1. GPCR/G Protein
  2. LPL Receptor
  3. LPA2 antagonist 2

LPA2 antagonist 2 (H2L 5226501) is a selective LPA2 antagonist with an IC50 of 28.3 nM and a Ki of 21.1 nM. LPA2 antagonist 2 is >480-fold more selective than LPA3 (IC50 of 13.85 μM).

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LPA2 antagonist 2

LPA2 antagonist 2 Estructura química

No. CAS : 36840-10-5

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Descripciòn

LPA2 antagonist 2 (H2L 5226501) is a selective LPA2 antagonist with an IC50 of 28.3 nM and a Ki of 21.1 nM. LPA2 antagonist 2 is >480-fold more selective than LPA3 (IC50 of 13.85 μM)[1].

IC50 & Target

IC50: 28.3 nM (LPA2); 13.85 μM (LPA3)[1]

Cellular Effect
Cell Line Type Value Description References
RH7777 IC50
13850 nM
Compound: 5226501
Antagonist activity at LPA3 receptor expressed in rat RH7777 cells assessed as inhibition of LPA-induced intracellular calcium concentration
Antagonist activity at LPA3 receptor expressed in rat RH7777 cells assessed as inhibition of LPA-induced intracellular calcium concentration
[PMID: 18467108]
RH7777 IC50
28.3 nM
Compound: 5226501
Antagonist activity at LPA2 receptor expressed in rat RH7777 cells assessed as inhibition of LPA-induced intracellular calcium concentration
Antagonist activity at LPA2 receptor expressed in rat RH7777 cells assessed as inhibition of LPA-induced intracellular calcium concentration
[PMID: 18467108]
In Vitro

Lysophosphatidic acid (LPA) is a phospholipid mediator that elicits a host of biological effects including cell proliferation, survival, motility and differentiation. LPA has been shown to regulate cancer cell invasion, metastasis, and resistance to both chemotherapeutics and radiation. LPA2 antagonist 2 (H2L 5226501) inhibits LPA1 with an Imax of 59.0% at 30 μM[1].

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

Peso molecular

380.35

Fòrmula

C20H16N2O6

No. CAS
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(O)/C=C/C(NC1=CC=C(C2=CC=C(NC(/C=C/C(O)=O)=O)C=C2)C=C1)=O

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvente y solubilidad
In Vitro: 

DMSO : 83.33 mg/mL (219.09 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 2.6292 mL 13.1458 mL 26.2916 mL
5 mM 0.5258 mL 2.6292 mL 5.2583 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.

  • Calculadora de molaridad

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

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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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C1

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Volume (start)

V1

=
Concentration (final)

C2

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V2

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

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(per animal)

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
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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, 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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6292 mL 13.1458 mL 26.2916 mL 65.7289 mL
5 mM 0.5258 mL 2.6292 mL 5.2583 mL 13.1458 mL
10 mM 0.2629 mL 1.3146 mL 2.6292 mL 6.5729 mL
15 mM 0.1753 mL 0.8764 mL 1.7528 mL 4.3819 mL
20 mM 0.1315 mL 0.6573 mL 1.3146 mL 3.2864 mL
25 mM 0.1052 mL 0.5258 mL 1.0517 mL 2.6292 mL
30 mM 0.0876 mL 0.4382 mL 0.8764 mL 2.1910 mL
40 mM 0.0657 mL 0.3286 mL 0.6573 mL 1.6432 mL
50 mM 0.0526 mL 0.2629 mL 0.5258 mL 1.3146 mL
60 mM 0.0438 mL 0.2191 mL 0.4382 mL 1.0955 mL
80 mM 0.0329 mL 0.1643 mL 0.3286 mL 0.8216 mL
100 mM 0.0263 mL 0.1315 mL 0.2629 mL 0.6573 mL
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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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Inquiry Information

Nombre del producto:
LPA2 antagonist 2
Cat. No.:
HY-113973
Cantidad:
MCE Japan Authorized Agent: