MK-3207 HCl

This product is for research use only, not for human use. We do not sell to patients.

MK-3207 HCl
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Size Price Stock
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500mg$2550Check With Us
1g$3825Check With Us

Cat #: V1495 CAS #: 957116-20-0 Purity ≥ 98%

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.

References: 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.

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Molecular Weight (MW)594.05
Molecular FormulaC31H29F2N5O3.HCl
CAS No.957116-20-0
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 119 mg/mL (200.3 mM)r
Water: 5 mg/mL (8.4 mM)r
Ethanol: 119 mg/mL (200.3 mM)
Solubility In Vivo1% DMSO+30% polyethylene glycol+1% Tween 80: 30mg/mL
SynonymsMK-3207; MK3207; MK 3207
ProtocolIn VitroMK-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.
In VivoMK-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%
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM1.6834 mL8.4168 mL16.8336 mL33.6672 mL
5mM0.3367 mL1.6834 mL3.3667 mL6.7334 mL
10mM0.1683 mL0.8417 mL1.6834 mL3.3667 mL
20mM0.0842 mL0.4208 mL0.8417 mL1.6834 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
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Volume
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Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid 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 master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (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.
  • (2) Be sure to add the solvent(s) in order.