Tanshinone IIA sulfonate sodium

Catalog No.S3766

For research use only.

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. Sodium tanshinone IIA sulfonate (STS) is a potent negative allosteric modulator of the human purinergic receptor P2X7. Sodium tanshinone IIA sulfonate (STS) inhibits the activity of CYP3A4 and store-operated Ca2+ entry (SOCE) through store-operated Ca2+ channels (SOCC) via downregulating the expression of transient receptor potential canonical proteins (TRPC).

Tanshinone IIA sulfonate sodium Chemical Structure

CAS No. 69659-80-9

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Biological Activity

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. Sodium tanshinone IIA sulfonate (STS) is a potent negative allosteric modulator of the human purinergic receptor P2X7. Sodium tanshinone IIA sulfonate (STS) inhibits the activity of CYP3A4 and store-operated Ca2+ entry (SOCE) through store-operated Ca2+ channels (SOCC) via downregulating the expression of transient receptor potential canonical proteins (TRPC).
Targets
SOCE [2]
()
P2X7 [4]
()
CYP3A4 [1]
(Cell-free assay)
6.377 μM
In vitro

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[1]. STS upregulates the protein expression of Bcl-2 and downregulates the proteins expression of Bax and Caspase-3[2]. 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[3].

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[1]. 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[2]. STS has been clinically used for decades in the treatment of numerous cardiovascular diseases, such as hypertension, atherosclerosis, and others[3].

Protocol (from reference)

Cell Research:

[3]

  • Cell lines: pulmonary arterial smooth muscle cells (PASMCs)
  • Concentrations: 12.5 μM
  • Incubation Time: 60 h
  • Method:

    Rat PASMCs are digested by collagenase and then cultured in low-sugar DMEM medium containing 10% fetal bovine serum. When the fusion of cells is at 60-70%, the medium is replaced with the low-sugar DMEM medium containing 0.5% fetal bovine serum in which cells are cultured for 24 h to be homogenized. After the cells are grown to ∼80%, they are randomly divided into four groups, two of which are treated with STS (12.5 μM). STS group and STS-free group are randomly exposed to normoxic environment and hypoxic conditions (4% O2, 60 h). 60 h of prolonged hypoxic stress (4% O2) can effectively lead to elevated proliferation and migration of primary cultured distal PASMCs. This mimics similar hypoxic responses as the PASMCs isolated from the CHPH rats, as the hypoxic elevation of [Ca2+]i, SOCE, and upregulation of TRPC expression in cultured PASMCs only occur at 60 h or later time points of hypoxic exposure. In this study, both incubators are set to 37°C, 5% CO2. The total protein of these cells is extracted by RIPA buffer.

  • (Only for Reference)
Animal Research:

[2]

  • Animal Models: Kunming mice
  • Dosages: 10 mg/kg and 20 mg/kg
  • Administration: oral administration
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 79 mg/mL
(199.29 mM)


* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 396.39
Formula

C19H17O6S.Na

CAS No. 69659-80-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(OC2=C1C(=O)C(=O)C3=C2C=CC4=C3CCCC4(C)C)S(=O)(=O)[O-].[Na+]

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