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LPA1 antagonist 1

Catalog No.GC31958

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

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LPA1 antagonist 1 Chemical Structure

Cas No.: 1396006-71-5

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Sample solution is provided at 25 µL, 10mM.

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Background

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

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].

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].

[1]. Qian Y, et al. Discovery of highly selective and orally active lysophosphatidic acid receptor-1 antagonists with potent activity on human lung fibroblasts. J Med Chem. 2012 Sep 13;55(17):7920-39.

Chemical Properties

Cas No. 1396006-71-5 SDF
Canonical SMILES CC(N=N1)=C(NC(O[C@@H](C2=CC=CC=C2)C)=O)N1C3=CC=C(C4=CC=C(C5(CC5)C(O)=O)C=C4)C=C3
Formula C28H26N4O4 M.Wt 482.53
Solubility Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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
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Average Rating: 5 ★★★★★ (Based on Reviews and 28 reference(s) in Google Scholar.)

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