| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
TIIAS targets the purinergic receptor P2X7 as a negative allosteric modulator, inhibiting its function. It also inhibits store-operated Ca²⁺ entry (SOCE). In vitro, it primarily inhibits CYP3A4 activity. It inhibits hypoxia-induced PKG and PPAR-γ at 12.5 μM. Its anti-inflammatory effects are mediated through these and other pathways.
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| ln Vitro |
In rat PASMC and distal pulmonary arteries, hypoxia-induced downregulation of PKG and PPAR-γ is inhibited by sodium tanshinone IIA sulfonate (12.5 μM). Specific knockdown of PKG or PPAR-γ can counteract the inhibitory effect of sodium tanshinone IIA sulfonate on TRPC1 and TRPC6 expression in hypoxic PASMC. PKG or PPAR-γ specific deletion can counteract the inhibitory effects of sodium tanshinone IIA sulfonate on basal calcium concentration and SOCE in hypoxic PASMC. The inhibition of hypoxia PASMC proliferation by sodium tanshinone IIA sulfonate involves the PKG-PPAR-γ signaling pathway. The protective effect of sodium tanshinone IIA sulfonate on basal [Ca2+]i and SOCE in hypoxic PASMCs is enhanced by PPAR-γ agonists [2]. In a dose-dependent manner, sodium tanshinone IIA sulfonate suppresses CYP3A4 activity via HLM and CYP3A4 isoforms. For CYP3A4, the KM and Vmax values of STS were 7.5±1.4 µM and 6.8±0.3 nmol/nmol P450/minute, respectively; for HLM, the values were 54.8±14.6 µM and 0.9±0.1 nmol/mg protein/min. The effects of CYP1A2, CYP2A6, CYP2C9, CYP2D6, CYP2E1, and CYP2C19 on STS metabolism are negligible or nonexistent [3]. In a dose-dependent manner, sodium tanshinone IIA sulfonate suppresses CYP3A4 activity in both HLM and CYP3A4 isoforms. In vitro, sodium tanshinone IIA sulfonate primarily inhibits CYP3A4 activity. However, it may also interact with other CYP3A4 substrates in a pharmacological capacity [4].
TIIAS primarily inhibits CYP3A4 activity in vitro. In a dose-dependent manner, sodium tanshinone IIA sulfonate suppresses CYP3A4 activity in both human liver microsomes (HLM) and CYP3A4 isoforms. It inhibits hypoxia-induced PKG and PPAR-γ at 12.5 μM. It exhibits anti-inflammatory properties in rodent models. |
| ln Vivo |
Donepezil and sodium tanshinone IIA sulfonate (10 mg/kg, 20 mg/kg) reduced the escape delay, increased the number of times the platform crossed its initial position, and lengthened the amount of time in the target quadrant. In the hippocampus and cortex of SCOP-treated animals, sodium tanshinone IIA sulfonate decreases acetylcholinesterase (AChE) activity and enhances choline acetyltransferase (ChAT) activity. In the hippocampus and cortex, tanshinone IIA sodium sulfonate decreases the amounts of reactive oxygen species (ROS) and malondialdehyde (MDA) while increasing the activity of superoxide dismutase (SOD) [1]. In the chronic hypoxic PH rat model, tanshinone IIA sodium sulfonate prophylaxis (30 mg/kg/day) can mitigate the distinctive alterations brought on by hypoxia [2]. Rats treated intraperitoneally with sodium tanshinone IIA sulfonate (20, 10 and 5 mg/kg) are able to successfully avoid peritoneal adhesions without compromising anastomotic recovery. In the peritoneal lavage fluid of the ischemic tissue in the sodium tanshinone IIA sulfonate treatment group, tPA activity and tPA/PAI-1 ratio rose compared to the adhesion model group, while the expression of TGF-β1 and type I collagen reduced [5].
TIIAS exhibits anti-inflammatory properties in rodent models of hepatitis and sepsis. It inhibits hypoxia-induced PKG and PPAR-γ. Its effects on cardiovascular diseases have been studied in preclinical models. Its ability to modulate P2X7 and SOCE contributes to its in vivo effects. |
| Enzyme Assay |
In vitro enzyme assays for TIIAS measure its inhibition of CYP3A4 activity. The enzyme is incubated with a specific substrate and varying concentrations of the compound, and metabolite formation is quantified. Its modulation of P2X7 can be assessed using calcium flux assays in cells expressing the receptor. Its inhibition of SOCE can be measured using calcium imaging techniques.
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| Cell Assay |
In vitro cellular assays for TIIAS involve treating cells with the compound and measuring its effects on calcium signaling, CYP3A4 activity, and cell viability. Its anti-inflammatory effects are assessed by measuring cytokine production in stimulated immune cells. Its effects on cardiovascular cells are studied by measuring cell survival and function under hypoxic conditions.
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| Animal Protocol |
In vivo animal models for TIIAS include rodent models of hepatitis and sepsis to evaluate its anti-inflammatory properties. Models of cardiovascular disease, such as myocardial ischemia-reperfusion injury, are used to study its cardioprotective effects. Its pharmacokinetics and toxicity are also evaluated in animal models.
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| ADME/Pharmacokinetics |
TIIAS is a water-soluble derivative, which improves its bioavailability compared to tanshinone IIA. It is administered intravenously in research settings. It is metabolized in the liver, and its metabolites are excreted in urine and feces. Its half-life and distribution are not well-characterized in the literature.
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| Toxicity/Toxicokinetics |
TIIAS is generally well-tolerated in preclinical studies. Its safety in humans has not been fully established. As a CYP3A4 inhibitor, it may cause drug-drug interactions. Its anti-inflammatory and cardiovascular effects are being studied, but its therapeutic use is not yet approved.
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| References |
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| Additional Infomation |
TIIAS is a water-soluble derivative of tanshinone IIA and a negative allosteric modulator of the P2X7 receptor. It inhibits SOCE and CYP3A4 activity. It exhibits anti-inflammatory properties in rodent models and is used in cardiovascular disease research. It is also known as Sodium tanshinone IIA sulfonate.
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| Molecular Formula |
C19H17NAO6S
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| Molecular Weight |
396.38
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| Exact Mass |
396.064
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| CAS # |
69659-80-9
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| PubChem CID |
23669322
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| Appearance |
Pink to red solid powder
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| LogP |
4.232
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
27
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| Complexity |
742
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
AZEZEAABTDXEHR-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C19H18O6S.Na/c1-9-13-15(20)16(21)14-10-5-4-8-19(2,3)12(10)7-6-11(14)17(13)25-18(9)26(22,23)24;/h6-7H,4-5,8H2,1-3H3,(H,22,23,24);/q;+1/p-1
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| Chemical Name |
sodium;1,6,6-trimethyl-10,11-dioxo-8,9-dihydro-7H-naphtho[1,2-g][1]benzofuran-2-sulfonate
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| Synonyms |
Danshen-201; Tanshinone II A sulfonate; TIIAS
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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 Note: (1). This product is not stable in solution, please use freshly prepared working solution for optimal results. (2). Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~62.5 mg/mL (~157.67 mM)
H2O : ~2 mg/mL (~5.05 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.25 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 20.8 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. Solubility in Formulation 2: 2.08 mg/mL (5.25 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5228 mL | 12.6142 mL | 25.2283 mL | |
| 5 mM | 0.5046 mL | 2.5228 mL | 5.0457 mL | |
| 10 mM | 0.2523 mL | 1.2614 mL | 2.5228 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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