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| 50mg |
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| 250mg |
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Purity: ≥98%
Ouabain (Ouabain Octahydrate; Acocantherine; G-Strophanthin; Strodival; NSC-25485; NSC25485) is a novel, potent and selective Na+/K+, -ATPase inhibitor with the potential to treat heart failure due to myocardial infarction. It binds to α2 /α3 subunit with Ki of 41 nM/15 nM. Ouabain (100 nM) inhibits ATPase activities with 25%. Ouabain (0.1 μM-1.0 μM) inhibits the Na+ pump and increases stored Ca2+ in cultured rat astrocytes. High Ouabain affinity isoforms are confined to a reticular distribution within the PM that paralleled underlying endoplasmic or sarcoplasmic reticulum.
| ln Vitro |
Ouabain (100 μM) stimulates NLRP3 inflammasome activation and IL-1β release in macrophages. Ouabain-induced NLRP3 inflammasome activation is mediated through K+ efflux[1]. Ouabain (3 nM) affects the expression of EMT markers in NHK and ADPKD cells, and modifies cell-cell adhesion qualities in ADPKD. Moreover, ouabain promotes migration of ADPKD cells, selectively modulates tight junctions, and modulates adherens junctions in ADPKD cells in a selective manner. Ouabain also promotes TGFβ-Smad3 signaling, changes TER in ADPKD cells[2]. Ouabain (25, 50 or 100 nM) administration dramatically lowers cell proliferation and viability in Raji cells in a dose-dependent manner, with IC50 of 76.48±4.03 nM. Ouabain increases the frequency of apoptotic cells, activates autophagy, and upregulates Beclin -1 in Raji cells[4].
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| ln Vivo |
When mice are primed with LPS, ouabain (3 mg/kg) dramatically reduces heart contractile force with an increased LVESD. A lack of IL-1β reduces the damage and malfunction of the heart caused by ouabain. Ouabain-induced cardiac inflammation is partly attributed to the secretion of IL-1β by infiltrating macrophages. The effects of ouabain-induced cardiac dysfunction and macrophage infiltration are mitigated by NLRP3 and Casp1 deficiency[1]. Wistar rat thymocytes' ABCB1 activity is modulated by ouabain (30 µg/kg, ip), and Swiss mice's thymocytes respond similarly to 300 µg/kg of the drug. Rats treated with ouabain for 14 days show a substantial increase in MAP[3].
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| Animal Protocol |
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| References |
[1]. Kobayashi M, et al. The cardiac glycoside ouabain activates NLRP3 inflammasomes and promotes cardiac inflammation and dysfunction. PLoS One. 2017 May 11;12(5):e0176676.
[2]. Venugopal J, et al. Ouabain promotes partial epithelial to mesenchymal transition (EMT) changes in human autosomal dominant polycystic kidney disease (ADPKD) cells. Exp Cell Res. 2017 Jun 15;355(2):142-152. [3]. Lima DB, et al. Ouabain-induced alterations in ABCB1 of mesenteric lymph nodes and thymocytes of rats and mice. Oncol Lett. 2016 Dec;12(6):5275-5280. [4]. Meng L, et al. Ouabain induces apoptosis and autophagy in Burkitt's lymphoma Raji cells. Biomed Pharmacother. 2016 Dec;84:1841-1848 |
| Molecular Formula |
C29H44O12.8H2O
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| Molecular Weight |
728.77
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| CAS # |
11018-89-6
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| Related CAS # |
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| SMILES |
O([H])[C@]12C([H])([H])C([H])([H])[C@]([H])(C3=C([H])C(=O)OC3([H])[H])[C@@]1(C([H])([H])[H])C([H])([H])[C@]([H])([C@]1([H])[C@@]3(C([H])([H])O[H])[C@@]([H])(C([H])([H])[C@@]([H])(C([H])([H])[C@]3(C([H])([H])C([H])([H])[C@]12[H])O[H])O[C@@]1([H])[C@@]([H])([C@@]([H])([C@]([H])([C@]([H])(C([H])([H])[H])O1)O[H])O[H])O[H])O[H])O[H]
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| InChi Key |
LPMXVESGRSUGHW-KAPJGFEOSA-N
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| InChi Code |
InChI=1S/C29H44O12/c1-13-22(34)23(35)24(36)25(40-13)41-15-8-19(32)28(12-30)21-17(3-5-27(28,37)9-15)29(38)6-4-16(14-7-20(33)39-11-14)26(29,2)10-18(21)31/h7,13,15-19,21-25,30-32,34-38H,3-6,8-12H2,1-2H3/t13-,15?,16+,17+,18+,19?,21+,22-,23+,24+,25-,26+,27?,28+,29-/m0/s1
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| Chemical Name |
3-(6-Deoxy-alpha-L-mannopyranosyloxy)-1,5,11a,14,19-pentahydroxycard-20(22)-enolide
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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 | 1.3722 mL | 6.8609 mL | 13.7218 mL | |
| 5 mM | 0.2744 mL | 1.3722 mL | 2.7444 mL | |
| 10 mM | 0.1372 mL | 0.6861 mL | 1.3722 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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