Siramesine(Lu 28-179) is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo. Siramesine can induce cell death in transformed cells through a mechanism including lysosomal destabilization.
In vivo, siramesine treatment of mice caused a depletion of the MC populations of the peritoneum and skin.
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Related Sigma Receptor Products|
AB10 is a selective S1R antagonist.
WLB-89462 is a selective σ2 receptor ligand (Ki: 13 nM).
Siramesine (Lu 28-179) fumarate is a potent sigma-2 receptor agonist.
|Sigma-1 receptor antagonist 5
Sigma-1 receptor antagonist 5 and histamine H3 (hH3R, Ki=7.7 nM, IC50=215 nM).
AB21 is a potent and selective S1R antagonist with Kis of 13, 102 nM for S1R and S2R.
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