Structure
Telcagepant, Inhibitor
Telcagepant
Purity
98.00%
Synonyms
Telcagepant; MK-0974; inhibitor
Purity/Purification
98.00%
Form/Format
Solid. Powder
Solubility
DMSO: 50mg/mL (88.26mM)
(<1mg/ml refers to the product slightly soluble or insoluble)
(<1mg/ml refers to the product slightly soluble or insoluble)
Formula
C26H27F5N6O3
SMILES
O=C1NC2=C(N1C3CCN(C(N[C@@H]4CC[C@@H](C5=CC=CC(F)=C5F)CN(CC(F)(F)F)C4=O)=O)CC3)C=CC=N2
CAS Number
781649-09-0
Target & IC50
human CGRP: ic50 0.77nM (ki)
rhesus CGRP: ic50 1.2nM (ki)
rhesus CGRP: ic50 1.2nM (ki)
In Vitro
The pharmacokinetics of Telcagepant (MK-0974) remains linear across 0.5-10mg/kg intravenous dose in monkeys, but the oral area under the plasma concentration-time curve (AUC) enhances (5-30mg/kg) is 15-fold over dose-proportional. Telcagepant (i.v. bolus, 1mg/kg) demonstrates that the efficacy of this antagonist is time-dependent and correlated with plasma levels[1][3].
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
-80 degree C for 2 years in solvent
Structure
Structure
Related Product Information for Telcagepant, inhibitor
Telcagepant is an orally active antagonist of calcitonin gene-related peptide (CGRP) receptor (Kis: 0.77nM and 1.2nM for human and rhesus CGRP receptors, respectively).
Product Categories/Family for Telcagepant, inhibitor
References
Salvatore CA, et al. Pharmacological characterization of MK-0974 [N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide], a potent and orally active calcitonin gene-related peptide receptor antagonist for the treatment,of migraine. J Pharmacol Exp Ther. 2008 Feb;324(2):416-2Epub 2007 Nov 26.
Salvatore CA, et al. Pharmacological characterization of MK-0974 [N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide], a potent and orally active calcitonin gene-related peptide receptor antagonist for the treatment,of migraine. J Pharmacol Exp Ther. 2008 Feb;324(2):416-21. Epub 2007 Nov 26.
Moore EL, et al. Examining the binding properties of MK-0974: a CGRP receptor antagonist for the acute treatment,of migraine. Eur J Pharmacol. 2009 Jan 14;602(2-3):250-4.
Moore EL, et al. Examining the binding properties of MK-0974: a CGRP receptor antagonist for the acute treatment,of migraine. Eur J Pharmacol. 2009 Jan 14;602(2-3):250-4.
Roller S, et al. Preclinical pharmacokinetics of MK-0974, an orally active calcitonin-gene related peptide (CGRP)-receptor antagonist, mechanism of dose dependency and species differences. Xenobiotica. 2009 Jan;39(1):33-45.
Roller S, et al. Preclinical pharmacokinetics of MK-0974, an orally active calcitonin-gene related peptide (CGRP)-receptor antagonist, mechanism of dose dependency and species differences. Xenobiotica. 2009 Jan;39(1):33-45.
Salvatore CA, et al. Pharmacological characterization of MK-0974 [N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide], a potent and orally active calcitonin gene-related peptide receptor antagonist for the treatment,of migraine. J Pharmacol Exp Ther. 2008 Feb;324(2):416-21. Epub 2007 Nov 26.
Moore EL, et al. Examining the binding properties of MK-0974: a CGRP receptor antagonist for the acute treatment,of migraine. Eur J Pharmacol. 2009 Jan 14;602(2-3):250-4.
Moore EL, et al. Examining the binding properties of MK-0974: a CGRP receptor antagonist for the acute treatment,of migraine. Eur J Pharmacol. 2009 Jan 14;602(2-3):250-4.
Roller S, et al. Preclinical pharmacokinetics of MK-0974, an orally active calcitonin-gene related peptide (CGRP)-receptor antagonist, mechanism of dose dependency and species differences. Xenobiotica. 2009 Jan;39(1):33-45.
Roller S, et al. Preclinical pharmacokinetics of MK-0974, an orally active calcitonin-gene related peptide (CGRP)-receptor antagonist, mechanism of dose dependency and species differences. Xenobiotica. 2009 Jan;39(1):33-45.
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Product Notes
The Telcagepant (Catalog #AAA5755198) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "Telcagepant, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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