Queen's Award Received in 2021 ISO 9001 Certified Delivered over 1,000,000 bio-reagents to life science researchers Trusted by Life Science Communities
Cart summary

You have no items in your shopping cart.

MK-0974

SKU: orb2655637

Description

A potent, selective, orally bioavailable CGRP receptor antagonist with Ki of 0.77 nM; shows >10,000-fold selectivity in a panel of assays representing over 160 receptors, transporters, and enzymes; inhibits CGRP-stimulated cAMP production in E10 cells with IC50 of 2.2 nM; inhibits the capsaicin-induced increase in dermal blood flow in monkey models.Migraine Phase 3 Discontinued.

Images & Validation

−
MK-0974

Key Properties

−
CAS Number781649-09-0
MW566.523
Purity>98% (HPLC)
FormulaC26H27F5N6O3
SMILESO=C(N1CCC(N(C2=CC=CN=C2N3)C3=O)CC1)N[C@H]4C(N(CC(F)(F)F)C[C@H](C5=CC=CC(F)=C5F)CC4)=O
TargetCGRP Receptor
Solubility10 mM in DMSO

Bioactivity

−
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. 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.
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. 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.

Storage & Handling

−
StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

−
Telcagepant

Similar Products

−
  • Telcagepant

    Telcagepant [orb2946025]

    98.98% (May vary between batches)

    781649-09-0

    566.52

    C26H27F5N6O3

    1 mg
Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Quick Database Links

Gene Symbol
CGRP Receptor

Protocol Information

Find More Protocols

Available Sizes

Select a size below

50 mg
$ 1,540.00
100 mg
$ 2,440.00
DispatchUsually dispatched within 5-10 working days
Bulk Enquiry
Need technical support? Find your Distributor Return and Tax Policy

Email

[email protected]

UK Office

+44 (0)1223 859353

US Office

+1 (415) 906-5211

CN Office

+86 (27)-87663101

Distributors

biorbyt.com/distributor