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
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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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
Cellular Effect
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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] |
In Vitro
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. Further protocols information, click here.
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
용액&용해도
In Vitro:
DMSO : 25 mg/mL (105.33 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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DSS-Induced Colitis
Dextran sulfate sodium (DSS)-induced colitis is generated by administering DSS in mouse drinking water, producing epithelial injury, barrier disruption, weight loss, diarrhea, fecal blood, colon shortening, histologic mucosal damage, and inflammatory mediator changes; the model is mainly used to study acute or chronic intestinal inflammation resembling selected features of ulcerative colitis. DSS injury is interpreted through clinical and tissue readouts rather than a single molecular endpoint: daily body weight, stool consistency, and bleeding are combined into a disease activity index, while colon length, histology, cytokines, myeloperoxidase activity, intestinal permeability, and tight-junction markers provide complementary measures of inflammation and barrier damage.
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TNBS-Induced Colitis
TNBS-induced colitis is produced by intrarectal delivery of 2,4,6-trinitrobenzene sulfonic acid in ethanol, where ethanol disrupts the mucosal barrier and TNBS haptenates colonic proteins, generating immune-mediated colonic inflammation with weight loss, diarrhea, ulceration, transmural injury, inflammatory-cell infiltration, and cytokine responses. The model is used as an experimental intestinal inflammation model with Crohn’s disease–like features, especially when Th1-type responses, IL-12–dependent inflammation, chronic relapsing inflammation, or fibrosis-related endpoints are studied.
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
순도&문서
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Data Sheet (268 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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.2134 mL | 21.0668 mL | 42.1336 mL | 105.3341 mL |
| 5 mM | 0.8427 mL | 4.2134 mL | 8.4267 mL | 21.0668 mL | |
| 10 mM | 0.4213 mL | 2.1067 mL | 4.2134 mL | 10.5334 mL | |
| 15 mM | 0.2809 mL | 1.4045 mL | 2.8089 mL | 7.0223 mL | |
| 20 mM | 0.2107 mL | 1.0533 mL | 2.1067 mL | 5.2667 mL | |
| 25 mM | 0.1685 mL | 0.8427 mL | 1.6853 mL | 4.2134 mL | |
| 30 mM | 0.1404 mL | 0.7022 mL | 1.4045 mL | 3.5111 mL | |
| 40 mM | 0.1053 mL | 0.5267 mL | 1.0533 mL | 2.6334 mL | |
| 50 mM | 0.0843 mL | 0.4213 mL | 0.8427 mL | 2.1067 mL | |
| 60 mM | 0.0702 mL | 0.3511 mL | 0.7022 mL | 1.7556 mL | |
| 80 mM | 0.0527 mL | 0.2633 mL | 0.5267 mL | 1.3167 mL | |
| 100 mM | 0.0421 mL | 0.2107 mL | 0.4213 mL | 1.0533 mL |
LY237 Related Classifications
HY-178234 Related Classifications
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