1. Metabolic Enzyme/Protease Apoptosis
  2. Prolyl Endopeptidase (PREP) Apoptosis
  3. S 17092

S 17092  (Synonyms: S 17092-1)

目录号: HY-15114 纯度: 99.78%
COA 产品使用指南 技术支持

S 17092 (S 17092-1) 是一种口服有效的脑脯氨酰内肽酶 (PEP) 抑制剂,IC50 为 1.2 nM。S 17092 的作用机制是抑制 PEP 的活性,减缓神经活性肽的降解,从而增强记忆功能。S 17092 抑制细胞凋亡 (apoptosis)。S 17092 可用于研究与脑衰老相关的记忆障碍和认知障碍。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

S 17092

S 17092 Chemical Structure

CAS No. : 176797-26-5

1.  客户无需承担相应的运输费用。

2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1815
In-stock
1 mg ¥750
In-stock
5 mg ¥1300
In-stock
10 mg ¥2100
In-stock
25 mg ¥4200
In-stock
50 mg 现货 询价
100 mg 现货 询价
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

S 17092 (S 17092-1) is an orally active cerebral prolyl-endopeptidase (PEP) inhibitor with an IC50 of 1.2 nM. S 17092 inhibits cell apoptosis. S 17092 mechanism of action is to inhibit the activity of PEP, slowing down the degradation of neuroactive peptides and thus enhancing memory function. S 17092 can be used for the research of memory impairment and cognitive disorders associated with cerebral aging[1][2][3].

体外研究
(In Vitro)

S 17092 可抑制 Wistar 大鼠大脑皮层中的 PEP 活性;最低有效药物浓度为 0.1 nM[1]
S 17092 (10-7-10 μM) 阻断了 HEK 293 细胞内的 PEP 样活性[1]
S 17092 (100 μM, 2-4 h) 抑制多种细胞中 TCR 介导的细胞凋亡,抑制 N3-6-71 细胞中 caspase-8caspase-3 的诱导活性[2]
S-17092 (1-30 μM, 4 h) 单独使用对 3H-CDPDAG 积累没有影响,但它可以逆转锂和甲基胆碱的作用,EC50 为 10 μM[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: N3-6-71, thymocytes and peripheral T cells of BALB/c mice
Concentration: 100 μM
Incubation Time: 2 h for thymocytes, 4 h for N3-6-71 and peripheral T cells
Result: Was able to entirely block activation-induced cell death (AICD) in N3-6-71 cells, inhibits the inducible activities of both caspase-8 and caspase-3.
Reduced PEP activity was observed as assessed by Suc-Gly-Pro-MCA cleavage in thymocytes.
Showed little or no toxicity when added alone at the concentrations tested in thymocytes.
Showed a reduced cell death in thymocytes and peripheral T cells.
体内研究
(In Vivo)

