MK-8825
MK-8825 is an orally active, selective CGRP receptor antagonist with a Ki value of 47 pM for human CGRP receptors and 17 nM for rat CGRP receptors. MK-8825 blocks CGRP-stimulated cAMP responses and exhibits competitive-like antagonism. MK-8825 can be used in the research of migraine and temporomandibular joint disorders.
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- CAS No.: 1380887-60-4
- Formule: C31H30F2N6O3
- Masse moléculaire:572.61
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.23 nM
Compound: 6, MK-8825
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Antagonist activity at human CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-induced cAMP response after 5 mins in the absence of human serum
Antagonist activity at human CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-induced cAMP response after 5 mins in the absence of human serum
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[PMID: 22607672] |
| HEK293 | IC50 |
0.34 nM
Compound: 6, MK-8825
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Antagonist activity at human CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-induced cAMP response after 5 mins in the presence of 50% human serum
Antagonist activity at human CGRP receptor expressed in HEK293 cells assessed as inhibition of CGRP-induced cAMP response after 5 mins in the presence of 50% human serum
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[PMID: 22607672] |
MK-8825 potently inhibits the binding of 125I-hCGRP to the native human CGRP receptor in SK-N-MC cells, with a Ki value of 0.052 nM[1].
MK-8825 potently inhibits the binding of 125I-hCGRP to rhesus monkey CGRP receptors, with a Ki value of 0.059 nM[1].
MK-8825 inhibits the binding of 125I-hCGRP to canine CGRP receptors, with a Ki value of 39 nM[1].
MK-8825 inhibits the binding of 125I-hCGRP to rabbit CGRP receptors, with a Ki value of 15 nM[1].
MK-8825 inhibits the binding of 125I-hCGRP to mouse CGRP receptors, with a Ki value of 19 nM[1].
MK-8825 potently blocks hCGRP-induced cAMP production in HEK293 cells expressing human CGRP receptors, with an IC50 of 0.23 nM[1].
MK-8825 inhibits the binding of human AM2 receptor with a Ki value of 590 nM[1].
MK-8825 inhibits the binding of human CT receptors with a Ki value of 3,200 nM[1].
MK-8825 inhibits the binding of human AMY1 receptor with a Ki value of 0.64 nM[1].
MK-8825 inhibits the binding of human AMY3 receptors with a Ki value of 1,100 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57Bl/6 (female, 5-7 weeks old, 20-30 g, injected with CFA into right masseter muscle)[2]
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Dosage:70 mg/kg
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Administration:s.c.; single dose
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Result:Significantly decreased the duration of spontaneous nociceptive facial grooming behaviors (forepaw face rubbing, chin/cheek rubbing, hindpaw face scratching).
Reduced Fos‑positive neurons in the trigeminal nucleus caudalis at 2 h and 24 h after CFA injection.
Did not change serum interleukin‑6 (IL‑6) levels induced by CFA at either time point.
Chemical Information
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CAS No. 1380887-60-4
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Masse moléculaire 572.61
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Formule C31H30F2N6O3
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SMILES
O=C1[C@]2(CC3=CC(NC(CN4[C@@](CNC5(CCCC5)C4=O)(C6=CC(F)=CC(F)=C6)C)=O)=CN=C3C2)C7=CC=CN=C7N1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Bell IM, et al. MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. Bioorg Med Chem Lett. 2012;22(12):3941-3945. [Content Brief]
[2]. Romero-Reyes M, et al. A potent and selective calcitonin gene-related peptide (CGRP) receptor antagonist, MK-8825, inhibits responses to nociceptive trigeminal activation: Role of CGRP in orofacial pain. Exp Neurol. 2015 Sep;271:95-103. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MK-8825 Related Classifications
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