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Tanshinone IIA sulfonate sodium

Catalog No. T2946   CAS 69659-80-9
Synonyms: Tanshinone IIA sulfonate, Sodium Tanshinone IIA sulfonate, Tanshinone IIA sodium sulfonate, sodium

Tanshinone IIA sulfonate sodium (Tanshinone IIA sodium sulfonate) is a water-soluble derivative of tanshinone IIA extracted from Savia miltiorrhiza; a potent negative allosteric modulator of the human purinergic receptor P2X7. Tanshinone IIA sulfonate sodium (12.5 μM) inhibits hypoxia-induced PKG and PPAR-γ downregulation in PASMCs and distal pulmonary arteries of rats.

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Tanshinone IIA sulfonate sodium Chemical Structure
Tanshinone IIA sulfonate sodium, CAS 69659-80-9
Pack Size Availability Price/USD Quantity
10 mg In stock $ 39.00
25 mg In stock $ 64.00
50 mg In stock $ 93.00
100 mg In stock $ 137.00
500 mg In stock $ 342.00
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Purity: 99.9%
Purity: 99.04%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Tanshinone IIA sulfonate sodium (Tanshinone IIA sodium sulfonate) is a water-soluble derivative of tanshinone IIA extracted from Savia miltiorrhiza; a potent negative allosteric modulator of the human purinergic receptor P2X7. Tanshinone IIA sulfonate sodium (12.5 μM) inhibits hypoxia-induced PKG and PPAR-γ downregulation in PASMCs and distal pulmonary arteries of rats.
Targets&IC50 CYP3A4:6.377 μM
In vitro Sodium Tanshinone IIA sulfonate (12.5 μM) effectively inhibits hypoxia-induced downregulation of PKG and PPAR-γ in PASMCs and the distal pulmonary arteries of rats, indicating its role in preserving pulmonary vascular function. This compound also prevents the reduction of TRPC1 and TRPC6 expression in hypoxic PASMCs, a process that is reversible upon specific knockdown of PKG or PPAR-γ. This suggests the involvement of the PKG-PPAR-γ signaling axis in mitigating the proliferative response of PASMCs under hypoxic conditions. Furthermore, a PPAR-γ agonist enhances the compound's ability to maintain basal calcium levels and store-operated calcium entry (SOCE) in PASMCs. In terms of drug metabolism, Sodium Tanshinone IIA sulfonate dose-dependently inhibits CYP3A4 activity in human liver microsomes (HLMs) and CYP3A4 isoform, with minimal impact on other CYP enzymes, suggesting a specific interaction with the CYP3A4 pathway. The kinetic parameters for its inhibition of CYP3A4 are detailed for both HLMs and the CYP3A4 isoform. Due to its significant inhibitory effect on CYP3A4, Sodium Tanshinone IIA sulfonate has the potential for drug-drug interactions when administered with other CYP3A4 substrates.
In vivo Sodium Tanshinone IIA sulfonate administered at dosages of 10 mg/kg and 20 mg/kg, in conjunction with Donepezil, effectively reduces escape latency, enhances the number of times subjects crossed the original platform location, and extends the duration spent in the target quadrant in experimental settings. This compound notably diminishes acetylcholinesterase (AChE) activity while boosting choline acetyltransferase (ChAT) activity within the hippocampus and cortex of SCOP-treated mice, alongside increasing superoxide dismutase (SOD) activity and reducing malondialdehyde (MDA) and reactive oxygen species (ROS) levels in the same regions. At a preventive dosage of 30 mg/kg/day, Sodium Tanshinone IIA sulfonate mitigates the characteristic alterations induced by hypoxia in a chronic hypoxia PH rat model. Moreover, when administered intraperitoneally at dosages of 20, 10, and 5 mg/kg, it effectively prevents peritoneal adhesion without impeding anastomotic healing in rats, demonstrating increased peritoneal lavage fluid tPA activity and tPA/PAI-1 ratio, alongside decreased TGF-β1 and collagen I expressions in ischemic tissues.
Source
Synonyms Tanshinone IIA sulfonate, Sodium Tanshinone IIA sulfonate, Tanshinone IIA sodium sulfonate, sodium
Molecular Weight 396.39
Formula C19H17O6S·Na
CAS No. 69659-80-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (126.14 mM), The compound is unstable in solution. Please use soon.

TargetMolReferences and Literature

1. Xu QQ, et al. Sodium Tanshinone IIA Sulfonate Attenuates Scopolamine-Induced Cognitive Dysfunctions via Improving Cholinergic System. Biomed Res Int. 2016;22016:19852536. 2. Jiang, Q., Lu, W., Yang, K., Hadadi, C., Fu, X., & Chen, Y. et al. (2016). Sodium tanshinone IIA sulfonate inhibits hypoxia-induced enhancement of SOCE in pulmonary arterial smooth muscle cells via the PKG-PPAR-γ signaling axis. American Journal Of Physiology-Cell Physiology, 311(1), C136-C149. doi: 10.1152/ajpcell.00252.2015 3. Ouyang DS, et al. Kinetics of cytochrome P450 enzymes for metabolism of sodium tanshinone IIA sulfonate in vitro. Chin Med. 2016 Mar 22;11:11. 4. Chen D, et al. Sodium tanshinone IIA sulfonate and its interactions with human CYP450s. Xenobiotica. 2016 Dec;46(12):1085-1092. Epub 2016 Mar 2. 5. Lin S, et al. [Sodium tanshinone IIA sulfonate prevents postoperative peritoneal adhesions in rats by enhancing the activity of the peritoneal fibrinolytic system]. Nan Fang Yi Ke Da Xue Xue Bao. 2016 Feb;36(2):260-4.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Inhibitor Library Anti-Cancer Clinical Compound Library Kinase Inhibitor Library FDA-Approved Kinase Inhibitor Library Drug Repurposing Compound Library Ion Channel Inhibitor Library Neuronal Signaling Compound Library Bioactive Compound Library

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Keywords

Tanshinone IIA sulfonate sodium 69659-80-9 Membrane transporter/Ion channel Metabolism Neuroscience Calcium Channel P450 CaMK CRAC Channel Calcium release-activated channels Tanshinone IIA sulfonate Sodium Tanshinone IIA sulfonate Ca2+ release-activated Ca2+ channels Tanshinone IIA sodium sulfonate inhibit Inhibitor sodium inhibitor

 

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