Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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Other Sizes |
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Targets |
LPA1 Receptor 1.7-14.5 nM (Kd)
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ln Vitro |
TAK-615 has a specific binding affinity of 1.7±0.5 nM for human LPA1 receptor-expressing membranes and 14.5±12.1 nM for Kd low affinity (KdLo) receptors[1]. Only about 40% of the LPA response can be inhibited by TAK-615 at 10 µM, with an IC50 of 23±13 nM in the β-arrestin assay, and 60% at 10 µM, with an IC50 of 91±30 nM in the calcium mobilization assay [1].
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References |
[1]. Jonathan Ellery, et al. Identification of Compounds Acting as Negative Allosteric Modulators of the LPA 1 Receptor. Eur J Pharmacol. 2018 Aug 15;833:8-15.
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Molecular Formula |
C25H22FNO4
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Molecular Weight |
419.44
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CAS # |
1664335-55-0
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SMILES |
FC1C=CC=CC=1OC1C=CC(=CC=1)C(N(CC1C=CC(C(=O)O)=CC=1)CC1CC1)=O
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: 125 mg/mL (298.02 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.96 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.96 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.3841 mL | 11.9207 mL | 23.8413 mL | |
5 mM | 0.4768 mL | 2.3841 mL | 4.7683 mL | |
10 mM | 0.2384 mL | 1.1921 mL | 2.3841 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.