LY237
Based on 1 Customer Validation
LY237 is a potent GPR84 full agonist, with EC50 values of 0.189 nM and 0.07 nM in cAMP inhibition assay and calcium flux assay, respectively. LY237 binds to the amphipathic orthosteric pocket of GPR84, stabilizes the active conformation of the receptor, and promotes its coupling with Gαi protein. LY237 can be used in research related to ulcerative colitis, fibrotic diseases, non-alcoholic steatohepatitis, and acute respiratory distress syndrome.
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。
- 純度: 99.96%
- CAS 番号: 1892576-07-6
- 分子式: C14H23NO2
- 分子量:237.34
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
0.00018 μM
Compound: 51
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Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay
|
[PMID: 27326330] |
| HEK293 | EC50 |
0.352 nM
Compound: 51
|
Agonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assay
Agonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assay
|
[PMID: 27326330] |
LY237 interacts with specific residues in the extracellular loop 2 and transmembrane domain of the receptor, thereby driving activation signal transduction[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 1892576-07-6
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性状 Solid
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分子量 237.34
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分子式 C14H23NO2
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Color White to off-white
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SMILES
O=C1C=C(C=C(CCCCCCCCC)N1)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
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
純度とドキュメンテーション
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データシート (264 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
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- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Ieremias L, et al. Minimal Structural Variation of GPR84 Full Agonist Causes Functional Switch to Inverse Agonism. Journal of medicinal chemistry. 2025 Apr 24;68(8):7973-8009. [Content Brief]
[2]. Liu H, et al. Structural insights into ligand recognition and activation of the medium-chain fatty acid-sensing receptor GPR84. Nature communications. 2023 Jun 06;14(1):3271. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)