GB-110
Based on 1 publication(s) in Google Scholar
GB-110 is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist. GB-110 selectively induces PAR2-mediated intracellular Ca2+ release in HT29 cells with an EC50 of 0.28 μM.
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: 1252806-70-4
- 分子式: C33H48N6O5
- 分子量:608.77
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
MedChemExpress(MCE)の使用を引用している文献 GB-110
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生物活性
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PAR2 .28 μM (EC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-29 | EC50 |
0.28 μM
Compound: 19
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Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
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[PMID: 20873792] |
In an intracellular Ca2+ (iCa2+) mobilization assay using HT29 colon cancer cells, GB110 (EC50 240±20 nM; pEC50 6.7±0.05) is equipotent with the peptide agonist 2f-LIGRLO-NH2 (EC50 210±30 nM; pEC50 6.6±0.05), 10-fold more potent than SLIGRL-NH2, but ~35-fold less potent than trypsin (EC50 6±0.5 nM; pEC50 8.2±0.8)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1252806-70-4
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分子量 608.77
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分子式 C33H48N6O5
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SMILES
O=C(C1=CC=NO1)N[C@@H](CC2CCCCC2)C(N[C@@H]([C@@H](C)CC)C(NCC3=CC=CC(C(N4CCC(CN)CC4)=O)=C3)=O)=O
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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.
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Mol Gastroenterol Hepatol
Elafin Reverses Intestinal Fibrosis by Inhibiting Cathepsin S-Mediated Protease-Activated Receptor 2. [Abstract]2022;14(4):841-876. PMID: 35840034
純度とドキュメンテーション
参考文献
[1]. Barry GD, et al. Novel agonists and antagonists for human protease activated receptor 2. J Med Chem. 2010 Oct 28;53(20):7428-40. [Content Brief]
[2]. Suen JY, et al. Modulating human proteinase activated receptor 2 with a novel antagonist (GB88) and agonist (GB110). Br J Pharmacol. 2012 Mar;165(5):1413-23. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)