2. GPCR/G Protein Neuronal Signaling
  3. Opioid Receptor Beta-secretase
  4. SRI-22136

SRI-22136 是一种能通过血脑屏障的 Delta 阿片受体 (DOR) 拮抗剂，其 IC50 为 0.42 nM。SRI-22136 没有对 DOR、MOR 和 KOR 没有激动活性，仅有拮抗活性，对 MOR 和 KOR 的 IC50 分别为 370nM 和 54 nM，因此可以避免成瘾/厌恶效应。SRI-22136 可以有效抑制由 DADLE (一种 DOR 激动剂) (HY-105343) 诱导的 BACE1 活性 (IC50 = 120 nM)。SRI-22136 可在小鼠模型中完全预防阿尔茨海默病样病理。SRI-22136 可用于阿尔茨海默病的研究。

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SRI-22136

SRI-22136 Chemical Structure

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SRI-22136 相关抗体

Top Publications Citing Use of Products

查看 Opioid Receptor 亚型特异性产品:

查看所有亚型
μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

查看 Beta-secretase 亚型特异性产品:

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BACE1 BACE2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

药代动力学
(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 %
体内研究
(In Vivo)

SRI-22136 (Compound 12) (0.1-10 mg/kg，腹腔注射，单剂量) 完全阻断了 DPDPE (HY-P1334) 诱导的抗伤害作用，在 1 和 10 mg/kg 剂量下显示出完全拮抗作用，在 0.1 和 0.32 mg/kg 剂量下显示出部分作用，表明其具有全身稳定性和血脑屏障穿透性[1]。
SRI-22136 (1 mg/kg，皮下注射，每日两次，持续 90 天) 完全预防了小鼠阿尔茨海默病样病理，包括记忆缺陷、β-分泌酶活性、Aβ1-42 蓄积和脑部炎症标志物[1]。

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.
分子量

501.02

Formula

C30H29ClN2O3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

SRI-22136 相关分类

  • 摩尔计算器

  • 稀释计算器

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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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目录号：
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