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
- Molecular Weight:
- 566.52
- MDL Number:
- MFCD22741412
- MOL File:
- 781649-09-0.mol
- MSDS File:
- SDS
| Density | 1.54 |
|---|---|
| storage temp. | Store at -20°C |
| solubility | Soluble in DMSO |
| form | Powder |
| pka | 12.03±0.20(Predicted) |
| FDA UNII | D42O649ALL |
MK 0974, Telcagepant price More Price(21)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 23960 | MK-0974 ≥98% | 781649-09-0 | 1mg | $68 | 2024-03-01 | Buy |
| Cayman Chemical | 23960 | MK-0974 ≥98% | 781649-09-0 | 5mg | $302 | 2024-03-01 | Buy |
| Cayman Chemical | 23960 | MK-0974 ≥98% | 781649-09-0 | 10mg | $535 | 2024-03-01 | Buy |
| American Custom Chemicals Corporation | API0006461 | TELCAGEPANT 95.00% | 781649-09-0 | 10MG | $780.15 | 2021-12-16 | Buy |
| ChemScene | CS-0291 | Telcagepant 99.55% | 781649-09-0 | 10mg | $336 | 2021-12-16 | Buy |
MK 0974, Telcagepant Chemical Properties,Uses,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
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Capot Chemical Co.,Ltd. | 571-85586718 +8613336195806 | sales@capotchem.com | China | 29797 | 60 |
| Hubei xin bonus chemical co. LTD | 86-13657291602 | linda@hubeijusheng.com | CHINA | 22968 | 58 |
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | sales@conier.com | China | 47465 | 58 |
| career henan chemical co | +86-0371-86658258 15093356674; | factory@coreychem.com | China | 29826 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| Shanxi Xuanran Import and Export Trade Co., Ltd. | +8617735180244 | mike_yan@xuanranglobal.com | CHINA | 4022 | 58 |
| Shaanxi Dideu Medichem Co. Ltd | +86-029-89586680 +86-18192503167 | 1026@dideu.com | China | 9409 | 58 |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | 1026@dideu.com | China | 29322 | 58 |
| Dayang Chem (Hangzhou) Co.,Ltd. | 571-88938639 +8617705817739 | info@dycnchem.com | CHINA | 52867 | 58 |
| Shanghai Acmec Biochemical Technology Co., Ltd. | +undefined18621343501 | product@acmec-e.com | China | 33349 | 58 |
View Lastest Price from MK 0974, Telcagepant manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2024-04-17 | MK 0974, Telcagepant
781649-09-0
|
US $1.10 / g | 1g | 99.0% min | 100 tons min | Shaanxi Dideu Medichem Co. Ltd | |
 |
2021-10-12 | MK 0974, Telcagepant
781649-09-0
|
US $1.10 / g | 1g | 99.00% | 100 Tons Min | Dideu Industries Group Limited | |
 |
2020-01-15 | MK 0974, Telcagepant
781649-09-0
|
US $1.00 / g | 1g | 99% | 200kg | Career Henan Chemical Co |
-
- MK 0974, Telcagepant
781649-09-0
- US $1.10 / g
- 99.0% min
- Shaanxi Dideu Medichem Co. Ltd
-
- MK 0974, Telcagepant
781649-09-0
- US $1.10 / g
- 99.00%
- Dideu Industries Group Limited
-
- MK 0974, Telcagepant
781649-09-0
- US $1.00 / g
- 99%
- Career Henan Chemical Co