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

Temanogrel (Synonyms: APD791)

Cat. No.: HY-10560 Purity: 98.14%
Handling Instructions

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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 432 In-stock
Estimated Time of Arrival: December 31
1 mg USD 150 In-stock
Estimated Time of Arrival: December 31
5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 750 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target

Ki: 4.9 nM (5-HT2A receptor)

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].

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].

Clinical Trial
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)

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
10 mM 0.2291 mL 1.1455 mL 2.2910 mL
*Please refer to the solubility information to select the appropriate solvent.
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
Molecular Weight

436.50

Formula

C₂₄H₂₈N₄O₄

CAS No.

887936-68-7

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

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Temanogrel
Cat. No.:
HY-10560
Quantity:

Temanogrel

Cat. No.: HY-10560