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Astemizole-d3

CAT: 0804-HY-12532SSize: 10 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-12532SSize:10 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
Astemizole-d3 is the deuterium labeled Astemizole. 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].
CAS Number
1189961-39-4
UNSPSC
12352005
Target
Histamine Receptor; Isotope-Labeled Compounds; Potassium Channel
Related Pathways
GPCR/G Protein; Immunology/Inflammation; Membrane Transporter/Ion Channel; Neuronal Signaling; Others
Field of Research
Inflammation/Immunology; Endocrinology
Purity
97.78
Solubility
10 mM in DMSO
Smiles
[2H]C([2H])([2H])OC(C=C1)=CC=C1CCN(CC2)CCC2NC3=NC4=CC=CC=C4N3CC5=CC=C(C=C5)F
Molecular Formula
C28H28D3FN4O
Molecular Weight
461.59
References & Citations
[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216. |[2]Laduron PM, et al. In vitro and in vivo binding characteristics of a new long-acting histamine H1 antagonist, astemizole. Mol Pharmacol. 1982 Mar;21 (2) :294-300.|[3]Richards DM, et al. Astemizole. A review of its pharmacodynamic properties and therapeutic efficacy. Drugs. 1984 Jul;28 (1) :38-61.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Isotope-Labeled Compounds
Clinical Information
No Development Reported
Isoform
H1 Receptor

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