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MK-3207 HCl

CAS# 957116-20-0

MK-3207 HCl

Catalog No. BCC4420----Order now to get a substantial discount!

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Chemical structure

MK-3207 HCl

3D structure

Chemical Properties of MK-3207 HCl

Cas No. 957116-20-0 SDF Download SDF
PubChem ID 49867927 Appearance Powder
Formula C31H30ClF2N5O3 M.Wt 594.05
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 100 mg/mL (168.34 mM)
*"≥" means soluble, but saturation unknown.
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
SMILES 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.Cl
Standard InChIKey VWKNXYACOMQRBX-KZCKSIIFSA-N
Standard InChI 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
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of MK-3207 HCl

DescriptionMK-3207 (Hydrochloride) is a potent and orally bioavailable CGRP receptor antagonist with IC50 of 0.12 nM and Ki of 0.024 nM, and is highly selective versus human AM1, AM2, CTR, and AMY3.In Vitro:MK-3207 displays a similar affinity (Ki) for the rhesus monkey receptor (0.024±0.001 nM; n=14) as for human, but it displays >400-fold lower affinity for the canine and rat receptors, with values of 10 nM and 10±1.2 nM, respectively. MK-3207 is highly selective versus the human AM1 (CLR/RAMP2) and AM2 (CLR/RAMP3) receptors, with Ki values of 16,500 nM and 156±17 nM, respectively. MK-3207 maintains a high degree of selectivity versus human CTR, with a Ki value of 1.9±0.58 μM. MK-3207 also displays good selectivity versus the AMY3 (CTR/RAMP3) receptor, with a Ki value of 128±25 nM, but it is less selective versus the AMY1 (CTR/RAMP1) receptor, with a Ki value of 0.75±0.13 nM. MK-3207 potently blocks 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 displays significantly lower potency for the rat CGRP receptor, with a pIC50=7.31±0.09[1].In Vivo:MK-3207 is CNS-penetrant and therefore significantly engaging central receptors. After an oral dose of 10 mg/kg MK-3207, the CSF/plasma ratio is 2 to 3%[1].

References:
[1]. Salvatore CA, et al. 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.

Protocol

Kinase Assay [1]
Amylin binding assays are conducted by combining MK-3207 and 40 pM 125I-rat amylin, followed by 25 μg of CTR/RAMP1 or 25 μg of CTR/RAMP3 membranes and incubated for 3 h at room temperature in binding buffer (10 mM HEPES, 5 mM MgCl2, and 0.2% bovine serum albumin) in a total volume of 1 mL. Calcitonin binding assays are with 25 μg of CTR membranes and 30 pM 125I-human calcitonin as the radioligand. Incubations are terminated by filtration through GF/B 96-well filter plates that has been blocked with 0.5% polyethylenimine. Data are analyzed using Prism, and the Ki value is determined using the equation Ki=IC50/1 + ([ligand]/KD). The KD value for each receptor is determined by saturation binding experiments.

Animal Administration [1]
A customized flexible silicone catheter is freely suspended in the cisterna magna, anchored firmly on both sides of the atlanto-occipital membrane, and tunneled subcutaneously to the midscapular region where it is fed into a surgically implanted port body. CSF is accessed by aseptically inserting a needle through the skin and membrane covering the port into the reservoir of the port body; blood samples are collected by peripheral venipuncture. After oral administration of MK-3207 at 10 mg/kg (0.5% methylcellulose, with an adjusted pH appr 3) to cisterna magna catheter and port-implanted rhesus monkeys, CSF and plasma samples are collected at 0.5, 1, 2, 4, 8, and 24 h and analyzed for compound levels.

References:
[1]. Salvatore CA, et al. 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.

MK-3207 HCl Dilution Calculator

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MK-3207 HCl Molarity Calculator

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Preparing Stock Solutions of MK-3207 HCl

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.6834 mL 8.4168 mL 16.8336 mL 33.6672 mL 42.084 mL
5 mM 0.3367 mL 1.6834 mL 3.3667 mL 6.7334 mL 8.4168 mL
10 mM 0.1683 mL 0.8417 mL 1.6834 mL 3.3667 mL 4.2084 mL
50 mM 0.0337 mL 0.1683 mL 0.3367 mL 0.6733 mL 0.8417 mL
100 mM 0.0168 mL 0.0842 mL 0.1683 mL 0.3367 mL 0.4208 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on MK-3207 HCl

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.

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Description

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

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