MK-3207
Based on 5 publication(s) in Google Scholar
MK-3207 is an orally active, highly selective and species-specific CGRP receptor antagonist (for human CGRP receptor: IC50=0.12 nM; Ki=0.024 nM). MK-3207 can be used for migraine studies.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.60%
- No. CAS: 957118-49-9
- Fòrmula: C31H29F2N5O3
- Peso molecular:557.59
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Almacenamiento:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) MK-3207
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.12 nM
Compound: 3, MK-3207
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Inhibition of human CGRP receptor expressed in huamn HEK293 cells coexpressing CLR/RAMP1 assessed as inhibition of CGRP-stimulated cAMP production after 1 hr
Inhibition of human CGRP receptor expressed in huamn HEK293 cells coexpressing CLR/RAMP1 assessed as inhibition of CGRP-stimulated cAMP production after 1 hr
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[PMID: 21982500] |
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 human CGRP receptor-expressing HEK293 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293 cells (stably expressing human CLR/RAMP1)
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Concentration:0.3, 0.6, 1.1, 2.3, 4.5, 9.0 nM
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Incubation Time:30 min (pre-treat)
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Result:Blocked human α-CGRP-stimulated cAMP responses with an IC50 value of 0.12 nM.
MK-3207 (10 mg/kg; p.o.; single) shows 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.
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Animal Model:Adult rhesus monkeys (4.8-12.7 kg; capsaicin-induced)[1].
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Dosage:0.3, 0.6, 2.1, 9.1, 21.2, 60.6 µg/kg
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Administration:Intravenous injection; single.
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Result:Resulted in an exposure-dependent decrease in capsaicin-induced dermal vasodilation in the rhesus monkey forearm.
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Animal Model:Adult rhesus monkeys (4.8-12.7 kg)[1].
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Dosage:10 mg/kg
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Administration:Oral administration; single.
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Result:Exhibited the CSF/plasma ratio was 2 to 3%, however the CSF/plasma ratio was approximately 30% of the unbound fraction (9.4%) in plasma.
Chemical Information
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No. CAS 957118-49-9
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Appearance Solid
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Peso molecular 557.59
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Fòrmula C31H29F2N5O3
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Color Off-white to light yellow
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (5)
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Journal Impact Factor
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Most Recent
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Science
2025 Feb 21;387(6736):892-900. PMID: 39977508 -
Eur J Pharmacol
2018 Jun 15:829:85-92. PMID: 29653090 -
Neuropharmacology
Calcitonin gene-related peptide (CGRP) exerts membrane, cellular and synaptic actions on serotonergic dorsal raphe neurons ex vivo: Functional implications for a role in dorsal raphe-controlled functions. [Abstract]2025 Apr 4:110457. PMID: 40189018 -
Vascul Pharmacol
Binding and functional pharmacological characteristics of gepant-type antagonists in rat brain and mesenteric arteries. [Abstract]2017 Mar:90:36-43. PMID: 28192258 -
Pharmacology
The Presence of Calcitonin Gene-Related Peptide and Its Receptors in Rat, Pig and Human Brain: Species Differences in Calcitonin Gene-Related Peptide Pharmacology. [Abstract]2019;104(5-6):332-341. PMID: 31484177
Solvente y solubilidad
DMSO : ≥ 150 mg/mL (269.01 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.48 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.48 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (283 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7934 mL | 8.9672 mL | 17.9343 mL | 44.8358 mL |
| 5 mM | 0.3587 mL | 1.7934 mL | 3.5869 mL | 8.9672 mL | |
| 10 mM | 0.1793 mL | 0.8967 mL | 1.7934 mL | 4.4836 mL | |
| 15 mM | 0.1196 mL | 0.5978 mL | 1.1956 mL | 2.9891 mL | |
| 20 mM | 0.0897 mL | 0.4484 mL | 0.8967 mL | 2.2418 mL | |
| 25 mM | 0.0717 mL | 0.3587 mL | 0.7174 mL | 1.7934 mL | |
| 30 mM | 0.0598 mL | 0.2989 mL | 0.5978 mL | 1.4945 mL | |
| 40 mM | 0.0448 mL | 0.2242 mL | 0.4484 mL | 1.1209 mL | |
| 50 mM | 0.0359 mL | 0.1793 mL | 0.3587 mL | 0.8967 mL | |
| 60 mM | 0.0299 mL | 0.1495 mL | 0.2989 mL | 0.7473 mL | |
| 80 mM | 0.0224 mL | 0.1121 mL | 0.2242 mL | 0.5604 mL | |
| 100 mM | 0.0179 mL | 0.0897 mL | 0.1793 mL | 0.4484 mL |
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