1. GPCR/G Protein
    Neuronal Signaling
  2. CGRP Receptor
  3. Telcagepant

Telcagepant (Synonyms: MK-0974)

Cat. No.: HY-32709 Purity: 99.07%
Handling Instructions

Telcagepant (MK-0974) is an orally active calcitonin gene-related peptide (CGRP) receptor antagonist with Kis of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors, respectively.

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

Telcagepant Chemical Structure

Telcagepant Chemical Structure

CAS No. : 781649-09-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 239 In-stock
Estimated Time of Arrival: December 31
2 mg USD 126 In-stock
Estimated Time of Arrival: December 31
5 mg USD 192 In-stock
Estimated Time of Arrival: December 31
10 mg USD 336 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1440 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2460 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

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  • References

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Description

Telcagepant (MK-0974) is an orally active calcitonin gene-related peptide (CGRP) receptor antagonist with Kis of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors, respectively.

IC50 & Target

Ki: 0.77 nM (human CGRP), 1.2 nM (rhesus CGRP)

In Vitro

Telcagepant (MK-0974) displays affinity (Ki) for the canine and rat receptors, with values of 1204 nM and 1192 nM (n=10), respectively. Telcagepant (MK-0974) potently blocks human α-CGRP-stimulated cAMP responses in human CGRP receptor expressing HEK293 cells with an IC50 of 2.2 nM[1]. Telcagepant (MK-0974) displays saturable binding to SK-N-MC membranes with a KD of 1.9 nM and Bmax of 479 fmol/mg protein. Telcagepant (MK-0974) also displays saturable binding to rhesus cerebellum homogenate with a KD of 1.3 nM and Bmax of 20 fmol/mg[2].

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

In Vivo

Telcagepant (MK-0974) (i.v. bolus, 1 mg/kg) demonstrates that the efficacy of this antagonist is time-dependent and correlated with plasma levels[1]. The pharmacokinetics of Telcagepant (MK-0974) remains linear across 0.5-10 mg/kg intravenous dose in monkeys, but the oral area under the plasma concentration-time curve (AUC) increase (5-30 mg/kg) is 15-fold over dose-proportional[3].

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

Clinical Trial
Molecular Weight

566.52

Formula

C₂₆H₂₇F₅N₆O₃

CAS No.

781649-09-0

SMILES

O=C1NC2=C(N1C3CCN(C(N[[email protected]@H]4CC[[email protected]@H](C5=CC=CC(F)=C5F)CN(CC(F)(F)F)C4=O)=O)CC3)C=CC=N2

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 : ≥ 50 mg/mL (88.26 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7652 mL 8.8258 mL 17.6516 mL
5 mM 0.3530 mL 1.7652 mL 3.5303 mL
10 mM 0.1765 mL 0.8826 mL 1.7652 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 3 mg/mL (5.30 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 3 mg/mL (5.30 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 3 mg/mL (5.30 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

HEK293 cells stably transfected with CLR/RAMP1 are plated in complete growth medium at 85,000 cells/well in 96-well poly-D-lysine-coated plates and cultured for 19 h before assay. Cells are washed with PBS and then incubated with inhibitor in the presence or absence of 50% human serum for 30 min at 37°C and 95% humidity in Cellgro Complete Serum-Free/Low-Protein medium with L-glutamine and 1 g/L bovine serum albumin. Isobutylmethylxanthine is added to the cells at a concentration of 300 μM and incubated for 30 min at 37°C. Human α-CGRP is added to the cells at a concentration of 0.3 nM and allowed to incubate at 37°C for 5 min. After α-CGRP stimulation, the cells are washed with PBS and processed for cAMP determination using the two-stage assay procedure according to the manufacturer's recommended protocol. Dose-response curves are plotted, and IC50 values are determined.

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

Animal Administration
[1]

Monkeys: Rhesus monkeys (male and female) weighing between 4 and 10 kg are used. The right saphenous vein is cannulated for intravenous drug delivery, and blood samples are obtained from the left saphenous artery. Four rubber O-rings (8 mm inner diameter) are placed on the ventral side of the forearm without directly being positioned over a visible vessel.

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

References
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Keywords:

TelcagepantMK-0974MK0974MK 0974CGRP ReceptorCalcitonin gene-related peptide receptorInhibitorinhibitorinhibit

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Telcagepant
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