Tanshinone IIA sulfonate (sodium)
Molecular Weight(MW): 396.39
Sodium tanshinone IIA sulfonate (STS) is a water-soluble derivative of tanshinone IIA isolated as the main pharmacologically active natural compound from a traditional Chinese herbal medicine, the dried root of Salvia miltiorrhiza Bunge known as Danshen; a potent negative allosteric modulator of the human purinergic receptor P2X7.
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|Description||Sodium tanshinone IIA sulfonate (STS) is a water-soluble derivative of tanshinone IIA isolated as the main pharmacologically active natural compound from a traditional Chinese herbal medicine, the dried root of Salvia miltiorrhiza Bunge known as Danshen; a potent negative allosteric modulator of the human purinergic receptor P2X7.|
Sodium tanshinone IIA sulfonate (STS) inhibits the activity of CYP3A4 in a dose-dependent manner in the HLMs and CYP3A4 isoform. Other CYP isoforms, including CYP1A2, CYP2A6, CYP2C9, CYP2D6, CYP2E1, and CYP2C19, show minimal or no effect on the metabolism of STS. Thus, STS is a potent inhibitor for CYP3A4. STS upregulates the protein expression of Bcl-2 and downregulates the proteins expression of Bax and Caspase-3. Sodium tanshinone IIA sulfonate (STS) inhibits store-operated Ca2+ entry (SOCE) through store-operated Ca2+ channels (SOCC) via downregulating the expression of transient receptor potential canonical proteins (TRPC). STS treatment can effectively prevent the hypoxia-mediated inhibition of the PKG-PPAR-γ signaling axis in rat distal pulmonary arterial smooth muscle cells (PASMCs) and distal pulmonary arteries. It can also prevent hypoxia-mediated increases in intracellular calcium homeostasis and cell proliferation, by targeting and restoring the hypoxia-inhibited PKG-PPAR-γ signaling pathway in PASMCs.
|In vivo||The metabolic rate of Sodium tanshinone IIA sulfonate (STS) in rats is fast, the T1/2 is not more than 0.9 h. tanshinone IIA has been reported to possess neuroprotective effects against Alzheimer’s disease (AD). STS decreases the activity of acetylcholinesterase (AChE) and increases the activity of choline acetyltransferase (ChAT) in the hippocampus and cortex of SCOP-treated mice. It increases the activity of superoxide dismutase (SOD) and decreases the levels of malondialdehyde (MDA) and reactive oxygen species (ROS) in hippocampus and cortex. STS administration (10 mg/kg and 20 mg/kg) could improve SCOP-induced learning and memory impairment in Kunming mice. Meanwhile, STS could obviously improve central cholinergic neurotransmission and attenuate oxidative damage. STS has cardioprotective effects on cardiovascular injury. STS has been clinically used for decades in the treatment of numerous cardiovascular diseases, such as hypertension, atherosclerosis, and others.|
|In vitro||DMSO||79 mg/mL (199.29 mM)|
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