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L-654284

CAT: 0931-T201031-01Size: 100 mgDry Ice: NoHazardous: No
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CAT#:0931-T201031-01Size:100 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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CAS Number
98719-20-1
Target
Adrenergic Receptor, Others
Related Pathways
Neuroscience, GPCR/G Protein, Others
Bioactivity
L-654284 is an α2-adrenergic receptor antagonist characterized by its notable selectivity. It competes with 3H-clonidine and 3H-rauwolscine for binding in vitro, exhibiting Ki values of 0.8 nM and 1.1 nM, respectively. L-654284 effectively blocks the pre-ejaculatory effects of clonidine in isolated rat vas deferens, with a pA2 value of 9.1. The compound demonstrates significant selectivity for α2 over α1 adrenergic receptors, with a Ki value of 110 nM against 3H-prazosin binding. In vivo, L-654284 significantly increases the turnover of norepinephrine in the rat cerebral cortex, indicating its activity in blocking α2-adrenergic receptors within the central nervous system.
Smiles
N(S(CCO)(=O)=O)(C)[C@H]1C[C@]2(C3=C(C=4C(O3)=CC=CC4)CCN2CC1)[H]
Molecular Formula
C18H24N2O4S
Molecular Weight
364.46
Shipping Conditions
Ice Packs
Storage Temperature
-20°C