| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| Other Sizes |
| Targets |
prodrug of PGI2; Vasodilator[1]
Beraprost sodium targets the prostacyclin (IP) receptor as an agonist. By activating the IP receptor, it stimulates adenylate cyclase, increasing intracellular cAMP levels. This leads to vasodilation, inhibition of platelet aggregation, and cytoprotection. Beraprost is a stable analog of prostacyclin, with a longer half-life than the natural compound. Its vasodilatory, antiplatelet, and cytoprotective effects are mediated through IP receptor activation. |
|---|---|
| ln Vitro |
Beraprost sodium (0.1, 1.0, and 10.0 μM; 24 hours) treatment leads
to a significant increase in the number of tube formation, BPS plays an
important role on angiogenic activity[1]. Beraprost sodium (0.1, 1.0,
and 10.0 μM; 24 hours) treatment let VE-cadherin at regions of cell–cell
contact becomes more abundant and the morphology of endothelial cells
tends to be normal compared with those cultured under hypoxia
conditions[1].
|
| ln Vivo |
Beraprost sodium (oral adminstration; 0.6 mg/kg; once daily; 3 or 7
days) can mitigate the development of renal interstitial fibrosis,
decrease renal oxidative stress through its potential vasodilation
effect, and further prevent renal interstitial fibrosis[1]. Animal
Model: 6-8-week-old C57Bl/6J Male Mice[1] Dosage: 0.6 mg/kg
Administration: Oral adminstration; 0.6 mg/kg; once daily; 3 or 7 days
Result: Mitigated the development of renal interstitial fibrosis.
|
| Enzyme Assay |
Tube formation assay[1]
In brief, endothelial cells (1 × 104) were seeded in a 48-well plate coated with 100 μl of growth factor-reduced Matrigel TM and incubated with and without varied concentrations of BPS (Beraprost sodium) at 0.1, 1.0, and 10.0 μmol/l for tube stabilization for 24 h at 37 °C. Tube formation was quantified by measuring the total tube loops in five random microscopic fields with a computer-assisted microscope
In vitro receptor binding assays for beraprost sodium involve measuring its binding affinity to the prostacyclin (IP) receptor. The receptor is incubated with a radiolabeled ligand and varying concentrations of beraprost. The displacement of the radiolabeled ligand is measured, and the IC₅₀ or Ki value is calculated. The compound's functional activity as an IP receptor agonist is assessed by measuring cAMP accumulation in cells expressing the IP receptor. These assays confirm the compound's mechanism as a prostacyclin analog. |
| Cell Assay |
The HUVECs were cultured in a modified minimum essential medium supplemented with 10% fetal bovine serum and 1% mycillin at 37 °C in 5% CO2 and 95% air. HUVECs in hypoxia group were cultured for 12 h into an airtight humidified chamber flushed with a gas mixture containing 5% CO2, 95% N2, and 1% O2 at 37 °C. HUVECs in hypoxia + BPS group were cultured with BPS (Beraprost sodium) at 1.0 μmol/l. The cells were cultured according to the manufacturer’s instructions and the culture medium was changed every 2 or 3 days. HUVECs at passage 3 were used for the following experiments[1].
In vitro cell-based assays for beraprost sodium evaluate its effects on platelet aggregation and vascular function. Platelets are treated with beraprost, and aggregation is induced by agonists such as ADP or collagen. Inhibition of platelet aggregation is measured using aggregometry. Vascular smooth muscle cells are treated with beraprost, and vasodilation is assessed by measuring changes in cell contraction or relaxation. These assays confirm the compound's functional activity as a prostacyclin analog. |
| Animal Protocol |
Animal/Disease Models: 6-8 weeks old C57Bl/6J male mice [1]br>
Doses: 0.6 mg/kg
Route of Administration: Oral; 0.6 mg/kg; one time/day; 3 or 7 daysbr> Experimental Results: Reduce renal interstitial fibrosis develop. In vivo animal experiments for beraprost sodium have been conducted in animal models of pulmonary hypertension and ischemia-reperfusion injury. The compound is administered orally or intravenously, and hemodynamic parameters such as pulmonary artery pressure and vascular resistance are measured. The compound's effects on platelet aggregation and tissue protection are assessed. Pharmacokinetic studies are conducted to determine the compound's half-life, clearance, and tissue distribution. Comprehensive in vivo studies are available from clinical development. |
| ADME/Pharmacokinetics |
Beraprost sodium is absorbed after oral administration and is metabolized in the liver. It has a molecular weight of 420.47 g/mol. The compound's half-life, bioavailability, and excretion profile have been characterized in clinical studies. Beraprost is used in the treatment of pulmonary hypertension and is available as a prescription medication in some countries.
