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MK-3207
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Catalog No. T21558Cas No. 957118-49-9
Alias MK3207
MK-3207 is a highly potent and orally bioavailable small molecule antagonist of the calcitonin gene-related peptide (CGRP) receptor, demonstrating an in vitro IC50 of 0.12 nM and a Ki of 0.024 nM for the human receptor with exceptional selectivity over the related human AM1, AM2, CTR, and AMY3 receptors, though it exhibits lower affinity for CGRP receptors from other species such as canine and rodent; in vitro studies confirm its potent antagonism of human and rhesus monkey CGRP receptors (K(i) = 0.024 nM), and in vivo models show it produces a concentration-dependent inhibition of dermal vasodilation, requiring plasma concentrations of 0.8 nM and 7 nM to block 50% and 90% of the blood flow increase, respectively.
MK-3207
Copy Product Info😃Good
Catalog No. T21558Alias MK3207Cas No. 957118-49-9
MK-3207 is a highly potent and orally bioavailable small molecule antagonist of the calcitonin gene-related peptide (CGRP) receptor, demonstrating an in vitro IC50 of 0.12 nM and a Ki of 0.024 nM for the human receptor with exceptional selectivity over the related human AM1, AM2, CTR, and AMY3 receptors, though it exhibits lower affinity for CGRP receptors from other species such as canine and rodent; in vitro studies confirm its potent antagonism of human and rhesus monkey CGRP receptors (K(i) = 0.024 nM), and in vivo models show it produces a concentration-dependent inhibition of dermal vasodilation, requiring plasma concentrations of 0.8 nM and 7 nM to block 50% and 90% of the blood flow increase, respectively.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $271 | 3-6 months | 3-6 months | |
| 10 mg | $468 | 3-6 months | 3-6 months | |
| 25 mg | Inquiry | 3-6 months | 3-6 months | |
| 50 mg | Inquiry | 3-6 months | 3-6 months |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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| Description | MK-3207 is a highly potent and orally bioavailable small molecule antagonist of the calcitonin gene-related peptide (CGRP) receptor, demonstrating an in vitro IC50 of 0.12 nM and a Ki of 0.024 nM for the human receptor with exceptional selectivity over the related human AM1, AM2, CTR, and AMY3 receptors, though it exhibits lower affinity for CGRP receptors from other species such as canine and rodent; in vitro studies confirm its potent antagonism of human and rhesus monkey CGRP receptors (K(i) = 0.024 nM), and in vivo models show it produces a concentration-dependent inhibition of dermal vasodilation, requiring plasma concentrations of 0.8 nM and 7 nM to block 50% and 90% of the blood flow increase, respectively. |
| In vitro | MK-3207 (0.3, 0.6, 1.1, 2.3, 4.5, 9.0 nM, 30 min) potently blocks human α-CGRP-stimulated cAMP responses in HEK293 cells expressing the human CGRP receptor. [1] |
| Synonyms | MK3207 |
| Molecular Weight | 557.59 |
| Formula | C31H29F2N5O3 |
| Cas No. | 957118-49-9 |
| Smiles | O=C1[C@@]2(C=3C(N1)=NC=CC3)CC=4C(C2)=CC=C(NC(CN5[C@@H](CNC6(C5=O)CCCC6)C7=CC(F)=CC(F)=C7)=O)C4 |
| Relative Density. | no data available |
| Storage | store at low temperature | store at 4°C | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO: ≥ 120 mg/mL, Sonication is recommended. |
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.59 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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