RO1138452

SKU: orb1302861

Description

CAY10441 is a potent, selective, and orally active prostacyclin (IP) receptor antagonist with a pKi of 8.3. It effectively blocks IP receptor-mediated cAMP accumulation in vitro and demonstrates significant in vivo analgesic activity in rat models at doses of 2-20 mg/kg, making it a valuable research tool for studying pain and vascular biology.

Research Area

Immunology & Inflammation, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 221529-58-4
• MW: 309.41
• Purity: 99.34% (May vary between batches)
• Formula: C₁₉H₂₃N₃O
• SMILES: CC(C)Oc1ccc(Cc2ccc(NC3=NCCN3)cc2)cc1
• Target: Prostaglandin Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.46 mM);DMSO:45 mg/mL (145.44 mM)

Bioactivity

• Target IC50:
  5-HT2A receptor (rat):5.71 (pKi)|5-HT2A receptor (rat):3040 nM|5-HT2C (porcine):6.11 (pKi)|5-HT2C (porcine):1190 nM|5-HT1B receptor (rat):6.11 (pKi)|5-HT1B receptor (rat):1130 nM|I2R (rat):8.33 (pKi)|I2R (rat):7 nM|Muscarinic M1 receptor (human):2570 nM|Muscarinic M1 receptor (human):5.66 (pKi)|PAF Receptor (rabbit):52.9 nM|PAF Receptor (rabbit):7.9 (pKi)|Muscarinic M2 receptor (human):2220 nM|Muscarinic M2 receptor (human):5.88 (pKi)|Muscarinic M4 receptor (human):1450 nM|Muscarinic M4 receptor (human):6.14 (pKi)|5-HT1A receptor (human):5.37 (pKi)|5-HT1A receptor (human):8580 nM|5-HT4 receptor (guinea pig):5.35 (pKi)|5-HT4 receptor (guinea pig):8910 nM|α2A-adrenoceptor (human):6.49 (pKi)|α2A-adrenoceptor (human):724 nM|α1B-adrenoceptor (rat):5.87 (pKi)|α1B-adrenoceptor (rat):3280 nM|Muscarinic M5 receptor (human):5.81 (pKi)|Muscarinic M5 receptor (human):3110 nM

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

prostacyclin receptor, Prostaglandin Receptor, ProstaglandinReceptor, RO1138452, RO-1138452, RO 1138452, CAY10441, CAY-10441, CAY 10441, inhibit, Inhibitor

Compound Identifiers

PubChem CID

9839644