1. GPCR/G Protein
    Neuronal Signaling
    Immunology/Inflammation
    Membrane Transporter/Ion Channel
  2. Histamine Receptor
    Potassium Channel
  3. Astemizole

Astemizole  (Synonyms: R 43512)

Cat. No.: HY-12532 Purity: 99.62%
COA Handling Instructions

Astemizole (R 43512), a second-generation antihistamine drug to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC50 of 4 nM. Astemizole also shows potent hERG K+ channel blocking activity with an IC50 of 0.9 nM. Astemizole has antipruritic effects.

For research use only. We do not sell to patients.

Astemizole Chemical Structure

Astemizole Chemical Structure

CAS No. : 68844-77-9

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10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
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Based on 2 publication(s) in Google Scholar

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Description

Astemizole (R 43512), a second-generation antihistamine drug to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC50 of 4 nM. Astemizole also shows potent hERG K+ channel blocking activity with an IC50 of 0.9 nM. Astemizole has antipruritic effects[1][2].

In Vivo

Astemizole (p.o., 10 and 30 mg/kg) and (i.v., 1 and 3 mg/kg) has no effect on respiratory rate, heart rate and blood pressure, and even at high doses of 30 mg/kg and 3 mg/kg, also has no effect on body temperature and exercise capacity in male common marmosets. But Astemizole can prolong the QT interval and induce premature ventricular contractions at 30 mg/kg (po) and 1 mg/kg (iv)[3].
Astemizole (p.o., 3 and 30 mg/kg) shows that the pre-drug control values (C) of the idioventricular rate, QT interval and QTcF are 31 beats/min, 319 ms and 256 at dose of 3 mg/kg, while those are 31 beats/min, 331 ms and 270 at dose of 30 mg/kg, respectively in mice. Moreover, Astemizole at a dose of 30 mg/kg (po) may cause tip-twisting ventricular tachycardia by inhibiting hERG K+ channels[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

458.57

Formula

C28H31FN4O

CAS No.
SMILES

COC1=CC=C(CCN2CCC(NC3=NC4=CC=CC=C4N3CC5=CC=C(F)C=C5)CC2)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (272.59 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1807 mL 10.9035 mL 21.8069 mL
5 mM 0.4361 mL 2.1807 mL 4.3614 mL
10 mM 0.2181 mL 1.0903 mL 2.1807 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 6.25 mg/mL (13.63 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 6.25 mg/mL (13.63 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.62%

References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Astemizole
Cat. No.:
HY-12532
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