Telcagepant

SKU: orb2946025

Description

Telcagepant (MK-0974) is a small molecule CGRP receptor antagonist used in migraine research. It has been studied in vitro for receptor binding and in vivo for efficacy in preclinical migraine models, demonstrating its role in blocking CGRP-mediated neurotransmission for potential pain relief.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	781649-09-0
MW	566.52
Purity	98.98% (May vary between batches)
Formula	C₂₆H₂₇F₅N₆O₃
SMILES	O=C1N(C=2C(N1)=NC=CC2)C3CCN(C(N[C@H]4C(=O)N(CC(F)(F)F)C[C@@H](CC4)C5=C(F)C(F)=CC=C5)=O)CC3
Target	CGRP Receptor
Solubility	10% DMSO+40% PEG300+5% Tween 80+45% Saline:2.5 mg/mL (4.41 mM);DMSO:40 mg/mL (70.61 mM)

Bioactivity

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Target IC50	CGRP-induced cAMP accumulation (human CGRP receptor-expressing HEK293 cells, 50% human serum):10.9  nM\|CGRP (rhesus):1.2 nM (ki)\|CGRP-induced cAMP accumulation (human CGRP receptor-expressing HEK293 cells):2.2  nM\|Capsaicin-induced vasodilation via CGRP receptor (rhesus monkey):994  nM (EC₉₀)\|Capsaicin-induced vasodilation via CGRP receptor (rhesus monkey):127  nM (EC₅₀)\|Capsaicin-induced vasodilation via CGRP receptor (rhesus monkey):0.77 nM (ki)
In Vivo	The in vivo activity of Telcagepant was assessed in a rhesus monkey dermal vasodilation model. Monkeys received intravenous Telcagepant (0.03–3.7 mg/kg bolus followed by 0.13–20 μg/kg/min infusion), and capsaicin (2 mg) was applied topically to induce dermal blood flow via endogenous CGRP release. Laser Doppler imaging showed that Telcagepant inhibited capsaicin-induced vasodilation in a plasma concentration-dependent manner, with calculated EC₅₀ and EC₉₀ values of 127 nM and 994 nM, respectively, confirming in vivo CGRP receptor blockade .
In Vitro	The in vitro activity of Telcagepant was evaluated in HEK293 cells stably expressing the human CGRP receptor (CLR/RAMP1). Cells were pretreated with Telcagepant for 30 minutes, followed by stimulation with α-CGRP (0.3 nM) for 5 minutes to assess cAMP levels. Telcagepant inhibited CGRP-induced cAMP accumulation in a concentration-dependent manner with an IC₅₀ of 2.2 nM, increasing to 10.9 nM in the presence of 50% human serum. Radioligand binding assays confirmed high affinity for human CGRP receptors (Ki = 0.77 nM) and much lower affinity for dog and rat receptors (Ki > 1200 nM), indicating strong species selectivity .

Storage & Handling

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Storage	-20°C
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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MK0974, MK-0974, MK 0974, human CGRP, rhesus CGRP, Telcagepant

Quality Guarantee

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Compound Identifiers

PubChem CID

11319053 ↗

Key Properties

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No computed properties available.

Protocol Information

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Purity:	>98% (HPLC)
CAS Number:	781649-09-0
MW:	566.523
Formula:	C₂₆H₂₇F₅N₆O₃

Telcagepant

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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