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| 10mg |
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| 50mg |
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| 100mg |
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| ln Vitro |
Temanogrel has a Ki of 4.9 nM and is an extremely selective antagonist of the 5-HT2A receptor. Temanogrel has an IC50 of 5.2 nM, which prevents the buildup of phosphoinositides. With IC50 values of 8.7 and 23.1 nM, respectively, temanogrel potently suppresses serotonin-mediated amplification of ADP-stimulated platelet aggregation in both humans and dogs [1]. Temanogrel pretreatment of aortic rings inhibited the concentration-dependent vasoconstriction elicited by 20 μM 5-HT. With an IC50 of 13±7 nM, Temanogrel preincubation likewise strongly suppresses 5-HT-stimulated DNA synthesis[3].
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| ln Vivo |
Throughout the experiment, there were no changes in heart rate or mean arterial pressure between the groups receiving saline or Temanogrel (i.e., P between groups = 0.508 for mean arterial pressure, P for interaction between groups = 0.540). Temanogrel-treated dogs exhibited a swift and steady rise in plasma Temanogrel levels, with mean increases of 25.5±4.1, 28.7±4.6, and 31.2±4.5 ng/mL at 10 minutes, 1.25 hours, and 2.25 hours following the initiation of therapy, respectively. 3].
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| References |
[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 thr
[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. [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 E |
| Additional Infomation |
Temanogrel is a member of benzamides.
See also: Temanogrel (annotation moved to). |
| Molecular Formula |
C24H28N4O4
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|---|---|
| Molecular Weight |
436.512
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| Exact Mass |
436.211
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| CAS # |
887936-68-7
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| PubChem CID |
11604525
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| Appearance |
White to off-white solid powder
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| LogP |
3.38
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
32
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| Complexity |
588
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1C=C(OC)C=CC=1)NC1C=C(C2N(C)N=CC=2)C(OCCN2CCOCC2)=CC=1
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| InChi Key |
ZEOQUKRCASTCFR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H28N4O4/c1-27-22(8-9-25-27)21-17-19(26-24(29)18-4-3-5-20(16-18)30-2)6-7-23(21)32-15-12-28-10-13-31-14-11-28/h3-9,16-17H,10-15H2,1-2H3,(H,26,29)
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| Chemical Name |
3-methoxy-N-[3-(2-methylpyrazol-3-yl)-4-(2-morpholin-4-ylethoxy)phenyl]benzamide
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| Synonyms |
APD 791; APD-791; APD791
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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 : ~125 mg/mL (~286.37 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (14.32 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 62.5 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: ≥ 6.25 mg/mL (14.32 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 62.5 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: ≥ 6.25 mg/mL (14.32 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 | 2.2909 mL | 11.4545 mL | 22.9090 mL | |
| 5 mM | 0.4582 mL | 2.2909 mL | 4.5818 mL | |
| 10 mM | 0.2291 mL | 1.1454 mL | 2.2909 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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