A2861

Astemizole

≥98% (HPLC), hERG potassium channel blocker, powder

• Synonym(s): 1-(4-Fluorobenzyl)-2-(1-[4-methoxyphenethyl]piperidin-4-yl)aminobenzimidazole
• Empirical Formula (Hill Notation): C₂₈H₃₁FN₄O
• CAS Number: 68844-77-9
• Molecular Weight: 458.57
• NACRES: NA.77
• PubChem Substance ID: 329770802
• UNSPSC Code: 41121800
• EC Number: 272-441-9
• MDL number: MFCD00153919
• Assay: ≥98% (HPLC)
• Form: powder
• Storage condition: desiccated, protect from light

Properties

• Product Name: Astemizole, ≥98% (HPLC)
• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• storage condition: desiccated, protect from light
• solubility: DMSO: >20 mg/mL
• originator: Johnson & Johnson
• storage temp.: 2-8°C
• SMILES string: COc1ccc(CCN2CCC(CC2)Nc3nc4ccccc4n3Cc5ccc(F)cc5)cc1
• InChI: 1S/C28H31FN4O/c1-34-25-12-8-21(9-13-25)14-17-32-18-15-24(16-19-32)30-28-31-26-4-2-3-5-27(26)33(28)20-22-6-10-23(29)11-7-22/h2-13,24H,14-20H2,1H3,(H,30,31)
• InChI key: GXDALQBWZGODGZ-UHFFFAOYSA-N
• Gene Information: human ... HRH1(3269)

Description

Biochem/physiol Actions

Astermizole is a potent hERG potassium channel blocker (IC₅₀ of 0.9 nM) and may used as a pharmacological chaperone to correct folding defects and restore protein function for some mutated forms of hERG channels. It has also been studied for treatment of malaria, hERG and hEAG channel function in cancer and as a second generation antihistamine H-1 antagonist.

Astermizole is a potent hERG potassium channel blocker (IC₅₀ of 0.9 nM).

Features and Benefits

This compound is featured on the Potassium Channels page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

This compound was developed by Johnson & Johnson. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Safety Information

• pictograms: GHS07
• signalword: Warning
• hcodes: H315,H319,H335
• pcodes: P261 - P264 - P271 - P280 - P302 + P352 - P305 + P351 + P338
• Hazard Classifications: Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
• target_organs: Respiratory system
• Storage Class: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable