CRT0273750

SKU: orb1304527

Description

CRT0273750 is a potent autotaxin (ATX) inhibitor with an IC50 of 14 nM, effectively modulating lysophosphatidic acid (LPA) levels. This small molecule is a valuable research tool for investigating the ATX-LPA axis in oncology, fibrosis, and inflammation, suitable for both in vitro biochemical assays and in vivo pharmacological studies.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1979939-16-6
• MW: 502.92
• Purity: 99.91% (May vary between batches)
• Formula: C₂₅H₂₂ClF₃N₄O₂
• SMILES: C[C@H](NC(=O)CCc1nc2cccnc2n1Cc1ccc(OC(F)(F)F)cc1)c1ccc(Cl)cc1
• Target: PDE,LPL Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween-80+45% Saline:3.3 mg/mL (6.56 mM);DMSO:200 mg/mL (397.68 mM)

Bioactivity

• Target IC50:
  ATX:0.014 μM
• In Vivo:
  CRT0273750 treatment shows the Cmax, AUC and t1/2 values of 3.8 μM, 3.2 μM.h and 1.4 h, respectively and shows a proportional increase.CRT0273750 has a moderate blood clearance, with value of 41 mL/min/kg.
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• In Vitro:
  CRT0273750 is also shown to inhibit the migration of 4T1 cells with an EC50 of 0.025μM. CRT0273750 shows high potency in both the biochemical (IC50 = 0.01 μM) and plasma choline release assay(IC50 = 0.014 μM).
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CRT 0273750, CRT-0273750, CRT0273750, clearance, blood, ATX (autotaxin), ATX/LPA, 4T1, LPA, inhibit, Inhibitor

Compound Identifiers

PubChem CID

122199235