CAS No. 171714-84-4

Batch: Purity:98.69
Lu-135252 Chemical Structure
Chemical Structure
Check the Lu-135252 product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Chemical Information

CAS Number 171714-84-4
Molecular Formula

C22H22N2O6

Molecular Weight (MW) 410.42
SMILES COC1=CC(=NC(=N1)OC(C(=O)O)C(C2=CC=CC=C2)(C3=CC=CC=C3)OC)OC

Ordering Information

Biological Activity

Lu-135252 (Darusentan) is a selective endothelin A receptor antagonist. By binding to endothelin A receptors, Lu-135252 inhibits endothelin-1-driven intracellular calcium mobilization, phospholipase C activation, and downstream ERK/MAPK signaling pathways. This targeted receptor inhibition effectively suppresses vascular smooth muscle cell contraction, cellular proliferation, and hypertrophic responses, thereby blunting endothelin-1-mediated vasoconstriction and structural cell remodeling. [1]

How to Prepare Stock Solution?

Concentration Volume Mass
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Solubility

Batch:
All in vitro solubility values are batch-tested experimental data (non-literature values).
Solvent Solubility & Note
DMSO 82 mg/mL (199.79 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO. The recommended stock concentration is 10 mM in DMSO.)
Ethanol 21 mg/mL
Water Insoluble
FAQ
Q: Why does a DMSO stock precipitate in media/saline?
A: It is caused by unheated aqueous media (supersaturation), local solvent shock, or incorrect mixing sequence.
How to fix it?
  • Preheat media/saline to 37°C.
  • Mix rapidly (pipette/vortex) upon addition.
  • For complex mixes, always add the aqueous phase last.
  • Re-dissolve minor precipitates with a 37°C water bath and sonication (≤30 min).
Note: Technical data last updated: Sep 1, 2026.