Astemizole (Hismanal) tritiated at the O-methyl group. Atemizole is an antagonist of the histamine H1-receptor and has been shown to block hERG potassium channels.
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Astemizole is an anithistamine drug that binds to the histmaine H1 receptor and suppresses edema and pruritus. Histamine H1 receptors are a group of GPCRs expressed in smooth muscle, vascular endothelial cells, and the central nervous system.
We offer both agonist and antagonist radioligands for autoradiographic visualization or performing saturation and competition assays to determine receptor expression levels (Bmax), dissociation constants (Kd), association and dissociation rates (kon and koff), and inhibitor constants (Ki) for a variety of receptors. We develop our radioligands to the highest specific activity possible and provide high purity resulting in low non-specific binding products. Each of our ultra-pure radioligands is fully characterized for pharmacological action and validated in receptor binding assays.
Radiolabeled ligands remain the most sensitive method for probing receptor binding biology; yielding unprecedented sensitivity gives results that technicians and scientists can trust. For over 50 years, PerkinElmer has been a leading supplier of New England Nuclear (NEN) radiochemicals, liquid scintillation cocktails, vials and nuclear counting detection instruments.
|Concentration||1.0 - 10 mCi/mL|
|Fresh Lot Days||2nd Monday in April and October|
|Label Position||Specifically Labeled|
|Product Brand Name||NEN Radiochemicals|
|Shipping Condition||Dry Ice|
|Special Ordering Information||This is a radioactive product - shipping address must have a license to receive radioactive materials.|
|Therapeutic Area||Cardiovascular, Cancer|
|Unit Size||250 µCi|
Astemizole is known to be a potent blocker of the hERG (human ether-a-go-go-related gene) potassium ion channel. Astemizole, [O-Methyl-3H]- was developed as a radioligand for the hERG K+ channel binding assay. The radioligand binding assay of the hERG channel is used to identify compounds which may have potential cardiotoxicity.