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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- Formel: C30H29ClN2O3
- Molecular Weight:501.02
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Alle Opioid Receptor Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
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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) |
| 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 % |
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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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
SRI-22136 Related Classifications
HY-175661 Related Classifications
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