MK-3207 HCl

Alias: MK-3207 Hydrochloride; MK-3207; MK3207; MK 3207
Cat No.:V1495 Purity: ≥98%
MK-3207 HCl (MK-3207; MK3207), the hydrochloride salt of MK3207, is a novel, potent and orally bioactive CGRP (Calcitonin gene related peptide) receptor antagonist with important biological activity.
MK-3207 HCl Chemical Structure CAS No.: 957116-20-0
Product category: CGRP Receptor
This product is for research use only, not for human use. We do not sell to patients.
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Other Forms of MK-3207 HCl:

  • MK-3207
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

MK-3207 HCl (MK-3207; MK3207), the hydrochloride salt of MK3207, is a novel, potent and orally bioactive CGRP (Calcitonin gene related peptide) receptor antagonist with important biological activity. It exhibits CGRP at IC50 and Ki of 0.12 nM and 0.022 nM, respectively.

Biological Activity I Assay Protocols (From Reference)
Targets
CGRP receptor ( IC50 = 0.12 nM )
ln Vitro

In vitro activity: MK-3207 exhibits a rhesus monkey receptor affinity (Ki) of 0.024±0.001 nM; n=14) that is comparable to that of humans, but its affinity for the canine and rat receptors is >400-fold lower, at 10 nM and 10±1.2 nM, respectively. With Ki values of 16,500 nM and 156±17 nM, respectively, MK-3207 exhibits high selectivity against the human AM1 (CLR/RAMP2) and AM2 (CLR/RAMP3) receptors. At 1.9±0.58 μM, MK-3207 exhibits a high level of selectivity against human CTR. With a Ki value of 128±25 nM, MK-3207 demonstrates good selectivity against the AMY3 (CTR/RAMP3) receptor as well. However, its Ki value of 0.75±0.13 nM indicates less selectivity against the AMY1 (CTR/RAMP1) receptor. MK-3207 potently inhibits human α-CGRP-stimulated cAMP responses in human CGRP receptor-expressing HEK293 cells, with an IC50 value of 0.12±0.02 nM. MK-3207 exhibits a significantly lower potency for the rat CGRP receptor, with a pIC50=7.31±0.09.

ln Vivo
MK-3207 profoundly activates central receptors because it is a CNS-penetrant. Following a 10 mg/kg oral dose of MK-3207, the ratio of CSF to plasma is 2 to 3%[1].
Enzyme Assay
MK-3207 and 40 pM rat amylin are combined in amylin binding assays, and then 25 μg of CTR/RAMP1 or 25 μg of CTR/RAMP3 membranes are added. The mixture is then incubated for three hours at room temperature in binding buffer (10 mM HEPES, 5 mM MgCl2, and 0.2% bovine serum albumin) in a volume of one milliliter. As the radioligand in calcitonin binding assays, 25 μg of CTR membranes are used with 30 pM 125I-human calcitonin. Filtration through GF/B 96-well filter plates blocked with 0.5% polyethylenimine ends the incubation process. Prism is utilized for data analysis, and the equation Ki=IC50/1 + ([ligand]/KD is used to calculate the Ki value. Saturation binding experiments are used to calculate the KD value for each receptor.
Animal Protocol
A specially made flexible silicone catheter is fed into a surgically implanted port body in the midscapular region after being fully suspended in the cisterna magna and securely anchored on both sides of the atlanto-occipital membrane. The catheter is tunneled subcutaneously to this location. Via the skin and membrane covering the port, a needle is aseptically inserted to access the CSF; peripheral venipuncture is used to obtain blood samples. 0.5, 1, 2, 4, 8, and 24 hour CSF and plasma samples are taken and subjected to compound level analysis following oral administration of MK-3207 at 10 mg/kg (0.5% methylcellulose, with an adjusted pH of approximately 3) to rhesus monkeys with port-implanted cisterna magna catheters.
References

[1]. Pharmacological properties of MK-3207, a potent and orally active calcitonin gene-related peptide receptor antagonist. J Pharmacol Exp Ther. 2010 Apr;333(1):152-60.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C31H29F2N5O3.HCL
Molecular Weight
594.05
Exact Mass
593.2
CAS #
957116-20-0
Appearance
Powder
SMILES
C1CCC2(C1)C(=O)N([C@@H](CN2)C3=CC(=CC(=C3)F)F)CC(=O)NC4=CC5=C(C[C@@]6(C5)C7=C(NC6=O)N=CC=C7)C=C4.Cl
InChi Key
VWKNXYACOMQRBX-KZCKSIIFSA-N
InChi Code
InChI=1S/C31H29F2N5O3.ClH/c32-21-10-19(11-22(33)13-21)25-16-35-31(7-1-2-8-31)29(41)38(25)17-26(39)36-23-6-5-18-14-30(15-20(18)12-23)24-4-3-9-34-27(24)37-28(30)40;/h3-6,9-13,25,35H,1-2,7-8,14-17H2,(H,36,39)(H,34,37,40);1H/t25-,30+;/m0./s1
Chemical Name
2-[(8R)-8-(3,5-difluorophenyl)-10-oxo-6,9-diazaspiro[4.5]decan-9-yl]-N-[(2R)-2'-oxospiro[1,3-dihydroindene-2,3'-1H-pyrrolo[2,3-b]pyridine]-5-yl]acetamide;hydrochloride
Synonyms
MK-3207 Hydrochloride; MK-3207; MK3207; MK 3207
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~119 mg/mL (~200.3 mM)
Water: ~5 mg/mL (~8.4 mM)
Ethanol: ~119 mg/mL (~200.3 mM)
Solubility (In Vivo)
1%DMSO+30% polyethylene glycol+1%Tween 80: 30mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.6834 mL 8.4168 mL 16.8336 mL
5 mM 0.3367 mL 1.6834 mL 3.3667 mL
10 mM 0.1683 mL 0.8417 mL 1.6834 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
  • MK-3207 HCl

    Selected CGRP Receptor Antagonists.2010 Jan 12;1(1):24-9.

  • MK-3207 HCl

    Model predictedvs. observed blood flow by MK-3207 plasma concentration at two capsaicin doses (300 and 1000 μg).2015 May;79(5):831-7.

  • MK-3207 HCl

    Simulated mean response of inhibition (%) of capsaicin-induced dermal vasodilatation (CIDV) byMK-3207vs.plasma concentrations ofMK-3207.2015 May;79(5):831-7.

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