Ragaglitazar
Based on 1 Customer Validation
Ragaglitazar is a PPARα and PPARγ agonist with potent lipid-lowering and insulin-sensitizing efficacy in animal models. Ragaglitazar improves glycemic control and lipid profile in type 2 diabetic.
For research use only. We do not sell to patients.
- Purity: 99.24%
- CAS No.: 222834-30-2
- Formula: C25H25NO5
- Molecular Weight:419.47
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CV-1 | EC50 |
0.57 μM
Compound: 3
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Transactivation of GAL4-fused Homo sapiens (human) PPARgamma DNA binding domain expressed in African green monkey CV1 cells by luciferase reporter gene assay
Transactivation of GAL4-fused Homo sapiens (human) PPARgamma DNA binding domain expressed in African green monkey CV1 cells by luciferase reporter gene assay
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10.1007/s00044-012-0003-4 |
| CV-1 | EC50 |
3.21 μM
Compound: 3
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Transactivation of GAL4-fused Homo sapiens (human) PPARalpha DNA binding domain expressed in African green monkey CV1 cells by luciferase reporter gene assay
Transactivation of GAL4-fused Homo sapiens (human) PPARalpha DNA binding domain expressed in African green monkey CV1 cells by luciferase reporter gene assay
|
10.1007/s00044-012-0003-4 |
| HEK-293T | EC50 |
0.57 μM
Compound: (S)-4b
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Agonist activity at GAL4 fused human PPARgamma LBD (174 to 475 residues) expressed in HEK293T cells after 18 hrs by luciferase reporter gene assay
Agonist activity at GAL4 fused human PPARgamma LBD (174 to 475 residues) expressed in HEK293T cells after 18 hrs by luciferase reporter gene assay
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[PMID: 28539218] |
| HEK-293T | EC50 |
2.8 μM
Compound: (S)-4b
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Agonist activity at GAL4 fused human PPARalpha LBD (174 to 475 residues) expressed in HEK293T cells after 18 hrs by luciferase reporter gene assay
Agonist activity at GAL4 fused human PPARalpha LBD (174 to 475 residues) expressed in HEK293T cells after 18 hrs by luciferase reporter gene assay
|
[PMID: 28539218] |
Chemical Information
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CAS No. 222834-30-2
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Appearance Solid
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Molecular Weight 419.47
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Formula C25H25NO5
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Color Off-white to light yellow
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SMILES
O=C(O)[C@@H](OCC)CC1=CC=C(OCCN2C3=C(C=CC=C3)OC4=CC=CC=C24)C=C1
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Synonyms
(-)-DRF 2725; NNC 61-0029
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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
DMSO : 100 mg/mL (238.40 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)
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 (5.96 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.
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.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Chakrabarti R, Vikramadithyan RK, Misra P, et al. Ragaglitazar: a novel PPAR alpha PPAR gamma agonist with potent lipid-lowering and insulin-sensitizing efficacy in animal models. Br J Pharmacol. 2003;140(3):527-537. [Content Brief]
[2]. Saad MF, Greco S, Osei K, et al. Ragaglitazar improves glycemic control and lipid profile in type 2 diabetic subjects: a 12-week, double-blind, placebo-controlled dose-ranging study with an open pioglitazone arm. Diabetes Care. 2004;27(6):1324-1329. [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 | 2.3840 mL | 11.9198 mL | 23.8396 mL | 59.5990 mL |
| 5 mM | 0.4768 mL | 2.3840 mL | 4.7679 mL | 11.9198 mL | |
| 10 mM | 0.2384 mL | 1.1920 mL | 2.3840 mL | 5.9599 mL | |
| 15 mM | 0.1589 mL | 0.7947 mL | 1.5893 mL | 3.9733 mL | |
| 20 mM | 0.1192 mL | 0.5960 mL | 1.1920 mL | 2.9800 mL | |
| 25 mM | 0.0954 mL | 0.4768 mL | 0.9536 mL | 2.3840 mL | |
| 30 mM | 0.0795 mL | 0.3973 mL | 0.7947 mL | 1.9866 mL | |
| 40 mM | 0.0596 mL | 0.2980 mL | 0.5960 mL | 1.4900 mL | |
| 50 mM | 0.0477 mL | 0.2384 mL | 0.4768 mL | 1.1920 mL | |
| 60 mM | 0.0397 mL | 0.1987 mL | 0.3973 mL | 0.9933 mL | |
| 80 mM | 0.0298 mL | 0.1490 mL | 0.2980 mL | 0.7450 mL | |
| 100 mM | 0.0238 mL | 0.1192 mL | 0.2384 mL | 0.5960 mL |