A2861

Astemizole

≥98% (HPLC)

• 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
• EC Number: 272-441-9
• MDL number: MFCD00153919
• UNSPSC Code: 41121800
• PubChem Substance ID: 329770802
• NACRES: NA.77

Properties

• Quality Level: 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.

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
• Signal Word: Warning
• Hazard Statements: H315,H319,H335
• Precautionary Statements: 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 Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable