Encequidar mesylate

SKU: orb1309569

Description

Encequidar mesylate

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 849675-87-2
• MW: 784.83
• Purity: 99.84%
• Formula: C₃₉H₄₀N₆O₁₀S
• SMILES: CS(O)(=O)=O.COc1cc2CCN(CCc3ccc(cc3)-n3nnc(n3)-c3cc(OC)c(OC)cc3NC(=O)c3cc(=O)c4ccccc4o3)Cc2cc1OC
• Target: P-gp
• Solubility: DMSO:55 mg/mL (70.08 mM)

Bioactivity

• In Vivo:
  When administered simultaneously, Encequidar demonstrates increased plasma concentrations with the microcapsule formulation compared to the powder, showing notable differences from 1 to 2 hours. The microcapsule formulation achieves a 1.7-fold quicker Tmax and a 1.6-fold greater AUC value than the powder (2.5±0.6 vs. 4.3±0.9 hours; 107.7±20.1 vs. 64.3±18.0 h ng/mL), indicating faster and more efficient absorption. This enhanced absorption of Encequidar in microcapsule format is likely attributed to its improved aqueous solubility and dissolution rates, facilitated by the conversion from crystalline to amorphous form and the reduction in particle size .
• In Vitro:
  Administration of Encequidar at concentrations of 0.1 or 1 nM resulted in a reduction of cell survival by 20% and 42% upon exposure to 100 nM and 1000 nM of NSC 125973, respectively .

Storage & Handling

• Storage: 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

Encequidar, Encequidar Mesylate, Encequidar mesylate, Inhibitor, HM 30181, HM 30181 Mesylate, HM30181, HM-30181, HM30181 Mesylate, HM30181 mesylate, HM-30181 Mesylate, HM30181A, HM30181A Mesylate, HM30181A mesylate, MDR1, Multidrug resistance protein 1, inhibit, ABCB1, Cluster of differentiation 243, CD243, P-glycoprotein, P-gp (P-glycoprotein), P-gp, Pgp

Compound Identifiers

PubChem CID

76971350