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Aplaviroc hydrochloride is a CCR5 antagonist derived from SDP, with IC50s ranging from 0.1-0.4 nM for HIV-1Ba-L, HIV-1JRFL, and HIV-1MOKW. It is intended for research use only.
Target: CCR5 antagonist
Potency: Potent activity against wild-type R5 HIV-1 strains with IC50 values of 0.1 to 0.4 nM
Mechanism: Suppresses infectivity and replication of HIV-1MDR variants at low concentrations (IC50 values of 0.4 to 0.6 nM)
Binding Affinity: Binds to CCR5 with high affinity (Kd value of 2.9±1.0 nM)
Inhibition: Potently blocks rgp120/sCD4 binding to CCR5 with an IC50 value of 2.7 nM
In Vivo Efficacy: Suppresses R5 HIV-1 viremia in hu-PBMC-NOG mice at a dosage of 60 mg/kg
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Clorgyline hydrochloride is an irreversible and selective inhibitor of monoamine oxidase A (MAO-A) used in scientific research. It has minimal effect on conjugated dopamine (DA) amounts in superfusates of rat striatum slices. This compound contains an Alkyne group, enabling it to undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Irreversible and selective inhibitor of monoamine oxidase A (MAO-A)
Structurally related to Pargyline
Contains an Alkyne group for copper-catalyzed azide-alkyne cycloaddition (CuAAc) with Azide groups
Increases nicotine infusions and motivation to obtain nicotine in rats at 2 mg/kg daily for 28 days
Pretreatment with 1 mg/kg intravenously for 1 hour has little effect on the efflux of conjugated dopamine (DA) and p-tyramine-evoked release of conjugated DA from slices of rat striatum
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SB-277011 hydrochloride is a potent and selective dopamine D3 receptor (D3R) antagonist, demonstrating high oral bioavailability and brain penetrance. It exhibits significant selectivity over other dopamine receptors and possesses an excellent pharmacokinetic profile in rats. This compound has been shown to effectively reverse the effects of quinelorane and reduce cocaine self-administration in preclinical studies.
Potent and selective D3 receptor antagonist
High oral bioavailability and brain penetrance
80- to 100-fold selectivity over other dopamine receptors
Excellent pharmacokinetic profile
Reverses quinelorane effects in nucleus accumbens
Reduces intravenous cocaine self-administration
Inhibits basal and cocaine-enhanced locomotion
Appearance: solid, off-white to light yellow
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Octodrine hydrochloride is a central nervous activator that functions by increasing the uptake of dopamine and noradrenaline. It has been observed to increase pain threshold, cardiac rate, and myocardial contractility.
Increases dopamine and noradrenaline uptake
Increases pain threshold
Positive chronotropic effect on cardiac rate
Positive inotropic effect on myocardial contractility
For research use only
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SRI-37330 hydrochloride is an orally bioavailable thioredoxin-interacting protein (TXNIP) inhibitor. It inhibits glucagon secretion and function, reduces hepatic glucose production, and reverses hepatic steatosis. It can be used for type 2 diabetes research.
Inhibits activity of human TXNIP promoter in INS-1 cells.
Inhibits mRNA and protein levels of TXNIP.
Inhibits polymerase II (Pol II) binding to the E-box motif region of the TXNIP promoter.
Lowers glucagon secretion in TC1-6 cells.
Inhibits glucagon-induced glucose output from primary hepatocytes.
Decreases glucagon secretion and blocks hepatic glucose output in mice.
Reverses obesity- and STZ-induced diabetes and hepatic steatosis in mice.
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