1. Immunology/Inflammation
  2. Toll-like Receptor (TLR)
  3. SARM1-IN-7

SARM1-IN-7 是一种强效活性位点 (正构) 且具有口服活性的 SARM1 抑制剂。SARM1-IN-7 持续激活 SARM1 的酶活性,从而在亚浓度下加剧 NAD 的耗竭。SARM1-IN-7 在 SARM1 激活的细胞模型和小鼠模型中表现出双重效应:高剂量发挥细胞/神经元保护作用,而低剂量加剧细胞/神经元损伤。SARM1-IN-7 可用于轴突变性研究。

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SARM1-IN-7

SARM1-IN-7 Chemical Structure

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查看 Toll-like Receptor (TLR) 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SARM1-IN-7 is a potent active site (orthosteric) and orally active SARM1 inhibitor. SARM1-IN-7 continuously activates the enzymatic activity of SARM1, thereby exacerbating the depletion of NAD at sub-minimal concentrations. SARM1-IN-7 demonstrated dual benefits in the SARM1-activated cell models and mouse models: a high dose exerted a cell/neuron protective effect, while a low dose exacerbated cell/neuron damage. SARM1-IN-7 can be used for the study of axon degeneration[1].

体外研究
(In Vitro)

EGFR-IN-172 (Compound NB-3) (0.06 nM-0.6 μM, 24 h) 在高浓度下抑制 SARM1,从而挽救 SH-SY5Y 细胞活力,但亚抑制浓度下则增强了 SARM1 诱导的 SH-SY5Y 细胞死亡[1]

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

体内研究
(In Vivo)

SARM1-IN-7 (Compound NB-3) (0.3-30 mg/kg, i.g., 单次或两次剂量) 在高剂量下显著降低血浆 NfL 水平,但低剂量加剧神经损伤,导致 Vacor 诱导的 SARM1 激活小鼠模型中出现嗜睡、无法活动,甚至死亡等不良事件,在低剂量 Vacor 模型和坐骨神经横断 (SNT) 模型中也观察到了同样的结果[1]

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

Animal Model: Vacor (30mg/kg and 50 mg/kg) induced SARM1 activation model established in 9-10 week old male and female mice (C57bl/6 J)[1]
Dosage: 0.3, 3 and 30 mg/kg (50 mg/kg Vacor model); 0.3 and 1 mg/kg (30mg/kg Vacor model)
Administration: Oral gavage (i.g.), 2 doses (1 hour before the administration of Vacor and 8 hours after the first administration)
Result: Significantly reduced the level of plasma NfL at high dose.
Caused exacerbates nerve damage, leading to adverse events such as drowsiness, immobility, and even death at low doses.
Did not cause nerve damage or adverse events use alone.
Animal Model: Sciatic nerve transection (SNT) model established in 9-10 week old male and female mice (C57bl/6 J)[1]
Dosage: 0.3, 1 and 30 mg/kg
Administration: Oral gavage (i.g.), single dose
Result: Observed the same phenomenon.
分子量

247.22

Formula

C10H12F3N3O

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

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产品名称:
SARM1-IN-7
目录号:
HY-175879
需求量: