Camlipixant

SKU: orb1741375

Description

Camlipixant (BLU-5937) is a potent, selective, and competitive oral P2X3 receptor antagonist with an IC50 of 25 nM for the human P2X3 homotrimer. It is a research tool for investigating chronic cough mechanisms and has demonstrated antitussive efficacy in clinical studies for refractory chronic cough.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1621164-74-6
• MW: 458.46
• Purity: 97.06% (May vary between batches)
• Formula: C₂₃H₂₄F₂N₄O₄
• SMILES: C(C1=C(N=C2N1C=CC(C)=C2)C3=C(F)C=C(C(NC)=O)C=C3F)[C@H]4CN(C(OC)=O)CCO4
• Target: P2X Receptor
• Solubility: DMSO:22.5 mg/mL (49.08 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.36 mM)

Bioactivity

• Target IC50:
  P2X2/3 (guinea pig):3450 nM|P2X3 (human):25 nM|P2X3 (rat):92 nM|P2X2/3 (rat):1820 nM|P2X3 (guinea pig):126 nM
• In Vivo:
  Camlipixant (BLU-5937 ; 3-30 mg/kg ; oral) reduces histamine and ATP-induced cough sensitization in guinea pigs. Camlipixant (BLU-5937 ; 10-20 mg/kg ; i.p.) did not alter taste perception compared to control animals. Camlipixant (BLU-5937) exhibits excellent drug-like properties, including good oral bioavailability, low predicted clearance in humans, no blood-brain barrier permeability, and high safety.
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• In Vitro:
  Camlipixant (BLU-5937 ; 500 nM) blocks ATP-mediated sensitization of dorsal root ganglion (DRG) neurons.

Storage & Handling

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

Alternative Names

BLU 5937, BLU5937, BLU-5937, Camlipixant, P2XReceptor, P2X3, P2X Receptor

Compound Identifiers

PubChem CID

76955630