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SRI-22136 is a Delta opioid receptor (DOR) antagonist that can cross the blood-brain barrier with an IC50 of 0.42 nM. It lacks agonistic activity on DOR, MOR, and KOR, functioning solely as an antagonist with IC50 values of 370 nM for MOR and 54 nM for KOR, thereby avoiding addiction/aversion effects. SRI-22136 effectively inhibits DADLE (a DOR agonist)-induced BACE1 activity with an IC50 of 120 nM. It can completely prevent Alzheimer’s disease-like pathology in mouse models and is applicable for Alzheimer's research.
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| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| Description | SRI-22136 is a Delta opioid receptor (DOR) antagonist that can cross the blood-brain barrier with an IC50 of 0.42 nM. It lacks agonistic activity on DOR, MOR, and KOR, functioning solely as an antagonist with IC50 values of 370 nM for MOR and 54 nM for KOR, thereby avoiding addiction/aversion effects. SRI-22136 effectively inhibits DADLE (a DOR agonist)-induced BACE1 activity with an IC50 of 120 nM. It can completely prevent Alzheimer’s disease-like pathology in mouse models and is applicable for Alzheimer's research. |
| Targets&IC50 | δ opioid receptor:0.42 nM |
| In vivo | SRI-22136 (Compound 12) effectively blocked DPDPE-induced antinociception, achieving full antagonism at doses of 1 and 10 mg/kg, and partial effects at 0.1 and 0.32 mg/kg, demonstrating systemic stability and blood-brain barrier penetration. Administered subcutaneously at 1 mg/kg twice daily for 90 days, SRI-22136 completely prevented Alzheimer's-like pathology in mice, including memory deficits, β-secretase activity, Aβ1-42 accumulation, and markers of brain inflammation. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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