GLPG2938 is a potent and selective S1P2 antagonist.GLPG2938 can be used in the study of idiopathic pulmonary fibrosis (IPF).
|Solubility (25°C)||DMSO ≥ 60 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
 Oscar Mammoliti, et al. J Med Chem. Discovery of the S1P2 Antagonist GLPG2938 (1-[2-Ethoxy-6-(trifluoromethyl)-4-pyridyl]-3-[[5-methyl-6-[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]pyridazin-3-yl]methyl]urea), a Preclinical Candidate for the Treatment of Idiopathic Pulmonary Fibrosis
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Sonepcizumab (LT 1009) is a fully humanized anti-S1P monoclonal antibody. Sonepcizumab has the potential for the research of metastatic renal cell carcinoma (mRCC).
|TC LPA5 4
TC LPA5 4 is a specific non-lipid LPA5 (GPR92) antagonist (IC50=0.8 μM in LPA5-RH7777 cells). Shows selectivity for LPA5 against 80 other screening targets.TC LPA5 4 was shown to inhibit LPA-induced aggregation of isolated human platelets.TC LPA5 4 inhibits proliferation and migration of thyroid cancer cells.
BMS-986278 is a potent LPA1 antagonist with a Kb of 6.9 nM.
The S1P1 agonist SAR247799 is a biased agonist of the S1P1 sphingosine receptor, preferentially activating G protein signaling over the β-arrestin and internalization pathways.
|LPA2 antagonist 1
LPA2 antagonist 1 is a LPA2 antagonist with an IC50 of 17 nM.
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