Abcam, ab144583, Astemizole, histamine H1 receptor antagonist and hERG K+ channel blocker

Size: 10mg / 50mg
MW 458.6 Da, Purity >99%. Potent, selective histamine H1 receptor antagonist (IC50 = 4 nM) and potent hERG K+ channel blocker (IC50 =0.9 nM). Orally active. Antiallergic agent. Active *in vivo* and *in vitro*.
Key facts
CAS number:68844-77-9,
Purity:>99%,
Form:SolidSee storage information,
Molecular weight:458.6 Da,
Molecular formula:C28H31FN4O,
PubChem:2247,
Nature:Synthetic,
Solubility:Soluble in DMSO to 50 mMSoluble in ethanol to 50 mM,
Biochemical name:Astemizole,
Biological description:Potent, selective histamine H1 receptor antagonist (IC50 = 4 nM) and potent hERG K+ channel blocker (IC50 =0.9 nM). Orally active. Antiallergic agent. Active *in vivo* and *in vitro*.,
Canonical smiles:COC1=CC=C(C=C1)CCN2CCC(CC2)NC3=NC4=CC=CC=C4N3CC5=CC=C(C=C5)F,
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),
InChiKey:GXDALQBWZGODGZ-UHFFFAOYSA-N,
IUPAC Name:1-[(4-fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]piperidin-4-yl]benzimidazol-2-amine

Properties and Storage Information:
Shipped at conditions-Ambient - Can Ship with Ice, Appropriate short-term storage conditions-Ambient, Appropriate long-term storage conditions-Ambient, Storage information-The product can be stored for up to 12 months

Supplementary Information:
This supplementary information is collated from multiple sources and compiled automatically.
The Sigma1-receptor is a protein with a molecular weight of approximately 25 kDa. This receptor found in the endoplasmic reticulum exhibits widespread expression in several tissues including the central nervous system and heart. The Sigma1-receptor does not resemble classic opioid receptors and displays unique binding characteristics. Its roles involve mediating signal transduction through physical interaction with other proteins.
Biological function summary
The Sigma1-receptor influences neurotransmitter release cellular survival and neuroplasticity. It acts as a chaperone protein interacting with ion channels and receptors to modulate their activity. The receptor forms dynamic complexes with various cellular components impacting calcium signaling and neuronal adaptation processes. It is also involved in regulating cellular stress responses.
Pathways
The Sigma1-receptor plays a significant role in the cellular stress response and calcium signaling pathways. It interacts closely with proteins such as the NMDA receptor and IP3 receptor within these pathways affecting intracellular calcium levels and cell survival. Through these interactions the Sigma1-receptor modulates synaptic plasticity and neuroprotection important in signal transduction processes.
The Sigma1-receptor has been associated with neurodegenerative diseases like Alzheimer's disease and psychiatric disorders such as depression. Its modulation of calcium homeostasis and cellular stress is critical in these conditions. Disorders related to NMDA receptor dysfunction often implicate the Sigma1-receptor highlighting its therapeutic potential in managing synaptic and neuroprotective processes.