HPGDS inhibitor 2
Based on 1 Customer Validation
HPGDS inhibitor 2 is a highly potent and selective hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with an IC50 of 9.9 nM.
For research use only. We do not sell to patients.
- Purity: 99.70%
- CAS No.: 2101626-26-8
- Formula: C20H24F2N2O3
- Molecular Weight:378.41
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Biological Activity
IC50: 9.9 nM (H-PGDS)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Mast cell | EC50 |
21 nM
Compound: 1a; GSK2894631A
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Anti-inflammatory activity against mast cell degranulation inflammatory C57BL/6J mouse model assessed as blood EC50 required for reduction in compound 48/80-induced PGD2 release into peritoneal lavage fluid administered orally with compound and 1 hr later
Anti-inflammatory activity against mast cell degranulation inflammatory C57BL/6J mouse model assessed as blood EC50 required for reduction in compound 48/80-induced PGD2 release into peritoneal lavage fluid administered orally with compound and 1 hr later
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[PMID: 33059303] |
| Mast cell | ED50 |
0.032 mg/kg
Compound: 1a; GSK2894631A
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Anti-inflammatory activity against mast cell degranulation inflammatory C57BL/6J mouse model assessed as reduction in compound 48/80-induced PGD2 release into peritoneal lavage fluid administered orally with compound and 1 hr later treated with compound 4
Anti-inflammatory activity against mast cell degranulation inflammatory C57BL/6J mouse model assessed as reduction in compound 48/80-induced PGD2 release into peritoneal lavage fluid administered orally with compound and 1 hr later treated with compound 4
|
[PMID: 33059303] |
Chemical Information
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CAS No. 2101626-26-8
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Appearance Solid
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Molecular Weight 378.41
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Formula C20H24F2N2O3
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Color White to off-white
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SMILES
FC(F)OC1=CC=C2C(N=CC(C(N[C@@H]3CC[C@@H](C(C)(C)O)CC3)=O)=C2)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : ≥ 150 mg/mL (396.40 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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 (6.61 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.61 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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 (269 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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 (sealed storage, away from moisture and light). 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 | 2.6426 mL | 13.2132 mL | 26.4264 mL | 66.0659 mL |
| 5 mM | 0.5285 mL | 2.6426 mL | 5.2853 mL | 13.2132 mL | |
| 10 mM | 0.2643 mL | 1.3213 mL | 2.6426 mL | 6.6066 mL | |
| 15 mM | 0.1762 mL | 0.8809 mL | 1.7618 mL | 4.4044 mL | |
| 20 mM | 0.1321 mL | 0.6607 mL | 1.3213 mL | 3.3033 mL | |
| 25 mM | 0.1057 mL | 0.5285 mL | 1.0571 mL | 2.6426 mL | |
| 30 mM | 0.0881 mL | 0.4404 mL | 0.8809 mL | 2.2022 mL | |
| 40 mM | 0.0661 mL | 0.3303 mL | 0.6607 mL | 1.6516 mL | |
| 50 mM | 0.0529 mL | 0.2643 mL | 0.5285 mL | 1.3213 mL | |
| 60 mM | 0.0440 mL | 0.2202 mL | 0.4404 mL | 1.1011 mL | |
| 80 mM | 0.0330 mL | 0.1652 mL | 0.3303 mL | 0.8258 mL | |
| 100 mM | 0.0264 mL | 0.1321 mL | 0.2643 mL | 0.6607 mL |