MK-3207

Research use only, not for human use.

A highly potent, selective CGRP receptor antagonist with Ki of 21 pM in in vitro binding assay and IC50 of 0.12 nM in cell-based functional assay.

A highly potent, selective CGRP receptor antagonist with Ki of 21 pM in in vitro binding assay and IC50 of 0.12 nM in cell-based functional assay; displays >50000-fold selectivity in a panel of 160 enzymes, receptors, channels, and 65-fold more potent than telcagepant; orally bioavailable.

MK-3207 (0.3, 0.6, 1.1, 2.3, 4.5, 9.0 nM; 30 min) potently blocks human α-CGRP-stimulated cAMP responses in human CGRP receptor-expressing HEK293 cells. Cell Viability Assay Cell Line:HEK293 cells (stably expressing human CLR/RAMP1)Concentration:0.3, 0.6, 1.1, 2.3, 4.5, 9.0 nM Incubation Time:30 min (pre-treat)Result:Blocked human α-CGRP-stimulated cAMP responses with an IC50 value of 0.12 nM.

MK-3207 (0.3, 0.6, 2.1, 9.1, 21.2, 60.6 μg/kg; i.v.; single) inhibits CIDV in rhesus monkeys with EC50 and Emax values of approximately 0.8 nM and 81%.MK-3207 (10 mg/kg; p.o.; single) shows the CSF/plasma ratio is 2 to 3%. Animal Model:Adult rhesus monkeys (4.8-12.7 kg; capsaicin-induced).Dosage:0.3, 0.6, 2.1, 9.1, 21.2, 60.6 μg/kg Administration:Intravenous injection; single.Result:Resulted in an exposure-dependent decrease in capsaicin-induced dermal vasodilation in the rhesus monkey forearm.Animal Model:Adult rhesus monkeys (4.8-12.7 kg).Dosage:10 mg/kg Administration:Oral administration; single.Result:Exhibited the CSF/plasma ratio was 2 to 3%, however the CSF/plasma ratio was approximately 30% of the unbound fraction (9.4%) in plasma.

MK3207 | MK 3207

GPCR/G Protein

CGRP Receptor

CGRP Receptor

Neurological Disease

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957118-49-9

557.5905

C31H29F2N5O3

>98% (HPLC)

10 mM in DMSO

C1CCC2(C1)C(=O)N(C(CN2)C3=CC(=CC(=C3)F)F)CC(=O)NC4=CC5=C(CC6(C5)C7=C(NC6=O)N=CC=C7)C=C4

6,9-Diazaspiro[4.5]decane-9-acetamide, 8-(3,5-difluorophenyl)-10-oxo-N-[(2R)-1,1',2',3-tetrahydro-2'-oxospiro[2H-indene-2,3'-[3H]pyrrolo[2,3-b]pyridin]-5-yl]-, (8R)-

(-20℃)

With Ice Pack

≥ 2 years