MK-3207 Hydrochloride

Name: MK-3207 Hydrochloride
Brand: MedChemExpress
SKU: HY-10302
Rating: 5.0 (3 reviews)

Cat. No.: HY-10302 Purity: 98.02%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

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

MK-3207 Hydrochloride Chemical Structure

CAS No. : 957116-20-0

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 251	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 251	In-stock	Estimated Time of Arrival: December 31
Solid
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

Other Forms of MK-3207 Hydrochloride:

MK-3207 In-stock

3 Publications Citing Use of MCE MK-3207 Hydrochloride

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: 0.12 nM (CGRP receptor)

In Vitro

MK-3207 displays a similar affinity (K_i) 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 K_i values of 16,500 nM and 156±17 nM, respectively. MK-3207 maintains a high degree of selectivity versus human CTR, with a K_i value of 1.9±0.58 μM. MK-3207 also displays good selectivity versus the AMY3 (CTR/RAMP3) receptor, with a K_i value of 128±25 nM, but it is less selective versus the AMY1 (CTR/RAMP1) receptor, with a K_i 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

594.05

Formula

C₃₁H₃₀ClF₂N₅O₃

CAS No.

957116-20-0

Appearance

Solid

Color

Off-white to pink

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (168.34 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 50 mg/mL (84.17 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 98.02%

Select Batch:

Data Sheet (285 KB) SDS (252 KB)

COA (260 KB) LCMS (130 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

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 K_i value is determined using the equation K_i=IC₅₀/1 + ([ligand]/K_D). The K_D value for each receptor is determined by saturation binding experiments. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	1.6834 mL	8.4168 mL	16.8336 mL	42.0839 mL
	5 mM	0.3367 mL	1.6834 mL	3.3667 mL	8.4168 mL
	10 mM	0.1683 mL	0.8417 mL	1.6834 mL	4.2084 mL
	15 mM	0.1122 mL	0.5611 mL	1.1222 mL	2.8056 mL
	20 mM	0.0842 mL	0.4208 mL	0.8417 mL	2.1042 mL
	25 mM	0.0673 mL	0.3367 mL	0.6733 mL	1.6834 mL
	30 mM	0.0561 mL	0.2806 mL	0.5611 mL	1.4028 mL
	40 mM	0.0421 mL	0.2104 mL	0.4208 mL	1.0521 mL
	50 mM	0.0337 mL	0.1683 mL	0.3367 mL	0.8417 mL
	60 mM	0.0281 mL	0.1403 mL	0.2806 mL	0.7014 mL
	80 mM	0.0210 mL	0.1052 mL	0.2104 mL	0.5260 mL
DMSO	100 mM	0.0168 mL	0.0842 mL	0.1683 mL	0.4208 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.