Temanogrel
Based on 1 Customer Validation
Temanogrel is a highly selective 5-HT2A receptor antagonist with a Ki of 4.9 nM.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.94%
- CAS. Nr.: 887936-68-7
- Formel: C24H28N4O4
- Molecular Weight:436.50
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
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5-HT2A Receptor |
5-HT2A Receptor 4.9 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
5.2 nM
Compound: 10k
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Inverse agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of inositol phosphate accumulation
Inverse agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of inositol phosphate accumulation
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[PMID: 20455563] |
| Platelet | IC50 |
23.1 nM
Compound: 10k
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Antiplatelet activity in dog platelet rich plasma assessed as inhibition of ADP-induced aggregation treated 10 mins after ADP challenge measured after 3 mins by turbidimetry
Antiplatelet activity in dog platelet rich plasma assessed as inhibition of ADP-induced aggregation treated 10 mins after ADP challenge measured after 3 mins by turbidimetry
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[PMID: 20455563] |
| Platelet | IC50 |
8.7 nM
Compound: 10k
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Antiplatelet activity in human platelet rich plasma assessed as inhibition of ADP-induced aggregation treated 10 mins after ADP challenge measured after 3 mins by turbidimetry
Antiplatelet activity in human platelet rich plasma assessed as inhibition of ADP-induced aggregation treated 10 mins after ADP challenge measured after 3 mins by turbidimetry
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[PMID: 20455563] |
Temanogrel is a highly selective 5-HT2A receptor antagonist with a Ki of 4.9 nM. Temanogrel inhibits inositol phosphate accumulation with an IC50 of 5.2 nM. Temanogrel exhibits potent inhibition of serotonin mediated amplification of ADP-stimulated human and dog platelet aggregation (IC50=8.7 and 23.1 nM, respectively)[1]. Pretreatment of aortic rings with Temanogrel prevents the vasoconstriction caused by 20 μM 5-HT in a concentration-dependent manner. Preincubation with Temanogrel also significantly inhibits the 5-HT-stimulated DNA synthesis with an IC50 of 13±7 nM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 887936-68-7
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Appearance Solid
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Molecular Weight 436.50
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Formel C24H28N4O4
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Color White to light yellow
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SMILES
CN1C(C2=C(OCCN3CCOCC3)C=CC(NC(C4=CC=CC(OC)=C4)=O)=C2)=CC=N1
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Synonyms
APD791
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (229.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 6.25 mg/mL (14.32 mM); Clear solution
This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.73 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
To provide further insights into the effect of Temanogrel on platelet-dependent clot formation in models devoid of vascular smooth muscle, two in vitro post hoc experiments are performed. Paired aliquots of heparinized whole blood are incubated with Temanogrel (100 nM) or vehicle for 10 min at 37°C, and then placed in a thromboelastogram (TEG) pin-and-cup system with 10 µm serotonin, reptilase, and activated factor XIII (n=3 paired samples). The maximum amplitude of torsion is quantified for all samples. Aliquots of citrated blood (n=3 pairs) are incubated with Temanogrel (100 nM) or vehicle for 10 min at 37°C, and then pipetted into collagen-ADP cartridges. For each sample, the time (in seconds) required for the complete platelet-mediated thrombotic occlusion of the membrane aperture is recorded[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Adult male beagle dogs (n=3) are used and receive a single oral gavage dose of Temanogrel at 10 mg/kg. Temanogrel is formulated in sterile water at 5 mL/kg. Animals are fasted before Temanogrel delivery. Serial sampling is used to obtain plasma concentration versus time profiles. Whole blood samples are collected via jugular vein venipuncture over a 24-h period. Plasma is prepared by centrifugation from sodium heparin-treated whole blood, frozen, and stored at approximately -20°C until bioanalytical analysis[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (278 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Xiong Y, et al. Discovery and structure-activity relationship of 3-methoxy-N-(3-(1-methyl-1H-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide (APD791): a highly selective 5-hydroxytryptamine2A receptor inverse agonist for the treatment of arterial thrombosis. J Med Chem. 2010 Jun 10;53(11):4412-21. [Content Brief]
[2]. Przyklenk K, et al. Targeted inhibition of the serotonin 5HT2A receptor improves coronary patency in an in vivo model of recurrent thrombosis. J Thromb Haemost. 2010 Feb;8(2):331-40. [Content Brief]
[3]. Adams JW, et al. APD791, 3-methoxy-n-(3-(1-methyl-1h-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide, a novel 5-hydroxytryptamine 2A receptor antagonist: pharmacological profile, pharmacokinetics, platelet activity and vascular biology. J Pharmacol Exp Ther. 2009 Oct;331(1):96-103. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2910 mL | 11.4548 mL | 22.9095 mL | 57.2738 mL |
| 5 mM | 0.4582 mL | 2.2910 mL | 4.5819 mL | 11.4548 mL | |
| 10 mM | 0.2291 mL | 1.1455 mL | 2.2910 mL | 5.7274 mL | |
| 15 mM | 0.1527 mL | 0.7637 mL | 1.5273 mL | 3.8183 mL | |
| 20 mM | 0.1145 mL | 0.5727 mL | 1.1455 mL | 2.8637 mL | |
| 25 mM | 0.0916 mL | 0.4582 mL | 0.9164 mL | 2.2910 mL | |
| 30 mM | 0.0764 mL | 0.3818 mL | 0.7637 mL | 1.9091 mL | |
| 40 mM | 0.0573 mL | 0.2864 mL | 0.5727 mL | 1.4318 mL | |
| 50 mM | 0.0458 mL | 0.2291 mL | 0.4582 mL | 1.1455 mL | |
| 60 mM | 0.0382 mL | 0.1909 mL | 0.3818 mL | 0.9546 mL | |
| 80 mM | 0.0286 mL | 0.1432 mL | 0.2864 mL | 0.7159 mL | |
| 100 mM | 0.0229 mL | 0.1145 mL | 0.2291 mL | 0.5727 mL |
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