2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. Temanogrel

Temanogrel is a highly selective 5-HT2A receptor antagonist with a Ki of 4.9 nM.

For research use only. We do not sell to patients.

Temanogrel Chemical Structure

Temanogrel Chemical Structure

CAS No. : 887936-68-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 275 In-stock
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10 mM * 1 mL in DMSO USD 275 In-stock
Solid
1 mg USD 110 In-stock
5 mg USD 250 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Temanogrel:

Temanogrel Related Antibodies

Top Publications Citing Use of Products

View All 5-HT Receptor Isoform Specific Products:

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5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Temanogrel is a highly selective 5-HT2A receptor antagonist with a Ki of 4.9 nM.

IC50 & Target

5-HT2A Receptor

4.9 nM (Ki)

In Vitro

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.

Temanogrel Related Antibodies
In Vivo

There are no differences in heart rate or mean arterial pressure between saline-treated and Temanogrel-treated groups at any time during the experiment (that is, for mean arterial pressure, P=0.508 between groups, and P=0.540 for group-time interaction). In dogs assigned to receive Temanogrel, plasma Temanogrel levels show a rapid and sustained increase, averaging 25.5±4.1, 28.7±4.6 and 31.2±4.5 ng/mL, respectively, at 10 min, 1.25 h and 2.25 h after the start of treatment[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

436.50

Formula

C24H28N4O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CN1C(C2=C(OCCN3CCOCC3)C=CC(NC(C4=CC=CC(OC)=C4)=O)=C2)=CC=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (286.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2910 mL 11.4548 mL 22.9095 mL
5 mM 0.4582 mL 2.2910 mL 4.5819 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% 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 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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References
Cell Assay
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[3]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

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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Temanogrel Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Temanogrel887936-68-7APD791APD 791APD-7915-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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