LPA2 antagonist 1

Name: LPA2 antagonist 1
Brand: MedChemExpress
SKU: HY-18075
Rating: 5.0 (3 reviews)

Cat. No.: HY-18075 Purity: 98.63%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

LPA2 antagonist 1 is a LPA2 antagonist with an IC₅₀ of 17 nM.

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

LPA2 antagonist 1 Chemical Structure

CAS No. : 1017606-66-4

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 385	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 385	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 350	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 560	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1400	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2100	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 3 publication(s) in Google Scholar

3 Publications Citing Use of MCE LPA2 antagonist 1

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Biological Activity
Purity & Documentation
References
Customer Review

Description

LPA2 antagonist 1 is a LPA2 antagonist with an IC₅₀ of 17 nM.

IC₅₀ & Target

IC50: 17 nM (LPA2)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
RH7777	IC₅₀	> 50 μM Compound: 35	Antagonist activity at LPA1 expressed in RH7777 cells with Gi4-protein and aequorin by calcium mobilization assay Antagonist activity at LPA1 expressed in RH7777 cells with Gi4-protein and aequorin by calcium mobilization assay	[PMID: 18178086]
RH7777	IC₅₀	> 50 μM Compound: 35	Antagonist activity at LPA3 expressed in RH7777 cells with Gi4-protein and aequorin by calcium mobilization assay Antagonist activity at LPA3 expressed in RH7777 cells with Gi4-protein and aequorin by calcium mobilization assay	[PMID: 18178086]
RH7777	IC₅₀	0.017 μM Compound: 35	Antagonist activity at LPA2 expressed in RH7777 cells with Gi4-protein and aequorin by calcium mobilization assay Antagonist activity at LPA2 expressed in RH7777 cells with Gi4-protein and aequorin by calcium mobilization assay	[PMID: 18178086]

In Vitro

LPA2 antagonist 1 inhibits the phosphorylation of Erk induced by LPA in a concentration dependent manner. LPA2 antagonist 1 inhibits HCT-116 colon cancer cell proliferation caused by LPA in a doses dependent manner^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

500.46

Formula

C₂₀H₂₃Cl₂N₅O₂S₂

CAS No.

1017606-66-4

Appearance

Solid

Color

White to off-white

SMILES

ClC1=C(Cl)C=C(S(=O)(N2CCN(C[C@@H](NC3=NC=NC4=C3SC=C4C)C)CC2)=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	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (199.82 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

DMF : ≥ 100 mg/mL (199.82 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9982 mL	9.9908 mL	19.9816 mL
5 mM	0.3996 mL	1.9982 mL	3.9963 mL
10 mM	0.1998 mL	0.9991 mL	1.9982 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, 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (5.00 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.00 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

Purity: 98.63%

Select Batch:

Data Sheet (275 KB) SDS (393 KB)

COA (252 KB) LCMS (96 KB)

Handling Instructions (2659 KB)

References

[1]. Beck HP, et al. Discovery of potent LPA2 (EDG4) antagonists as potential anticancer agents. Bioorg Med Chem Lett. 2008 Feb 1;18(3):1037-41. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / DMF	1 mM	1.9982 mL	9.9908 mL	19.9816 mL	49.9540 mL
	5 mM	0.3996 mL	1.9982 mL	3.9963 mL	9.9908 mL
	10 mM	0.1998 mL	0.9991 mL	1.9982 mL	4.9954 mL
	15 mM	0.1332 mL	0.6661 mL	1.3321 mL	3.3303 mL
	20 mM	0.0999 mL	0.4995 mL	0.9991 mL	2.4977 mL
	25 mM	0.0799 mL	0.3996 mL	0.7993 mL	1.9982 mL
	30 mM	0.0666 mL	0.3330 mL	0.6661 mL	1.6651 mL
	40 mM	0.0500 mL	0.2498 mL	0.4995 mL	1.2489 mL
	50 mM	0.0400 mL	0.1998 mL	0.3996 mL	0.9991 mL
	60 mM	0.0333 mL	0.1665 mL	0.3330 mL	0.8326 mL
	80 mM	0.0250 mL	0.1249 mL	0.2498 mL	0.6244 mL
	100 mM	0.0200 mL	0.0999 mL	0.1998 mL	0.4995 mL