| 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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Purity: ≥98%
Rostafuroxin (formerly PST2238; PST-2238) is an ouabain and Na/K-ATPase antagonist with antihypertensive activities. It is able to displace [3H]ouabain from the dogkidney Na+/K+-ATPase with IC50 of 1.5 nM. Rostafuroxin protects from podocyte injury and proteinuria induced by adducin genetic variants and ouabain. Rostafuroxin ameliorates endothelial dysfunction and oxidative stress in resistance arteries from deoxycorticosterone acetate-salt hypertensive rats: the role of Na+K+-ATPase/ cSRC pathway. Rostafuroxin corrects renal and vascular Na+-K+- ATPase alterations in ouabain and adducin-dependent hypertension.
| ln Vitro |
Ouabain binding and signaling are competitively inhibited by rostafuroxin (PST 2238). Rostafuroxin reverses ouabain-induced Src-dependent phosphorylation and activates Na+,K+-ATPase, counteracting the molecular and functional effects of ouabain [3][4]. Within 24 hours of treatment, the viability of A549 and HSAEC cells was lowered by less than 20% by rostafuroxin (0.125–128 μM). In HSAEC (IC50=1.8 μM) and A549 cells (IC50=14.8 μM), prostafuroxin suppresses RSV-GFP expression [3]. Rostafuroxin lacks cardiotonic activity in isolated guinea pig atria, replaces [3H]Ouabain at the dog kidney Na+,K+-ATPase receptor (IC50=1.5 nM), and is consistent with hormone (estrogen, progesterone, androgen, mineralocorticoid) and general (R1, R2, a1, a2, A1, A2, M1, M2, H1, H2, 5-HT1, 5-HT2, Ca2+ channels, TXA2/PGH2, PAF, GABAA, GABAB, DA-NE-5-HT uptake, glutamate, glycine, benzodiazepines) receptors [1].
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| ln Vivo |
Rostafuroxin (PST 2238; gavage; 1 mg/kg/day; 3 weeks) improves acetylcholine-induced relaxation and lowers SBP [4].
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| Animal Protocol |
Animal/Disease Models: Male 7weeks old Wistar rats [4]
Doses: 1 mg/kg Route of Administration: gavage; daily; for 3 weeks Experimental Results: diminished systolic blood pressure, improved acetylcholine through enhanced nitric oxide synthesis and bioavailability Induced relaxation reduces superoxide anion production by NAD(P)H oxidase and cyclooxygenase-2, and reduces phosphorylation of the cytoplasmic tyrosine kinase Src. |
| References |
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| Additional Infomation |
Rostafuroxin has been used in trials studying the treatment of Essential Hypertension.
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| Molecular Formula |
C23H34O4
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|---|---|
| Molecular Weight |
374.51366
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| Exact Mass |
374.245
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| CAS # |
156722-18-8
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| PubChem CID |
153976
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
451.3±45.0 °C at 760 mmHg
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| Flash Point |
226.7±28.7 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.591
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| LogP |
3.56
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
27
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| Complexity |
609
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| Defined Atom Stereocenter Count |
8
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| SMILES |
C[C@]12CC[C@@H](C[C@H]1CC[C@@H]3[C@@H]2CC[C@]4([C@@]3(CC[C@@]4(C5=COC=C5)O)O)C)O
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| InChi Key |
AEAPORIZZWBIEX-DTBDINHYSA-N
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| InChi Code |
InChI=1S/C23H34O4/c1-20-8-5-17(24)13-15(20)3-4-19-18(20)6-9-21(2)22(25,10-11-23(19,21)26)16-7-12-27-14-16/h7,12,14-15,17-19,24-26H,3-6,8-11,13H2,1-2H3/t15-,17+,18+,19-,20+,21-,22+,23+/m1/s1
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| Chemical Name |
(3S,5R,8R,9S,10S,13S,14S,17S)-17-(furan-3-yl)-10,13-dimethylhexadecahydro-14H-cyclopenta[a]phenanthrene-3,14,17-triol
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| Synonyms |
PST2238; PST 2238; PST-2238; Rostafuroxin
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ≥ 50 mg/mL (~133.51 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.68 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.68 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.68 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6702 mL | 13.3508 mL | 26.7016 mL | |
| 5 mM | 0.5340 mL | 2.6702 mL | 5.3403 mL | |
| 10 mM | 0.2670 mL | 1.3351 mL | 2.6702 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.
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