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.
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- Purity: 99.96%
- CAS No.: 1892576-07-6
- 화학식: C14H23NO2
- 분자량:237.34
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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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
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[PMID: 27326330] |
| HEK293 | EC50 |
0.352 nM
Compound: 51
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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
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[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.
Chemical Information
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CAS No. 1892576-07-6
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Appearance Solid
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분자량 237.34
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
순도&문서
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Data Sheet (264 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LY237 Related Classifications
HY-178234 Related Classifications
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