S18886 (Synonyms: Terutroban,Triplion) |
Catalog No.GC17410
One-Click Copy Product Info
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S18886 is a thromboxane-prostaglandin receptor antagonist.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 165538-40-9
Sample solution is provided at 25 µL, 10mM.
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IC50: 16.4 nM for TP receptor
S18886 is a potent thromboxane A2 (TP) inhibitor.
The lipid mediator thromboxane A2 (TXA2) plays a critical role in platelet aggregation and vascular and bronchial smooth muscle constriction. The actions of TXA2 are mediated via the specific G protein coupled-receptor, TXA2 receptor (TP).
In vitro: S18886 was identified as the active isomer of the potent TP receptor antagonist S18204. S18886 was also found to be a selective antagonist of thromboxaneprostaglandin receptors in platelets and in the vessel wall [1].
In vivo: In a previous animal study, it was found that S18886 treatment could reduce the portal pressure in both animal models without producing significant changes in portal blood flow, indicating a reduction in hepatic vascular resistance. S18886 could not significantly change arterial pressure in CCl4 -cirrhotic rats but could significantly decrease it in BDL-cirrhotic rats [2].
Clinical trial: A previoius trial aiming to evaluate S18886 versus aspirin in patients with cerebral ischaemic events showed similar rates of the primary endpoint with S18886 and aspirin, without safety advantages for S18886 [3].
References:
[1] Cimetière B, Dubuffet T, Landras C, Descombes JJ, Simonet S, Verbeuren TJ, Lavielle G. New tetrahydronaphthalene derivatives as combined thromboxane receptor antagonists and thromboxane synthase inhibitors. Bioorg Med Chem Lett. 1998 Jun 2;8(11):1381-6.
[2] Rosado E, Rodríguez-Vilarrupla A, Gracia-Sancho J, Tripathi D, García-Calderó H, Bosch J, García-Pagán JC. Terutroban, a TP-receptor antagonist, reduces portal pressure in cirrhotic rats. Hepatology. 2013 Oct;58(4):1424-35.
[3] Bousser MG, Amarenco P, Chamorro A, Fisher M, Ford I, Fox KM, Hennerici MG, Mattle HP, Rothwell PM, de Cordoüe A, Fratacci MD; PERFORM Study Investigators. Terutroban versus aspirin in patients with cerebral ischaemic events (PERFORM): a randomised, double-blind, parallel-group trial. Lancet. 2011 Jun 11;377(9782):2013-22.
| Cas No. | 165538-40-9 | SDF | |
| Synonyms | Terutroban,Triplion | ||
| Chemical Name | (6R)-6-[[(4-chlorophenyl)sulfonyl]amino]-5,6,7,8-tetrahydro-2-methyl-1-naphthalenepropanoic | ||
| Canonical SMILES | CC1=C(CCC(O)=O)C2=C(C=C1)C[C@H](NS(C3=CC=C(Cl)C=C3)(=O)=O)CC2 | ||
| Formula | C20H22ClNO4S | M.Wt | 407.9 |
| Solubility | ≤2mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4516 mL | 12.2579 mL | 24.5158 mL |
| 5 mM | 490.3 μL | 2.4516 mL | 4.9032 mL |
| 10 mM | 245.2 μL | 1.2258 mL | 2.4516 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)