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astemizole - ≥98%, high purity , Histamine H1 receptor antagonist, CAS No.68844-77-9, Histamine H1 receptor antagonist

  • Moligand™
  • ≥98%
Item Number
A133983
Grouped product items
SKUSizeAvailabilityPrice Qty
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

Basic Description

Synonymsastemizole|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
Specifications & Purity≥98%
Storage TempStore at 2-8°C,Protected from light
Shipped InWet ice
GradeMoligand™
Action TypeANTAGONIST, CHANNEL BLOCKER
Mechanism of actionHistamine H1 receptor antagonist

Product Properties

ALogP6

Associated Targets

ABCB1 Tchem Multidrug resistance protein 1 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HRH1 Tclin Histamine H1 receptor 5 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

SLC6A3 Tclin Sodium-dependent dopamine transporter 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

SLC6A4 Tclin Sodium-dependent serotonin transporter 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TMEM97 Tchem Sigma intracellular receptor 2 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

SIGMAR1 Tclin Sigma non-opioid intracellular receptor 1 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HTR2A Tclin 5-hydroxytryptamine receptor 2A 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HTR2C Tclin 5-hydroxytryptamine receptor 2C 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HTR2B Tclin 5-hydroxytryptamine receptor 2B 2 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

KCNH1 Tclin Potassium voltage-gated channel subfamily H member 1 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GLRA1 Tclin Glycine receptor subunit alpha-1 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 27 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name 1-[(4-fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]piperidin-4-yl]benzimidazol-2-amine
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

Certificates

Certificate of Analysis(COA)

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

10 results found

Lot NumberCertificate TypeDateItem
E2007147Certificate of AnalysisDec 11, 2023 A133983
K2120174Certificate of AnalysisSep 15, 2023 A133983
K2120178Certificate of AnalysisSep 15, 2023 A133983
K2120180Certificate of AnalysisSep 15, 2023 A133983
E2310423Certificate of AnalysisDec 02, 2022 A133983
E2310427Certificate of AnalysisDec 02, 2022 A133983
E2310434Certificate of AnalysisDec 02, 2022 A133983
E2310435Certificate of AnalysisDec 02, 2022 A133983
E2310436Certificate of AnalysisDec 02, 2022 A133983
E2310437Certificate of AnalysisDec 02, 2022 A133983

Chemical and Physical Properties

SolubilityIt is soluble in DMSO (25 mg/ml ), ethanol (25 mg/ml), chloroform, methanol, and water (partly miscible).
Sensitivitylight sensitive

Safety and Hazards(GHS)

Pictogram(s) GHS07
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

Related Documents

References

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,  (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]

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