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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1380887-60-4
- 分子式: C31H30F2N6O3
- 分子量:572.61
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
Cellular Effect
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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] |
体外実験
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. .
体内実験
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.
化学情報
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CAS 番号 1380887-60-4
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分子量 572.61
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
MK-8825 関連分類
HY-117694 関連分類
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