DG-041
Based on 3 publication(s) in Google Scholar
DG-041 is a potent, high affinity and selective EP3 receptor antagonist with IC50s of 4.6 nM and 8.1 nM in the binding and FLIPR assay, respectively. DG-041 inhibits PGE2 facilitation of platelet aggregation. DG-041 crosses the blood-brain barrier.
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: 99.61%
- CAS 番号: 861238-35-9
- 分子式: C23H15Cl4FN2O3S2
- 分子量:592.32
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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
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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 DG-041
More
生物活性
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EP3 4.6-8.1 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Platelet | IC50 |
218 nM
Compound: 50
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Antiplatelet activity against human platelet rich plasma assessed as inhibition of collagen and sulprostone-induced platelet aggregation by platelet aggregometer
Antiplatelet activity against human platelet rich plasma assessed as inhibition of collagen and sulprostone-induced platelet aggregation by platelet aggregometer
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[PMID: 19957930] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male SpragueDawley rat[1]
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Dosage:1.78 mg/kg (intravenous) or 9.62 mg/kg (oral)
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Administration:Intravenous or oral
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Result:Had t1/2 of 2.7 hours, 4.06 hours and Cmax of 9.46 μM, 2.74 μM for intravenous and oral administration, respectively.
化学情報
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CAS 番号 861238-35-9
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性状 Solid
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分子量 592.32
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分子式 C23H15Cl4FN2O3S2
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Color Light yellow to green yellow
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SMILES
O=C(NS(=O)(C1=CC(Cl)=C(Cl)S1)=O)/C=C/C2=CC(F)=CC3=C2N(CC4=CC=C(Cl)C=C4Cl)C=C3C
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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
Publications (3)
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Journal Impact Factor
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Most Recent
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Arterioscler Thromb Vasc Biol
Endothelial YAP Mediates Hyperglycemia-Induced Platelet Hyperactivity and Arterial Thrombosis. [Abstract]2024 Jan;44(1):254-270. PMID: 37916416 -
J Thromb Haemost
Endothelial NADPH oxidase 5 overexpression promotes thrombosis and alters thrombus composition by sex-dependent mechanisms in mice. [Abstract]2025 May 26:S1538-7836(25)00334-4. PMID: 40436274 -
Mol Cell Endocrinol
In vitro primary hyperparathyroidism model application of computationally repurposed drugs. [Abstract]2024 Apr 1:583:112159. PMID: 38228226
溶剤 & 溶解度
DMSO : 250 mg/mL (422.07 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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: ≥ 2.08 mg/mL (3.51 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
純度とドキュメンテーション
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データシート (279 KB)
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SDS (251 KB)
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- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Singh J, et al. Antagonists of the EP3 receptor for prostaglandin E2 are novel antiplatelet agents that do not prolong bleeding. ACS Chem Biol. 2009 Feb 20;4(2):115-26. [Content Brief]
[2]. Hategan G, et al. Heterocyclic 1,7-disubstituted indole sulfonamides are potent and selective human EP3 receptorantagonists. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6797-800. [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 | 1.6883 mL | 8.4414 mL | 16.8828 mL | 42.2069 mL |
| 5 mM | 0.3377 mL | 1.6883 mL | 3.3766 mL | 8.4414 mL | |
| 10 mM | 0.1688 mL | 0.8441 mL | 1.6883 mL | 4.2207 mL | |
| 15 mM | 0.1126 mL | 0.5628 mL | 1.1255 mL | 2.8138 mL | |
| 20 mM | 0.0844 mL | 0.4221 mL | 0.8441 mL | 2.1103 mL | |
| 25 mM | 0.0675 mL | 0.3377 mL | 0.6753 mL | 1.6883 mL | |
| 30 mM | 0.0563 mL | 0.2814 mL | 0.5628 mL | 1.4069 mL | |
| 40 mM | 0.0422 mL | 0.2110 mL | 0.4221 mL | 1.0552 mL | |
| 50 mM | 0.0338 mL | 0.1688 mL | 0.3377 mL | 0.8441 mL | |
| 60 mM | 0.0281 mL | 0.1407 mL | 0.2814 mL | 0.7034 mL | |
| 80 mM | 0.0211 mL | 0.1055 mL | 0.2110 mL | 0.5276 mL | |
| 100 mM | 0.0169 mL | 0.0844 mL | 0.1688 mL | 0.4221 mL |
DG-041 関連分類
HY-10835 関連分類
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