S 17092 (1-10 mg/kg;口服;7 天) 以剂量依赖性方式改善 MPTP (HY-15608) 处理的猴子的认知任务 (VDR、DMS、DA) 的表现[1]
S 17092 (10 mg/kg;口服;7 天,并在每次每日记忆测试前 1 小时再次服用) 可缓解 Scopolamine (HY-N0296) 引起的记忆缺陷,改善年轻和中老年 C57BL/6 小鼠的学习和工作记忆表现[1]
S 17092 (0.01-30 mg/kg;腹腔注射;分别在第 1 次治疗前 60 或 120 分钟,然后 24 小时后,在第 2 次治疗前 60 或 120 分钟注射) 剂量依赖性地增加了大鼠记忆保留时间,从而减轻了 Scopolamine 引起的遗忘症[1]
S 17092 是一种长效 PEP 抑制剂 (t1/2 > 9 小时)。口服一小时后,在 Wistar 大鼠和 NMRI 小鼠中皮质中的 PEP 活性 50% 抑制剂量(ID50)分别为 7.4 和 13.4 mg/kg[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 3-5 months old male C57BL/6 mice[1]
Dosage: 10 mg/kg
Administration: Oral gavage (p.o.); twice daily for 7 days and 60 min prior to the training sessions
Result: Correct responses in the experimental group were 55, 58, and 74% in sessions 1, 2, and 3, respectively. Performance in experimental group was similar to that in non-amnesic controls.
Improved learning and memory performances in young amnesic C57BL/6 mice.
Animal Model: Adult male Macaca fascicularis monkeys treated with MPTP[1]
Dosage: 1, 3, 10 mg/kg
Administration: Oral gavage (p.o.); 7 days
Result: Significantly improved variable delayed response (VDR) performance (76.9% correct responses vs. post-MPTP only) at 3 mg/kg, but not at 1 or 10 mg/kg doses.
VDR performance tended to revert back to a normal delay-dependent pattern of response, performance significantly improved on shorter (2, 5, and 10 sec delay) but not on longer delay trials at the 3mg/kg dose. Improved performance on shorter delay trials was not seen with either the 1 or 10 mg/kg doses.
Significant improvements in DMS (delayed matching-to-sample) performance were observed after administration at either 3 or 10 mg/kg doses.
Significantly improved DA (delayed alternation) performance at the 3 mg/kg dose, from 79% at baseline to 90.6% after 7-days or longer treatments.
Animal Model: 21-22 and 25 months old C57BL/6 mice[1]
Dosage: 10 mg/kg
Administration: Oral gavage (p.o.); 7 days and again 1 h before each daily memory test
Result: With correct responses of 45 and 70% in control and experimental animals, respectively, in session 5 and 46 and 65%, respectively, in session 6 in 21-22 months old C57BL/6 mice.
Had a beneficial effect on the selective deficit observed 25 months old C57BL/6 mice.
Animal Model: Rats treated with scopolamine[1]
Dosage: 0.01-30 mg/kg
Administration: Intraperitoneal injection (i.p.); 60 or 120 min before session 1 then 24 h later 60 or 120 min before session 2, respectively
Result: Dose-dependently increased the retention time, alleviating scopolamine-induced amnesia. The maximum effect using 10 mg/kg with the 60 min pretest dosing interval was achieved using 3 mg/kg in the 120 min tests, suggesting that brain neuropeptide turnover may have been increased by increasing the time interval between the administration and the test.
分子量

384.53

Formula

C22H28N2O2S

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : ≥ 100 mg/mL (260.06 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6006 mL 13.0029 mL 26.0058 mL
5 mM 0.5201 mL 2.6006 mL 5.2012 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6006 mL 13.0029 mL 26.0058 mL 65.0144 mL
5 mM 0.5201 mL 2.6006 mL 5.2012 mL 13.0029 mL
10 mM 0.2601 mL 1.3003 mL 2.6006 mL 6.5014 mL
15 mM 0.1734 mL 0.8669 mL 1.7337 mL 4.3343 mL
20 mM 0.1300 mL 0.6501 mL 1.3003 mL 3.2507 mL
25 mM 0.1040 mL 0.5201 mL 1.0402 mL 2.6006 mL
30 mM 0.0867 mL 0.4334 mL 0.8669 mL 2.1671 mL
40 mM 0.0650 mL 0.3251 mL 0.6501 mL 1.6254 mL
50 mM 0.0520 mL 0.2601 mL 0.5201 mL 1.3003 mL
60 mM 0.0433 mL 0.2167 mL 0.4334 mL 1.0836 mL
80 mM 0.0325 mL 0.1625 mL 0.3251 mL 0.8127 mL
100 mM 0.0260 mL 0.1300 mL 0.2601 mL 0.6501 mL
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.

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称:

 

* 需求量:

* 客户姓名:

 

* Email:

* 电话:

 

* 公司或机构名称:

   留言给我们:

Bulk Inquiry

Inquiry Information

产品名称:
S 17092
目录号:
HY-15114
需求量: