PRX-08066 Maleic acid5-HT2B receptor antagonist,potent and selective CAS# 866206-55-5 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 866206-55-5 | SDF | Download SDF |
| PubChem ID | 51348293 | Appearance | Powder |
| Formula | C23H21ClFN5O4S | M.Wt | 517.96 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble in DMSO > 10 mM | ||
| Chemical Name | (Z)-but-2-enedioic acid;5-[[4-[(6-chlorothieno[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]methyl]-2-fluorobenzonitrile | ||
| SMILES | C1CN(CCC1NC2=C3C=C(SC3=NC=N2)Cl)CC4=CC(=C(C=C4)F)C#N.C(=CC(=O)O)C(=O)O | ||
| Standard InChIKey | RPYIKXHIQXRXEM-BTJKTKAUSA-N | ||
| Standard InChI | 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- | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | PRX-08066 Maleic acid is a selective antagonist of 5-HT2B receptor with IC50 value of 3.4 nM. | |||||
| Targets | 5-HT2B | |||||
| IC50 | 3.4 nM | |||||
PRX-08066 Maleic acid Dilution Calculator
PRX-08066 Maleic acid Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.9307 mL | 9.6533 mL | 19.3065 mL | 38.613 mL | 48.2663 mL |
| 5 mM | 0.3861 mL | 1.9307 mL | 3.8613 mL | 7.7226 mL | 9.6533 mL |
| 10 mM | 0.1931 mL | 0.9653 mL | 1.9307 mL | 3.8613 mL | 4.8266 mL |
| 50 mM | 0.0386 mL | 0.1931 mL | 0.3861 mL | 0.7723 mL | 0.9653 mL |
| 100 mM | 0.0193 mL | 0.0965 mL | 0.1931 mL | 0.3861 mL | 0.4827 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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PRX-08066 Maleic acid is a selective 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist [1].
5-HT receptors are a group of G protein-coupled receptors and play an important role in schizophrenia, feeding disorders, perception, depression, migraines, hypertension, anxiety, hallucinogens, and gastrointestinal dysfunctions.
In NET cell line, KRJ-I, PRX-08066 inhibited 5-HT secretion and cell proliferation and decreased ERK1/2 phosphorylation and profibrotic growth factor synthesis and secretion (TGFβ1, CTGF and FGF2). In the KRJ-I:HEK293 coculture system, PRX-08066 significantly reduced 5-HT release, Ki67, CTGF, TGFβ1 and FGF2 transcription in the KRJ-I cell line. 5-HT itself stimulated HEK293 proliferation [2].
PRX-08066 has preclinical safety profile, good bioavailability, and low acute toxicity, which is under phase II clinical trials for the treatment of hypoxia-induced pulmonary hypertension syndromes and pulmonary hypertension [3].
In the monocrotaline (MCT)-induced PAH male rats model, PRX-08066 (100 mg/kg) significantly increased right ventricular ejection fraction and reduced peak PA pressure at 50 and 100 mg/kg. Morphometric assessment of pulmonary arterioles showed PRX-08066 significantly reduced medial wall thickening, lumen occlusion and RV hypertrophy. Also, PRX-08066 diminished pulmonary vascular remodeling [1].
References:
[1]. Porvasnik SL, Germain S, Embury J, 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, Kidd M, Giovinazzo F, 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. Cance, 2010, 116(12): 2902-2912.
[3]. Kim SK, Li Y, Abrol R, et al. Predicted structures and dynamics for agonists and antagonists bound to serotonin 5-HT2B and 5-HT2C receptors. J Chem Inf Model, 2011, 51(2): 420-433.
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