DA-1241
Based on 1 Customer Validation
DA-1241 is a GPR119 agonist. DA-1241 reduces macrophage differentiation through downregulation of NFκB signaling by activating GPR119. DA-1241, alone and in combination with a DPP4 inhibitor, reduces liver inflammation and restores inflammation-related liver gene expression. DA-1241 can be used for the research of metabolic dysfunction-associated steatohepatitis (MASH).
For research use only. We do not sell to patients.
- Purity : 99.18%
- CAS No.: 1914136-10-9
- Formula: C25H31F2N5O2
- Molecular Weight:471.54
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Storage: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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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1914136-10-9
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Appearance Solid
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Molecular Weight 471.54
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Formula C25H31F2N5O2
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Color White to off-white
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SMILES
CC(C1=NC(C2=C(F)C=C(OCCCC3CCN(C4=NC=C(CC)C=N4)CC3)C=C2F)=NO1)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (212.07 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.30 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Protocols
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RT-PCR
Reverse transcription technology uses RNA as a template to synthesize DNA. RT-PCR is simple, specific and sensitive, and can be used to detect gene expression levels and expression differences in cells; detect RNA virus content; clone cDNA sequences of specific genes.
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Primary monocyte-to-macrophage differentiation
Primary human monocytes can be differentiated ex vivo into monocyte-derived macrophages by culturing purified blood monocytes for approximately 5-7 days in macrophage-supporting cytokine conditions; M-CSF commonly yields CD14^high/CD163^high macrophages, while GM-CSF yields a phenotypically distinct macrophage population, so the cytokine condition should be chosen according to the downstream model. The readout of successful differentiation is a combined change in morphology, adherence, surface phenotype, and function: differentiated macrophages become adherent, enlarge, acquire macrophage-associated markers such as CD14, CD68, CD163, CD206, or HLA-DR depending on culture condition, and show increased phagocytic capacity compared with starting monocytes.
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THP-1 macrophage-like differentiation
THP-1 monocytes are differentiated into macrophage-like adherent cells by exposure to phorbol 12-myristate 13-acetate (PMA), a phorbol ester used across published THP-1 macrophage differentiation studies; differentiation is assessed by adherence, macrophage-like morphology, altered macrophage-associated surface markers such as CD11b, CD14, CD36, and CD204, phagocytic capacity, lysosomal/mitochondrial enrichment, cytokine responsiveness, and transcriptomic or proteomic remodeling. Because PMA concentration, exposure duration, and post-PMA resting time change downstream phenotype and immune responses, this protocol treats PMA differentiation as a model-generation step rather than a universal macrophage replacement method; low-dose PMA with a rest period is preferred when subsequent inflammatory or infection assays are planned.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
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Real Time qPCR (Q-PCR)
Real-time quantitative PCR (qPCR) quantifies an amplifiable nucleic-acid target by monitoring fluorescence during PCR cycling rather than measuring product only after amplification. The increase in fluorescence tracks accumulation of PCR product, and the quantification cycle (Cq; historically also Ct/CP) is related to the initial amount of target: samples containing more starting target generally reach the defined fluorescence threshold in fewer cycles.
Purity & Documentation
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Data Sheet (269 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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 |
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| DMSO | 1 mM | 2.1207 mL | 10.6036 mL | 21.2071 mL | 53.0178 mL |
| 5 mM | 0.4241 mL | 2.1207 mL | 4.2414 mL | 10.6036 mL | |
| 10 mM | 0.2121 mL | 1.0604 mL | 2.1207 mL | 5.3018 mL | |
| 15 mM | 0.1414 mL | 0.7069 mL | 1.4138 mL | 3.5345 mL | |
| 20 mM | 0.1060 mL | 0.5302 mL | 1.0604 mL | 2.6509 mL | |
| 25 mM | 0.0848 mL | 0.4241 mL | 0.8483 mL | 2.1207 mL | |
| 30 mM | 0.0707 mL | 0.3535 mL | 0.7069 mL | 1.7673 mL | |
| 40 mM | 0.0530 mL | 0.2651 mL | 0.5302 mL | 1.3254 mL | |
| 50 mM | 0.0424 mL | 0.2121 mL | 0.4241 mL | 1.0604 mL | |
| 60 mM | 0.0353 mL | 0.1767 mL | 0.3535 mL | 0.8836 mL | |
| 80 mM | 0.0265 mL | 0.1325 mL | 0.2651 mL | 0.6627 mL | |
| 100 mM | 0.0212 mL | 0.1060 mL | 0.2121 mL | 0.5302 mL |
DA-1241 Related Classifications
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