2. GPCR/G Protein Neuronal Signaling
  3. Opioid Receptor Beta-secretase
  4. 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.

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SRI-22136

SRI-22136 Chemical Structure

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SRI-22136 Related Antibodies

Top Publications Citing Use of Products

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μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

View All Beta-secretase Isoform Specific Products:

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BACE1 BACE2

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Description

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[1].

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[1]
Species Dose Route Indicator value
Mice 1 mg/kg i.v. T1/2 1.02 h
Mice 5 mg/kg i.p. T1/2 1.05 h
Mice 5 mg/kg p.o. T1/2 2.15 h
Mice 5 mg/kg s.c. T1/2 0.99 h
Mice 1 mg/kg i.v. AUClast 223 ng·h/mL
Mice 5 mg/kg i.p. Tmax 0.25 h
Mice 5 mg/kg p.o. Tmax 0.83 h
Mice 5 mg/kg s.c. Tmax 0.50 h
Mice 1 mg/kg i.v. ClF_obs 75.6 mL/min/kg
Mice 5 mg/kg i.p. Cmax 0.98 μM
Mice 5 mg/kg p.o. Cmax 0.16 μM
Mice 5 mg/kg s.c. Cmax 0.98 μM
Mice 1 mg/kg i.v. Vss 3.75 L/kg
Mice 5 mg/kg i.p. AUClast 601 ng·h/mL
Mice 5 mg/kg p.o. AUClast 162 ng·h/mL
Mice 5 mg/kg s.c. AUClast 1153 ng·h/mL
Mice 5 mg/kg i.p. F 53.9 %
Mice 5 mg/kg p.o. F 14.6 %
Mice 5 mg/kg s.c. F > 99 %
In Vivo

SRI-22136 (Compound 12) (0.1-10 mg/kg, i.p., single dose) fully blocks DPDPE (HY-P1334)-induced antinociception, shows full antagonist efficacy at 1 and 10 mg/kg, with partial efficacy at 0.1 and 0.32 mg/kg, suggesting systemic stability and blood-brain barrier penetration[1].
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.

Animal Model: Acute tail flick induced by DPDPE established in wild type male and female CD-1 mice[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p.), single dose
Result: Blocked robust acute tail flick antinociception induced by DPDPE.
Animal Model: Alzheimer’s-like pathology model established in 8-week male C57BL/6 mice[1]
Dosage: 1 mg/kg
Administration: Subcutaneous injection (s.c.), twice daily for 90 days
Result: Significantly reduced Aβ1-42 levels.
Increased BACE1 activity.
Reduced activated microglia in cortical brain tissue.
Molecular Weight

501.02

Formula

C30H29ClN2O3
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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SRI-22136 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SRI-22136SRI22136SRI 22136Opioid ReceptorBeta-secretaseBACEβ-SecretaseAlzheimer’s DiseaseDelta Opioid ReceptorAntagonistAβ1?42Inhibitorinhibitorinhibit

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