In the SI-NET cell line KRJ-I that expressed 5-HT2B, PRX-08066 suppressed proliferation and secretion of 5-HT while also lowering phosphorylation of ERK1/2 and profibrotic growth factor synthesis and secretion (fibroblast growth factor [FGF2], connective tissue growth factor [CTGF], and transforming growth factor beta 1 [TGFbeta1]).

Biological Activity I Assay Protocols (From Reference)
Targets
5-HT2B ( IC50 = 3.4 )
ln Vitro

In vitro activity: PRX-08066 suppresses thymidine incorporation with an IC50 of 3 nM and inhibits 5-HT-induced mitogen-activated protein kinase activation with an IC50 of 12 nM in Chinese hamster ovary cells expressing the human 5-HT2BR, indicating that PRX-08066 may be able to prevent the pathologic 5-HT-induced vascular muscularization linked to PAH.[1] In the 5-HT(2B) expressing SI-NET cell line, KRJ-I, PRX-08066 inhibits cell proliferation with an IC50 of 0.46 nM and a maximum inhibition of 20%; in 5-HT secretion, it has an IC50 of 6.9 nM and a maximum inhibition of 30%; in NCI-H720 cells, PRX-08066 inhibits isoproterenol-stimulated 5-HT release with an IC50 of 1.25 nM and a maximum inhibition of 60%. 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. In KRJ-I cells, PRX-08066 increases the transcript levels of caspase 3 and decreases the levels of Ki67 (84%) and Ki67 protein (36.8%). In KRJ-I cells, PRX-08066 reduces the amount of TGFβ1, FGF2, and TPH1 transcripts. In KRJ-I cells, PRX-08066 considerably raises the percentage of dead cells (34%) when compared to untreated controls. In HEK293 cells, PRX-08066 significantly raises caspase 3 activity (52%) and the proportion of dead/caspase 3 positive cells (76%).[2]

ln 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. In comparison to rats treated with MCT, PRX-08066 also significantly lowers the right ventricle (RV)/body weight and the RV/left ventricle + septum. While maintaining cardiac function, PRX-08066 significantly reduces the increase in pulmonary artery pressure and RV hypertrophy. In both rats and mice, PRX-08066 dramatically lowers the hypoxia-dependent rise in right ventricular systolic pressure without changing the animals' systemic mean arterial pressure. PRX-08066 (100 mg/kg) prevents ERK phosphorylation induced by monocrotaline in whole lung homogenates as well as right ventricular systolic pressure in rats.[3]
Cell Assay
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). Following a 24-hour period, mitochondrial activity is assessed by adding 3-[4,5-dimethylthiazol-2-ly]-2.5-diphenyltetrazolium bromide (0.5 mg/mL per well) and waiting three hours. A microplate reader is used to measure the optical density photospectroscopically at 595 nm. 29 Results are normalized to control (unstimulated cells) and the effective half-maximal concentrations calculated.
Animal Protocol
Dissolved in 0.5% methylcellulose (w/v); 100 mg/kg; Oral gavage
Male Sprague-Dawley rats
References

[1]. J Pharmacol Exp Ther . 2010 Aug;334(2):364-72.

[2]. Cancer . 2010 Jun 15;116(12):2902-12.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C23H21CLFN5O4S
Molecular Weight
517.96
Exact Mass
517.1
CAS #
866206-55-5
SMILES
C1CN(CCC1NC2=C3C=C(SC3=NC=N2)Cl)CC4=CC(=C(C=C4)F)C#N.C(=C\C(=O)O)\C(=O)O
InChi Key
RPYIKXHIQXRXEM-BTJKTKAUSA-N
InChi Code
InChI=1S/C19H17ClFN5S.C4H4O4/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;5-3(6)1-2-4(7)8/h1-2,7-8,11,14H,3-6,10H2,(H,23,24,25);1-2H,(H,5,6)(H,7,8)/b;2-1-
Chemical Name
(Z)-but-2-enedioic acid;5-[[4-[(6-chlorothieno[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]methyl]-2-fluorobenzonitrile
Synonyms
PRX-08066; MT500; MT-500; PRX 08066; PRX08066; MT 500
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~104 mg/mL (~200.8 mM)
Water: ~104 mg/mL (~200.8 mM)
Ethanol: ~98 mg/mL (~189.2 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.9307 mL 9.6533 mL 19.3065 mL
5 mM 0.3861 mL 1.9307 mL 3.8613 mL
10 mM 0.1931 mL 0.9653 mL 1.9307 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Biological Data
  • PRX-08066 Maleic acid
    MRI assessment of RV mass and ejection fraction after 4 weeks of PRX-08066 treatment.J Pharmacol Exp Ther.2010 Aug;334(2):364-72.
  • PRX-08066 Maleic acid
    The effects of PRX-08066 on hemodynamic function in the rat MCT model.J Pharmacol Exp Ther.2010 Aug;334(2):364-72.
  • PRX-08066 Maleic acid
    Pulmonary artery remodeling after 5 weeks of PXR-08066 treatment.J Pharmacol Exp Ther.2010 Aug;334(2):364-72.
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