TAK-615
Based on 1 Customer Validation
TAK-615 is a negative allosteric modulator (NAM) of the LPA1 receptor for the research of pulmonary fibrosis. TAK-615 binds the LPA1 receptor with high affinity (Kd high affinity of 1.7 nM and Kd low affinity of 14.5 nM).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.07%
- No. CAS: 1664335-55-0
- Fòrmula: C25H22FNO4
- Peso molecular:419.44
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Almacenamiento: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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
LPA1 Receptor 1.7-14.5 nM (Kd) |
In Vitro
TAK-615 specifically binds to membranes expressing the human LPA1 receptor with estimated Kd high affinity (KdHi) of 1.7±0.5 nM and Kd low affinity (KdLo) of 14.5±12.1 nM[1].
TAK-615 is only able to partially inhibit the LPA response (~ 40% at 10 μM with an IC50 of 23±13 nM in β-arrestin assay; 60% at 10 μM, IC50 of 91±30 nM in calcium mobilisation assay) [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1664335-55-0
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Appearance Solid
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Peso molecular 419.44
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Fòrmula C25H22FNO4
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Color White to off-white
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SMILES
O=C(O)C1=CC=C(CN(CC2CC2)C(C3=CC=C(OC4=CC=CC=C4F)C=C3)=O)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 125 mg/mL (298.02 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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.96 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 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.
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 (272 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3841 mL | 11.9207 mL | 23.8413 mL | 59.6033 mL |
| 5 mM | 0.4768 mL | 2.3841 mL | 4.7683 mL | 11.9207 mL | |
| 10 mM | 0.2384 mL | 1.1921 mL | 2.3841 mL | 5.9603 mL | |
| 15 mM | 0.1589 mL | 0.7947 mL | 1.5894 mL | 3.9736 mL | |
| 20 mM | 0.1192 mL | 0.5960 mL | 1.1921 mL | 2.9802 mL | |
| 25 mM | 0.0954 mL | 0.4768 mL | 0.9537 mL | 2.3841 mL | |
| 30 mM | 0.0795 mL | 0.3974 mL | 0.7947 mL | 1.9868 mL | |
| 40 mM | 0.0596 mL | 0.2980 mL | 0.5960 mL | 1.4901 mL | |
| 50 mM | 0.0477 mL | 0.2384 mL | 0.4768 mL | 1.1921 mL | |
| 60 mM | 0.0397 mL | 0.1987 mL | 0.3974 mL | 0.9934 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 |
TAK-615 Related Classifications
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