LAS191859
Based on 1 Customer Validation
LAS191859 is an orally active, potent and selective CRTh2 antagonist with an IC50 of 9.58 nM against human CRTh2. LAS191859 can be used for the research of chronic asthma.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.93%
- No. CAS: 1420071-13-1
- Fòrmula: C24H24F3N3O3
- Peso molecular:459.46
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Almacenamiento:Powder -20°C, 3 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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
IC50: 7.6 nM (guinea pig CRTh2), 9.58 nM (human CRTh2), 14 nM (rat CRTh2), 15.5 nM (mouse CRTh2)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| CHO-K1 | IC50 |
10 nM
Compound: 14
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Antagonist activity at CRTh2 receptor (unknown origin) overexpressed in CHOK1 cell membranes assessed as inhibition of [35S]-GTPgammaS binding measured after 2 hrs by liquid scintillation counting analysis
Antagonist activity at CRTh2 receptor (unknown origin) overexpressed in CHOK1 cell membranes assessed as inhibition of [35S]-GTPgammaS binding measured after 2 hrs by liquid scintillation counting analysis
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[PMID: 25437505] |
Chemical Information
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No. CAS 1420071-13-1
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Appearance Solid
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Peso molecular 459.46
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Fòrmula C24H24F3N3O3
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Color White to off-white
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SMILES
CCN(CC1=CC(C(F)(F)F)=CC=C1N2C=C(C3=C2N=C(C=C3)C)CC(O)=O)C(C4CC4)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (217.65 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 (5.44 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.
Pureza y Documentación
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Ficha de datos (277 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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Instrucciones de manejo (2659 KB)
Referencias
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 | 2.1765 mL | 10.8823 mL | 21.7647 mL | 54.4117 mL |
| 5 mM | 0.4353 mL | 2.1765 mL | 4.3529 mL | 10.8823 mL | |
| 10 mM | 0.2176 mL | 1.0882 mL | 2.1765 mL | 5.4412 mL | |
| 15 mM | 0.1451 mL | 0.7255 mL | 1.4510 mL | 3.6274 mL | |
| 20 mM | 0.1088 mL | 0.5441 mL | 1.0882 mL | 2.7206 mL | |
| 25 mM | 0.0871 mL | 0.4353 mL | 0.8706 mL | 2.1765 mL | |
| 30 mM | 0.0725 mL | 0.3627 mL | 0.7255 mL | 1.8137 mL | |
| 40 mM | 0.0544 mL | 0.2721 mL | 0.5441 mL | 1.3603 mL | |
| 50 mM | 0.0435 mL | 0.2176 mL | 0.4353 mL | 1.0882 mL | |
| 60 mM | 0.0363 mL | 0.1814 mL | 0.3627 mL | 0.9069 mL | |
| 80 mM | 0.0272 mL | 0.1360 mL | 0.2721 mL | 0.6801 mL | |
| 100 mM | 0.0218 mL | 0.1088 mL | 0.2176 mL | 0.5441 mL |
LAS191859 Related Classifications
HY-123596 Related Classifications
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