Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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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]).
Targets |
5-HT2B ( IC50 = 3.4 )
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ln Vitro |
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ln Vivo |
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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.
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Animal Protocol |
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References |
Molecular Formula |
C23H21CLFN5O4S
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Molecular Weight |
517.96
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Exact Mass |
517.1
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CAS # |
866206-55-5
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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
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InChi Key |
RPYIKXHIQXRXEM-BTJKTKAUSA-N
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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-
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Chemical Name |
(Z)-but-2-enedioic acid;5-[[4-[(6-chlorothieno[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]methyl]-2-fluorobenzonitrile
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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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.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.