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SRI-22136

Catalog No. T212989 Copy Product Info
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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.

SRI-22136

Copy Product Info
🥰Excellent
Catalog No. T212989

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.

SRI-22136
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For research use only—not for human use. No sales to individuals. Use as intended only.
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Product Introduction

Bioactivity
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.
Chemical Properties
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent 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.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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