| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
Purity: ≥98%
| Targets |
Seratrodast targets the thromboxane A2 (TXA2) receptor, also known as the T-prostanoid receptor (TP). As a selective antagonist, it blocks the binding of thromboxane A2 to its receptor, thereby inhibiting its signaling pathway. This leads to vasodilation and antiplatelet activity. It also inhibits ferroptosis by suppressing lipid peroxidation.
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| ln Vitro |
In vitro, Seratrodast is a potent and selective antagonist of the TXA2 receptor. It has an IC50 of 7.4 nM for guinea pig platelets. It reduces lipid ROS production, modulates the systemic xc-/GSH/GPX4 axis, and inhibits JNK phosphorylation and p53 expression. It also inhibits peroxide-induced vasoconstriction in human placenta.
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| ln Vivo |
In vivo, Seratrodast is used as an antiasthmatic agent. By selectively antagonizing the thromboxane A2 receptor, it inhibits TXA2-mediated bronchoconstriction. Its antioxidant and ferroptosis inhibitory effects may also contribute to its therapeutic actions.
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| Enzyme Assay |
In vitro receptor binding assays for Seratrodast involve measuring its affinity for the thromboxane A2 receptor (TP). Radioligand binding studies using membranes from cells expressing the receptor and a labeled TP ligand are performed to determine the compound's binding affinity (Ki). Functional activity is assessed by measuring the compound's ability to inhibit TP receptor-mediated signaling, such as calcium mobilization or platelet aggregation.
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| Cell Assay |
In vitro cellular assays for Seratrodast are performed using cell lines to study its effects on ferroptosis and inflammation. Cells are treated with the compound and then exposed to ferroptosis inducers. Lipid ROS production, glutathione levels, and markers of ferroptosis (e.g., GPX4 expression) are measured.
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| Animal Protocol |
In vivo animal experiments for Seratrodast are conducted in models of asthma or airway inflammation. The compound is administered orally, and its effects on airway resistance, inflammatory cell infiltration, and cytokine levels are measured. Its vasodilatory and antiplatelet effects can be assessed in appropriate animal models.
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| ADME/Pharmacokinetics |
Metabolism / Metabolites
The known human metabolites of celastrol include (2S,3S,4S,5R)-3,4,5-trihydroxy-6-[7-phenyl-7-(2,4,5-trimethyl-3,6-dioxocyclohex-1,4-dien-1-yl)heptanoyl]oxoxacyclohexane-2-carboxylic acid. Seratrodast is an orally active compound. Its PK profile in humans has been characterized, supporting its clinical use as an antiasthmatic agent. It is available in oral dosage forms. |
| Toxicity/Toxicokinetics |
Seratrodast has a well-established safety profile. As an approved drug, its toxicological profile has been evaluated in clinical trials and post-marketing surveillance. Common adverse effects may include gastrointestinal disturbances.
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| References |
[3]. Lou B. Crystal structure of 7-phenyl-7-(2,4,5-trimethyl-3,6-dioxo-cyclo-hexa-1,4-dien-1-yl)hepta-noate 1,3-dihy-droxy-2-(hy-droxy-meth-yl)propan-2-aminium monohydrate: a new solid form of seratrodast. Acta Crystallogr Sect E Struct Rep Online. 2014 Sep 20;70(Pt 10):228-30. doi: 10.1107/S1600536814020625. PubMed PMID: 25484659; PubMed Central PMCID: PMC4257156. |
| Additional Infomation |
Seratrodast is an organic molecular entity. Seratrodast (INN) is a thromboxane receptor antagonist primarily used to treat asthma.
Seratrodast is also known as AA 2414 and STD. It is a thromboxane A2 receptor antagonist and ferroptosis inhibitor. It was first approved in 1995 for the treatment of airway obstruction. It is marketed in some countries as an antiasthmatic agent. |
| Molecular Formula |
C22H26O4M
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|---|---|
| Molecular Weight |
354.4394
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| Exact Mass |
354.183
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| CAS # |
112665-43-7
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| PubChem CID |
2449
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| Appearance |
Yellow to orange solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
522.3±49.0 °C at 760 mmHg
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| Melting Point |
118-120°C
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| Flash Point |
283.8±26.3 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.555
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| LogP |
5.25
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
26
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| Complexity |
633
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ZBVKEHDGYSLCCC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H26O4/c1-14-15(2)22(26)20(16(3)21(14)25)18(17-10-6-4-7-11-17)12-8-5-9-13-19(23)24/h4,6-7,10-11,18H,5,8-9,12-13H2,1-3H3,(H,23,24)
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| Chemical Name |
(+-)-7-(3,5,6-Trimethyl-1,4-benzoquinon-2-yl)-7-phenylheptanoic acid
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| Synonyms |
AA2414 AA-2414 Abbott 73001 Abbott-73001 ABT 001 ABT-001 CCRIS 8939.
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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 |
| 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 : ≥ 100 mg/mL (~282.14 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.05 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.05 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 25.0 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.05 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8214 mL | 14.1068 mL | 28.2135 mL | |
| 5 mM | 0.5643 mL | 2.8214 mL | 5.6427 mL | |
| 10 mM | 0.2821 mL | 1.4107 mL | 2.8214 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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