|
| Toxicity/Toxicokinetics |
The toxicity of beraprost sodium is generally low at therapeutic doses. Common side effects include headache, flushing, nausea, and dizziness. The compound should be used with caution in patients with bleeding disorders or hypotension. Beraprost is available as a prescription medication for pulmonary hypertension in some countries.
|
| References |
[1] Effect of orally active\nprostacyclin analogue on survival of outpatients with primary pulmonary\nhypertension. J Am Coll Cardiol 34 1188-1192 (1999). [2] Platelet-aggregation inhibition and\nhemodynamic effects of beraprost sodium, a new oral prostacyclin\nderivative: A study in healthy male subjects. Can J Physiol Pharmacol 74\n887-893 (1996). [3] Effect\nof beraprost sodium, a stable prostaglandin I2 analogue, on platelet\naggregation in diabetes mellitus. Int J Clin Pharmacol Res 16 99-102\n(1996). |
| Additional Infomation |
Beraprost sodium is the organic sodium salt of beraprost. In Japan, it is used to treat chronic arterial occlusive disease and primary pulmonary hypertension. It has antihypertensive, platelet aggregation inhibitory, prostaglandin receptor agonist inhibitory, vasodilatory, and anti-inflammatory effects. It contains beraprost (1-).
Beraprost sodium is a synthetic prostacyclin analog with vasodilatory, antiplatelet, and cytoprotective effects. It inhibits platelet aggregation and dilates pulmonary vessels. Beraprost is used in the treatment of pulmonary hypertension and is being studied for reperfusion injury. It has a molecular formula of C₂₄H₂₉NaO₅ and a molecular weight of 420.47 g/mol. Beraprost is available as a prescription medication in some countries. |
| Molecular Formula |
C24H29NAO5
|
|---|---|
| Molecular Weight |
420.47
|
| Exact Mass |
420.191
|
| Elemental Analysis |
C, 68.56; H, 6.95; Na, 5.47; O, 19.02
|
| CAS # |
88475-69-8
|
| Related CAS # |
88430-50-6 (free acid);88475-69-8 (sodium); 496807-11-5
|
| PubChem CID |
23663404
|
| Appearance |
Typically exists as White to light yellow solids at room temperature
|
| Boiling Point |
572.1ºC at 760 mmHg
|
| Melting Point |
204-206ºC
|
| Flash Point |
193.1ºC
|
| LogP |
1.951
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
30
|
| Complexity |
665
|
| Defined Atom Stereocenter Count |
5
|
| SMILES |
[Na].O=C(CCCC1C2OC3C(C=2C=CC=1)C(C=CC(C(CC#CC)C)O)C(O)C3)O
|
| InChi Key |
YTCZZXIRLARSET-WGMXHSAISA-M
|
| InChi Code |
InChI=1S/C24H30O5.Na/c1-3-4-7-15(2)19(25)13-12-17-20(26)14-21-23(17)18-10-5-8-16(24(18)29-21)9-6-11-22(27)28;/h5,8,10,12-13,15,17,19-21,23,25-26H,6-7,9,11,14H2,1-2H3,(H,27,28);/q;+1/p-1/b13-12+;/t15?,17-,19+,20+,21-,23-;/m1./s1
|
| Chemical Name |
sodium;4-[(1R,2R,3aS,8bS)-2-hydroxy-1-[(E,3S)-3-hydroxy-4-methyloct-1-en-6-ynyl]-2,3,3a,8b-tetrahydro-1H-cyclopenta[b][1]benzofuran-5-yl]butanoate
|
| Synonyms |
BERAPROST SODIUM; Beraprost sodium salt; Procylin; 88475-69-8; Dorner; TRK-100; Berasus LA; TRK-100STP;
|
| HS Tariff Code |
2934.99.9001
|
| 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 (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3783 mL | 11.8915 mL | 23.7829 mL | |
| 5 mM | 0.4757 mL | 2.3783 mL | 4.7566 mL | |
| 10 mM | 0.2378 mL | 1.1891 mL | 2.3783 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
