HPGDS inhibitor 1
Based on 1 Customer Validation
HPGDS inhibitor 1 is a potent, selective and orally active Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50s of 0.6 nM and 32 nM in enzyme and cellular assays, respectively. HPGDS inhibitor 1 does not inhibit human L-PGDS, mPGES, COX-1, COX-2, or 5-LOX.
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- Pureté : 99.42%
- CAS No.: 1033836-12-2
- Formule: C19H19F4N3O
- Masse moléculaire:381.37
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
IC50: 0.6 nM (HPGDS in enzyme assays) and 32 nM (HPGDS in cellular assays)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MEG-01 | EC50 |
0.035 μM
Compound: 1
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Inhibition HPGDS in human MEG01 cells assessed as reduction in PGD2 production incubated for 30 mins followed by stimulation with 5 uM ionomycin for 30 mins by enzyme immunoassay method
Inhibition HPGDS in human MEG01 cells assessed as reduction in PGD2 production incubated for 30 mins followed by stimulation with 5 uM ionomycin for 30 mins by enzyme immunoassay method
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[PMID: 25978964] |
In Vitro
HPGDS inhibitor 1 has equal potency against purified HPGDS from human, rat, dog, and sheep (IC50, 0.5-2.3 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
Rats dosed orally with 1 mg/kg and 10 mg/kg HPGDS inhibitor 1 (compound 8) are sacrificed at various times. Oral administration of HPGDS inhibitor 1 blocks PGD2 production in the rat spleen; inhibition of PGD2 is inversely correlated with the plasma concentration of HPGDS inhibitor 1 in a time- and dose-dependent manner[1].
HPGDS inhibitor 1 (compound 8; 1 mg/mL) illustrates efficacy in an in vivo sheep model of asthma[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1033836-12-2
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Appearance Solid
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Masse moléculaire 381.37
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Formule C19H19F4N3O
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Color White to off-white
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SMILES
O=C(NC1CCN(CC(F)(F)F)CC1)C2=CC=C(C3=CC=CC(F)=C3)N=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvant et solubilité
In Vitro:
DMSO : 50 mg/mL (131.11 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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.
Pureté et documentation
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Fiche technique (275 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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Instruction de manipulation (2659 KB)
Références
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6221 mL | 13.1106 mL | 26.2213 mL | 65.5531 mL |
| 5 mM | 0.5244 mL | 2.6221 mL | 5.2443 mL | 13.1106 mL | |
| 10 mM | 0.2622 mL | 1.3111 mL | 2.6221 mL | 6.5553 mL | |
| 15 mM | 0.1748 mL | 0.8740 mL | 1.7481 mL | 4.3702 mL | |
| 20 mM | 0.1311 mL | 0.6555 mL | 1.3111 mL | 3.2777 mL | |
| 25 mM | 0.1049 mL | 0.5244 mL | 1.0489 mL | 2.6221 mL | |
| 30 mM | 0.0874 mL | 0.4370 mL | 0.8740 mL | 2.1851 mL | |
| 40 mM | 0.0656 mL | 0.3278 mL | 0.6555 mL | 1.6388 mL | |
| 50 mM | 0.0524 mL | 0.2622 mL | 0.5244 mL | 1.3111 mL | |
| 60 mM | 0.0437 mL | 0.2185 mL | 0.4370 mL | 1.0926 mL | |
| 80 mM | 0.0328 mL | 0.1639 mL | 0.3278 mL | 0.8194 mL | |
| 100 mM | 0.0262 mL | 0.1311 mL | 0.2622 mL | 0.6555 mL |
HPGDS inhibitor 1 Related Classifications
HY-10439 Related Classifications
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