957116-20-0

Name	MK-3207 (Hydrochloride)
Synonyms	CS-549 MK-3207 MK3207 HCl MK-3207 HCl salt MK3207 HYDROCHLORIDE MK 3207 hydrochloride MK 3207 HYDROCHLORIDE MK-3207 (Hydrochloride) 2-((R)-8-(3,5-difluorophenyl)-10-oxo-6,9-diazaspiro[4.5]decan-9-yl)-N-((R)-2'-oxo-1,1',2',3-tetrahydrospiro[indene-2,3'-pyrrolo[2,3-b]pyridin]-5-yl)acetamide hydrochloride 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]-, hydrochloride (8R)-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]-6,9-diazaspiro[4.5]decane-9-acetamide hydrochloride
CAS	957116-20-0
EINECS	200-258-5

Molecular Formula	C31H30ClF2N5O3
Molar Mass	594.06
Solubility	10 mM in DMSO
Storage Condition	-20℃
In vitro study	Compared with CGRP receptor in other species (including dogs and rodents) (Ki of 10 nM),MK 3207 acts on self and recombinant human CGRP receptor and rhesus monkey CGRP receptor, significantly higher affinity, Ki 24 pM, 24 pM and 22 pM, although the AMY1(CTR/RAMP1) receptor has affinity, Ki 0.75 nM, but related to human AM1(CLR/RAMP2) receptor, AM2 (CLR/RAMP3) receptor, AMY3 (CTR/RAMP3) receptor, Compared to CTR (Ki 16.5 μm, 0.156 μm, 0.128 μm, and 1.9 μm, respectively),MK 3207 significantly selective for the human CGRP receptor. MK 3207 acts on HEK293 cells stably expressing human CLR/RAMP1, effectively inhibiting human alpha-CGRP-induced cAMP production with an IC50 of 0.12 nM and in the presence of 50% human serum, similar potency was maintained with an IC50 of 0.17 nM, indicating that MK 3207 activity was not affected by plasma binding proteins in vivo. In an in vitro human plasma transfer functional assay, MK 3207 was 65-fold more effective than TELC agepant with an IC50 of 10.9 nM.
In vivo study	MK 3207 inhibited capsaicin-induced cutaneous vasodilation in a concentration-dependent manner and inhibited blood flow with an EC50 of 0.8 nM and EC90 of 7 nM. In the cynomolgus CIDV experiment, MK 3207 was more than 100 times more effective than TELC agepant with an EC90 of 994 nM.

Last Update：2024-01-02 23:10:35

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Product Name: MK-3207 (Hydrochloride) Visit Supplier Webpage Request for quotation
CAS: 957116-20-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409

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957116-20-0

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