SRI-22136
SRI-22136 is a Delta Opioid Receptor (DOR) antagonist that can cross blood-brain barrier with a IC50 of 0.42 nM. SRI-22136 does not have agonistic activity but antagonistic activity against DOR, MOR (IC50 = 370 nM), KOR (IC50 = 54 nM) and can avoid addiction/aversion effects. SRI-22136 can effectively inhibit the BACE1 activity induced by DADLE (a DOR agonist) (HY-105343) (IC50 = 120 nM). SRI-22136 prevents completely Alzheimer’s-like pathology in mouse model. SRI-22136 can used for the study of Alzheimer’s disease.
For research use only. We do not sell to patients.
- Formula: C30H29ClN2O3
- Molecular Weight:501.02
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Opioid Receptor Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
δ Opioid Receptor/DOR 0.42 nM (IC50) |
κ Opioid Receptor/KOR 54 nM (IC50) |
μ Opioid Receptor/MOR 370 nM (IC50) |
BACE1 120 nM (IC50) |
Parmacokinetics
| Species | Dose | Route | T1/2 | AUClast | ClF_obs | Vss | Tmax | Cmax | F |
|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 1 mg/kg | i.v. | 1.02 h | 223 ng·h/mL | 75.6 mL/min/kg | 3.75 L/kg | / | / | / |
| Mice[1] | 5 mg/kg | i.p. | 1.05 h | 601 ng·h/mL | / | / | 0.25 h | 0.98 μM | 53.9 % |
| Mice[1] | 5 mg/kg | p.o. | 2.15 h | 162 ng·h/mL | / | / | 0.83 h | 0.16 μM | 14.6 % |
| Mice[1] | 5 mg/kg | s.c. | 0.99 h | 1153 ng·h/mL | / | / | 0.50 h | 0.98 μM | > 99 % |
In Vivo
SRI-22136 (1 mg/kg, s.c., twice daily for 90 days) completely prevented mice Alzheimer’s-like pathology, including memory deficits, β-secretase activity, Aβ1-42 accumulation, and brain inflammatory markers[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Acute tail flick induced by DPDPE established in wild type male and female CD-1 mice[1]
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Dosage:10 mg/kg
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Administration:Intraperitoneal injection (i.p.), single dose
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Result:Blocked robust acute tail flick antinociception induced by DPDPE.
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Animal Model:Alzheimer’s-like pathology model established in 8-week male C57BL/6 mice[1]
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Dosage:1 mg/kg
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Administration:Subcutaneous injection (s.c.), twice daily for 90 days
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Result:Significantly reduced Aβ1-42 levels. Increased BACE1 activity. Reduced activated microglia in cortical brain tissue.
Chemical Information
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Molecular Weight 501.02
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Formula C30H29ClN2O3
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SMILES
ClC(C=C1)=CC=C1C2=CC(C[C@]([C@H](N(CC3)CC4CC4)C5)(OC)[C@@]63C7=C5C=CC(O)=C7O[C@@H]86)=C8N=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Protocol for Hematoxylin-Eosin (H&E) Staining
Hematoxylin-eosin staining is a routine histological method that stains nuclei mainly blue-purple with hemalum and stains cytoplasm, extracellular matrix, and many stromal components pink with eosin, allowing tissue architecture, cell morphology, necrosis, inflammation, fibrosis, tumor growth pattern, and treatment-associated injury to be evaluated by light microscopy. In cancer cells, primary neurons, mouse tumor models, intestinal organoids, inflammatory macrophage preparations, and drug-screening tissues, H&E is a morphology assay rather than a molecular assay; it should be interpreted with complementary molecular or immunostaining assays when the biological question concerns specific proteins, RNA levels, ferroptosis, mitophagy, or immune phenotypes.
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How to Choose the Right Model Animal
Choosing the right model animal is a validity-driven decision in which the species, strain, sex, age, genetic background, disease-induction method, outcome measures, and welfare burden must match the scientific question rather than laboratory tradition or convenience. A model should be selected by judging face validity, construct validity, and predictive validity: whether it resembles the human phenotype, whether it reproduces relevant mechanisms, and whether results are likely to predict human biology or treatment response. Animal studies often fail to translate because of species differences, weak disease resemblance, poor experimental design, inadequate reporting, publication bias, and underuse of randomization, blinding, and sample-size justification. Unresolved questions include how to rank competing models objectively, how much human-disease complexity must be reproduced for a given objective, and when non-animal systems such as organoids, ex vivo tissue, or computational models
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)