1. GPCR/G Protein
  2. LPL Receptor
  3. TAK-615

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).

For research use only. We do not sell to patients.

TAK-615 Chemical Structure

TAK-615 Chemical Structure

CAS No. : 1664335-55-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 308 In-stock
Solution
10 mM * 1 mL in DMSO USD 308 In-stock
Solid
1 mg USD 110 In-stock
5 mg USD 280 In-stock
10 mg USD 440 In-stock
25 mg USD 790 In-stock
50 mg USD 1180 In-stock
100 mg USD 1780 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

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)[1].

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.

Molecular Weight

419.44

Formula

C25H22FNO4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)C1=CC=C(CN(CC2CC2)C(C3=CC=C(OC4=CC=CC=C4F)C=C3)=O)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (4.96 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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+
%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
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. 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
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TAK-615 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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TAK-615
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