1. GPCR/G Protein
  2. LPL Receptor

LPA1 antagonist 1 

Cat. No.: HY-18076
Handling Instructions

LPA1 antagonist 1 is a highly selective Lysophosphatidic Acid receptor-1 (LPA1) antagonist with an IC50 of 25 nM.

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

LPA1 antagonist 1 Chemical Structure

LPA1 antagonist 1 Chemical Structure

CAS No. : 1396006-71-5

Size Stock
250 mg Get quote
500 mg Get quote

* Please select Quantity before adding items.

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

LPA1 antagonist 1 is a highly selective Lysophosphatidic Acid receptor-1 (LPA1) antagonist with an IC50 of 25 nM.

IC50 & Target

IC50: 25 nM (LPA1)[1].

In Vitro

LPA1 antagonist 1 (compound 2) displays very potent and highly selective inhibitory activity toward LPA1, with little inhibition on LPA3 even at very high concentrations. To our knowledge, LPA1 antagonist 1 is the most selective nonlipid LPA1 antagonist so far reported. It appears that compounds (e.g., LPA1 antagonist 1) from the N-aryltriazole chemical class are much more selective for LPA1 than compounds from the corresponding pyrazole series. In comparison with Ki16425 and AM095, LPA1 antagonist 1 shows much improved antiproliferative activity. LPA1 antagonist 1 demonstrates the highest LPA1 selectivity and attenuated LPA-induced NHLF proliferation and contraction with high potency[1].

In Vivo

Oral dosing of LPA1 antagonist 1 in mice causes a dose-dependent reduction in serum histamine levels induced following intravenous LPA stimulation. When mice are orally dosed with LPA1 antagonist 1 (100 mg/kg, aqueous suspension) prior to intravenous LPA injection, the LPA-induced histamine level is significantly blocked A clear PK/PD relationship is demonstrated by the correlation between the levels of LPA1 antagonist 1 and LPA-induced histamine concentrations in plasma. Although AM095 almost completely blocks histamine release (100 mg/kg), analysis of plasma samples revealed more than 65-fold higher concentrations of AM095 than LPA1 antagonist 1 (100 mg/kg). The ability of LPA1 antagonist 1 to block histamine release at much lower plasma concentration suggests that further improvement of pharmacokinetic properties of this chemical class could lower the effective dose[1].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0724 mL 10.3621 mL 20.7241 mL
5 mM 0.4145 mL 2.0724 mL 4.1448 mL
10 mM 0.2072 mL 1.0362 mL 2.0724 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

482.53

Formula

C₂₈H₂₆N₄O₄

CAS No.

1396006-71-5

SMILES

CC(N=N1)=C(NC(O[[email protected]@H](C2=CC=CC=C2)C)=O)N1C3=CC=C(C4=CC=C(C5(CC5)C(O)=O)C=C4)C=C3

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
LPA1 antagonist 1
Cat. No.:
HY-18076
Quantity:

LPA1 antagonist 1

Cat. No.: HY-18076