Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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A133983-10mg | 10mg | In stock | $68.90 | |
A133983-50mg | 50mg | In stock | $162.90 | |
A133983-250mg | 250mg | In stock | $733.90 |
Potent, selective histamine H1 receptor antagonist and potent hERG K + channel blocker
Synonyms | astemizole|68844-77-9|Hismanal|Histaminos|Paralergin|Laridal|Retolen|Astemison|Histamen|Kelp|Astemizol|Astemizolum|1-[(4-Fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]-4-piperidinyl]-1H-benzimidazol-2-amine|1-(p-Fluorobenzyl)-2-((1-(p-methoxypheneth |
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Specifications & Purity | ≥98% |
Storage Temp | Store at 2-8°C,Protected from light |
Shipped In | Wet ice |
Grade | Moligand™ |
Action Type | ANTAGONIST, CHANNEL BLOCKER |
Mechanism of action | Histamine H1 receptor antagonist |
ALogP | 6 |
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IUPAC Name | 1-[(4-fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]piperidin-4-yl]benzimidazol-2-amine |
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INCHI | 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 |
Canonical SMILES | COC1=CC=C(C=C1)CCN2CCC(CC2)NC3=NC4=CC=CC=C4N3CC5=CC=C(C=C5)F |
Isomeric SMILES | COC1=CC=C(C=C1)CCN2CCC(CC2)NC3=NC4=CC=CC=C4N3CC5=CC=C(C=C5)F |
WGK Germany | 3 |
RTECS | DD8968000 |
PubChem CID | 2247 |
Molecular Weight | 458.57 |
PubChem CID | 2247 |
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DrugBank Ligand | DB00637 |
CAS Registry No. | 68844-77-9 |
ChEBI | CHEBI:2896 |
ChEMBL Ligand | CHEMBL296419 |
BindingDB Ligand | 24226 |
Wikipedia | Astemizole |
RCSB PDB Ligand | XB7 |
DrugCentral Ligand | 249 |
GPCRdb Ligand | astemizole |
Enter Lot Number to search for COA:
To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section
Lot Number | Certificate Type | Date | Item |
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E2007147 | Certificate of Analysis | Dec 11, 2023 | A133983 |
K2120174 | Certificate of Analysis | Sep 15, 2023 | A133983 |
K2120178 | Certificate of Analysis | Sep 15, 2023 | A133983 |
K2120180 | Certificate of Analysis | Sep 15, 2023 | A133983 |
E2310423 | Certificate of Analysis | Dec 02, 2022 | A133983 |
E2310427 | Certificate of Analysis | Dec 02, 2022 | A133983 |
E2310434 | Certificate of Analysis | Dec 02, 2022 | A133983 |
E2310435 | Certificate of Analysis | Dec 02, 2022 | A133983 |
E2310436 | Certificate of Analysis | Dec 02, 2022 | A133983 |
E2310437 | Certificate of Analysis | Dec 02, 2022 | A133983 |
Solubility | It is soluble in DMSO (25 mg/ml ), ethanol (25 mg/ml), chloroform, methanol, and water (partly miscible). |
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Sensitivity | light sensitive |
Pictogram(s) | GHS07 |
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Signal | Warning |
Hazard Statements | H315:Causes skin irritation H319:Causes serious eye irritation H335:May cause respiratory irritation |
Precautionary Statements | P261:Avoid breathing dust/fume/gas/mist/vapors/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing. P280:Wear protective gloves/protective clothing/eye protection/face protection. P302+P352:IF ON SKIN: wash with plenty of water. P321:Specific treatment (see ... on this label). P405:Store locked up. P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P271:Use only outdoors or in a well-ventilated area. P304+P340:IF INHALED: Remove person to fresh air and keep comfortable for breathing. P403+P233:Store in a well-ventilated place. Keep container tightly closed. P362+P364:Take off contaminated clothing and wash it before reuse. P264+P265:Wash hands [and …] thoroughly after handling. Do not touch eyes. P337+P317:If eye irritation persists: Get medical help. P332+P317:If skin irritation occurs: Get medical help. P319:Get medical help if you feel unwell. |
WGK Germany | 3 |
RTECS | DD8968000 |
1. Zhou Z, Vorperian VR, Gong Q, Zhang S, January CT. (1999) Block of HERG potassium channels by the antihistamine astemizole and its metabolites desmethylastemizole and norastemizole.. J Cardiovasc Electrophysiol, 10 (6): (836-43). [PMID:10376921] |
2. Cao Q, Wang X, Zhao M, Yang R, Malik R, Qiao Y, Poliakov A, Yocum AK, Li Y, Chen W et al.. (2014) The central role of EED in the orchestration of polycomb group complexes.. Nat Commun, 5 (3): (3127). [PMID:24457600] |
3. Kong X, Chen L, Jiao L, Jiang X, Lian F, Lu J, Zhu K, Du D, Liu J, Ding H et al.. (2014) Astemizole arrests the proliferation of cancer cells by disrupting the EZH2-EED interaction of polycomb repressive complex 2.. J Med Chem, 57 (22): (9512-21). [PMID:25369470] |
4. Zhang KL et al.. (2019) AZD9291 inactivates the PRC2 complex to mediate tumor growth inhibition.. Acta Pharmacol Sin, 40 (12): (1587-1595). [PMID:31171828] |