A-803467

SKU: orb1223559

Description

A-803467 is a selective NaV1.8 channel blocker with IC50 of 8 nM, blocks tetrodotoxin-resistant currents, exhibits >100-fold selectivity against human NaV1.2, NaV1.3, NaV1.5, and NaV1.7.

Key Properties

• CAS Number: 944261-79-4
• MW: 357.79
• Purity: >98% (HPLC)
• Formula: C₁₉H₁₆ClNO₄
• SMILES: O=C(C1=CC=C(C2=CC=C(Cl)C=C2)O1)NC3=CC(OC)=CC(OC)=C3
• Target: Sodium Channel
• Solubility: Ethanol: 11 mg/mL (30.74 mM); DMSO: 72 mg/mL (201.23 mM)

Bioactivity

• In Vivo:
  A-803467 (35 mg/kg; p.o.) shows no noticeable toxicity in the male NCR nude mice. A-803467 in combination with topotecan, significantly decreases the tumor growth in mice implanted with ABCG2 overexpressing H460/MX20 cells. A-803467 effectively restores the sensitivity of tumors overexpressing ABCG2 transporter to topotecan without having any significant effect on tumors lacking ABCG2 expression. Animal model: Nude mice. Dosage: 35 mg/kg. Administration: p.o. Result: Showed no noticeable toxicity in the male NCR nude mice.
• In Vitro:
  A-803467 selectively and significantly reverses the ABCG2-mediated multidrug resistance. A-803467 (7.5 μM) significantly increases the cytotoxicity of mitoxantrone and topotecan in ABCG2-transfected cell lines. A-803467 (7.5 μM) significantly enhanced theintracellular [3H]-MX accumulation in ABCG2-transfected cells. A-803467 (7.5 μM; 0~120 minutes) significantly blocks the intracellular [3H]-MX efflux at different time periods from ABCG2-transfected cells. A-803467 stimulates the ATPase activity of ABCG2.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

A-803467 | A 803467 | A803467

Quick Database Links

Gene Symbol

Sodium Channel