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Merck

A2861

Sigma-Aldrich

Astemizole

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

동의어(들):

1-(4-Fluorobenzyl)-2-(1-[4-methoxyphenethyl]piperidin-4-yl)aminobenzimidazole

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크기 선택

제품정보 (DICE 배송 시 비용 별도)

실험식(Hill 표기법):
C28H31FN4O
CAS 번호:
68844-77-9
Molecular Weight:
458.57
EC Number:
272-441-9
MDL number:
MFCD00153919
UNSPSC 코드:
41121800
PubChem Substance ID:
329770802
NACRES:
NA.77

주요 문서

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제품 이름

Astemizole, ≥98% (HPLC)

Quality Level

100

분석

≥98% (HPLC)

양식

powder

저장 조건

desiccated
protect from light

solubility

DMSO: >20 mg/mL

주관자

Johnson & Johnson

저장 온도

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

유전자 정보

human ... HRH1(3269)

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관련 카테고리

생화학적/생리학적 작용

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).

특징 및 장점

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.

픽토그램

Exclamation mark
GHS07

신호어

Warning

유해 및 위험 성명서

H315,H319,H335

Hazard Classifications

Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

표적 기관

Respiratory system

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable

가장 최신 버전 중 하나를 선택하세요:

시험 성적서(COA)

Lot/Batch Number
079K4707V
079K47073
079K47072
079K47071
079K4707

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특정 버전이 필요한 경우 로트 번호나 배치 번호로 특정 인증서를 찾을 수 있습니다.

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문서 라이브러리 방문

M F Nilsson et al.
Reproductive toxicology (Elmsford, N.Y.), 29(2), 156-163 (2010-02-11)
Drugs blocking the potassium current IKr of the heart (via hERG channel-inhibition) have the potential to cause hypoxia-related teratogenic effects. However, this activity may be missed in conventional teratology studies because repeat dosing may cause resorptions. The aim of the
Andrew M Sawayama et al.
Chemistry (Weinheim an der Bergstrasse, Germany), 15(43), 11723-11729 (2009-09-24)
Herein we demonstrate that a small panel of variants of cytochrome P450 BM3 from Bacillus megaterium covers the breadth of reactivity of human P450s by producing 12 of 13 mammalian metabolites for two marketed drugs, verapamil and astemizole, and one
Astemizole. A nonsedating antihistamine with fast and sustained activity.
M M Janssens
Clinical reviews in allergy, 11(1), 35-63 (1993-01-01)
Tjøstil Vlaar et al.
Angewandte Chemie (International ed. in English), 51(52), 13058-13061 (2012-11-20)
O(2) in, H(2)O out: Various diamines and related bisnucleophiles readily undergo oxidative isocyanide insertion with Pd(OAc)(2) (1 mol %) as the catalyst and O(2) as the terminal oxidant to give a diverse array of medicinally relevant N heterocycles. The utility
Chitalu C Musonda et al.
Bioorganic & medicinal chemistry letters, 19(2), 481-484 (2008-12-05)
A dual activity, conjugated approach has been taken to form hybrid molecules of two known antimalarial drugs, chloroquine (CQ) and the non-sedating H1 antagonist astemizole. A variety of linkers were investigated to conjugate the two agents into one molecule. Compounds
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