MK 0974, Telcagepant
- Product Name
- MK 0974, Telcagepant
- CAS No.
- 781649-09-0
- Chemical Name
- MK 0974, Telcagepant
- Synonyms
- Mk0974;MK0947;CS-454;Mk-0974;Mk 0974;Telcagepant;MK 0974, Telcagepant;Telcagepant (MK-0974);TELCAGEPANT;MK0974;MK 0974;MK 0974, Telcagepant ISO 9001：2015 REACH
- CBNumber
- CB81872361
- Molecular Formula
- C26H27F5N6O3
- Formula Weight
- 566.52
- MOL File
- 781649-09-0.mol
MK 0974, Telcagepant Property
- Density
- 1.54
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- form
- Powder
- pka
- 12.03±0.20(Predicted)
- color
- Light yellow to yellow
N-Bromosuccinimide Price
- Product number
- 23960
- Product name
- MK-0974
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $68
- Updated
- 2024/03/01
- Product number
- 23960
- Product name
- MK-0974
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $302
- Updated
- 2024/03/01
- Product number
- 23960
- Product name
- MK-0974
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $535
- Updated
- 2024/03/01
- Product number
- FD74910
- Product name
- MK 0974
- Packaging
- 1mg
- Price
- $125
- Updated
- 2021/12/16
- Product number
- CS-0291
- Product name
- Telcagepant
- Purity
- 99.55%
- Packaging
- 2mg
- Price
- $126
- Updated
- 2021/12/16
MK 0974, Telcagepant Chemical Properties,Usage,Production
Biological Activity
mk-0974 (telcagepant) is a highly potent, selective, and orally bioavailable antagonist of cgrp receptor with ic50 value of 0.77 nm [1].calcitonin gene-related peptide (cgrp) receptor is a heteromeric transmembrane receptor composed of a g protein-coupled receptor which is called calcitonin receptor-like receptor (calcrl) and a receptor activity modifying protein 1 (ramp1). cgrp receptor is functional for mediating the activity of cgrp, which is widely distributed in human peripheral and central neuron system. the cgrp/cgrp receptor signaling pathway modulate a variety of physiological functions of respiratory, immune and cardiovascular system, and play a key role in the pathophysiology of migraine headache.when binding study was carried out, it was found mk-0974 had high affinity for cgrp receptor but had no affinity for related human adrenomedullin receptors, which suggested the high specificity of mk-0974 [1]. in human hek293 cells expressing cgrp receptor, treatment of mk-0974 resulted in potent blockage of α-cgrp-stimulated camp producation, which indicated a significant inhibition of cgrp receptor activity. however, addition of 50% human serum reduced the inhibition potency of mk-0974 by 5-fold [1]. mk-0974 displayed reversible and saturable binding to both sk-n-mc membranes and rhesus cerebellum with a kd of 1.9 nm and 1.3 nm, respectively [2].in rhesus model, capsaicin-induced release of endogenous cgrp resulted in dermal vasodilation. following treatment of mk-0974 produced a dose-dependent inhibition of dermal vasodilation, with plasma concentrations of 127 and 994 nm required to block 50 and 90% of the blood flow increase, respectively. the suppression of cgrp function indicated the inhibition of cgrp receptor by mk-0974 [1]. in monkey model, mk-0974 showed moderate clearance (14-20 ml min-1 kg-1), while oral bioavailability was 6%. the pharmacokinetics of mk-0974 remained linear across 0.5-10 mg kg-1 intravenous dose in monkeys, but the oral area under the plasma concentration-time curve (auc) increase (5-30 mg kg-1) was 15-fold over dose-proportional [3].
target
CGRP receptor
References
[1] salvatore c a 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, 324(2): 416-421.
[2] moore e l et al. , examining the binding properties of mk-0974: a cgrp receptor antagonist for the acute treatment of migraine. eur j pharmacol. 2009, 602(2-3): 250-254.
[3]. 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, 39(1): 33-45.
MK 0974, Telcagepant Preparation Products And Raw materials
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View Lastest Price from MK 0974, Telcagepant manufacturers
- Product
- MK 0974, Telcagepant 781649-09-0
- Price
- US $1.10/g
- Min. Order
- 1g
- Purity
- 99.0% min
- Supply Ability
- 100 tons min
- Release date
- 2021-05-12
- Product
- MK 0974, Telcagepant 781649-09-0
- Price
- US $1.00/g
- Min. Order
- 1g
- Purity
- 99%
- Supply Ability
- 200kg
- Release date
- 2020-01-14