1. GPCR/G Protein
    Neuronal Signaling
  2. CGRP Receptor
  3. MK-3207

MK-3207 

Cat. No.: HY-10301 Purity: 98.76%
Handling Instructions

MK-3207 is a potent and orally bioavailable CGRP receptor antagonist (IC50= 0.12 nM; Ki value= 0.024 nM); highly selective versus human AM1, AM2, CTR, and AMY3.

For research use only. We do not sell to patients.

MK-3207 Chemical Structure

MK-3207 Chemical Structure

CAS No. : 957118-49-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 236 In-stock
Estimated Time of Arrival: December 31
5 mg USD 192 In-stock
Estimated Time of Arrival: December 31
10 mg USD 330 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

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Description

MK-3207 is a potent and orally bioavailable CGRP receptor antagonist (IC50= 0.12 nM; Ki value= 0.024 nM); highly selective versus human AM1, AM2, CTR, and AMY3. IC50 Value: 0.024 nM (Ki, Human CGRP) [1] In common with other CGRP receptor antagonists, MK-3207 displays lower affinity for human CGRP receptors from other species, including canine and rodent. in vitro: MK-3207 is a potent antagonist of the human and rhesus monkey CGRP receptors (K(i) = 0.024 nM). in vivo: MK-3207 produced a concentration-dependent inhibition of dermal vasodilation, with plasma concentrations of 0.8 and 7 nM required to block 50 and 90% of the blood flow increase, respectively. The tritiated analog [3H]MK-3207 was used to study the binding characteristics on the human CGRP receptor. [3H]MK-3207 displayed reversible and saturable binding (K(D) = 0.06 nM), and the off-rate was determined to be 0.012 min(-1), with a t(1/2) value of 59 min [1]. After the first interim analysis, the two lowest MK-3207 doses (2.5, 5 mg) were identified as showing insufficient efficacy. Per the pre-specified adaptive design decision rule, only the 2.5-mg group was discontinued and the five highest doses (5, 10, 20, 50, 100 mg) were continued into the second stage [2]. Clinical trial: MK-3207 for the treatment of acute migraines. Phase 2b

Clinical Trial
Molecular Weight

557.59

Formula

C₃₁H₂₉F₂N₅O₃

CAS No.

957118-49-9

SMILES

O=C1C2(NC[[email protected]@H](C3=CC(F)=CC(F)=C3)N1CC(NC4=CC5=C(C[[email protected]@]6(C(NC7=C6C=CC=N7)=O)C5)C=C4)=O)CCCC2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (179.34 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7934 mL 8.9672 mL 17.9343 mL
5 mM 0.3587 mL 1.7934 mL 3.5869 mL
10 mM 0.1793 mL 0.8967 mL 1.7934 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.48 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.48 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.48 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

MK-3207MK3207MK 3207CGRP ReceptorCalcitonin gene-related peptide receptorInhibitorinhibitorinhibit

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MK-3207
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