2. Immunology/Inflammation
  3. Toll-like Receptor (TLR)
  4. SARM1-IN-10

SARM1-IN-10 是一种口服有效的 SARM1 抑制剂，其 pIC50 为 7.1，pKd 为 8.3。SARM1-IN-10 作为碱基交换抑制剂，可在 SARM1 的 TIR 结构域活性位点形成 NAD+ 加合物，阻断酶功能，并在 SARM1 的催化位点诱导独特的 W662 旋转异构态。SARM1-IN-10 在低剂量下是反常的神经变性诱导剂，高剂量下则为抑制剂，可根据浓度加剧或保护 SARM1 介导的神经变性。SARM1-IN-10 可用于周围神经变性的研究。

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SARM1-IN-10

SARM1-IN-10 Chemical Structure

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SARM1-IN-10 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SARM1-IN-10 is an orally active SARM1 inhibitor with a pIC50 of 7.1 and a pKd of 8.3. As a base-exchange inhibitor, SARM1-IN-10 forms a NAD+ adduct at the active site of the TIR domain of SARM1, blocks enzymatic function, and induces a unique rotameric state of W662 at the catalytic site of SARM1. SARM1-IN-10 acts as a paradoxical neurodegeneration inducer at low doses and an inhibitor at high doses, and it can exacerbate or protect against SARM1-mediated neurodegeneration depending on concentration. SARM1-IN-10 can be used in studies of peripheral neurodegeneration[1].

体外研究
(In Vitro)

SARM1-IN-10 (Compound 19) (25 h) 可保护诱导型 SAM-TIR HEK293 细胞免受 SARM1 介导的细胞死亡，其 pEC50 为 7.8[1]。
SARM1-IN-10 (48 h) 可保护原代大鼠 DRG 轴突免受 Vincristine (HY-N0488A) 诱导的变性，其 EC50 为 55 nM[1]。
SARM1-IN-10 (48 h) 可保护原代小鼠 DRG 轴突免受 Vincristine 诱导的变性，其 EC50 为 113 nM[1]。
SARM1-IN-10 ( 过夜) 在轻度应激条件下，于表达全长人源 SARM1 (无 MTS) 的 HEK293 细胞中，在浓度低于 100 nM 时会加重 CZ-48 (HY-129522) 诱导的细胞死亡，而在更高浓度下则起到保护作用[1]。
SARM1-IN-10 (9 或 25 h) 在轻度应激条件下的原代大鼠 DRG 中，低浓度时会加重 CZ-48 诱导的轴突变性，而高浓度时则具有轴突保护作用[1]。
SARM1-IN-10 (49 h) 在轻度应激条件下，于低浓度时会加重 hiPSC 来源皮质神经元中 vacor 诱导的轴突变性，而在高浓度时则对轴突具有保护作用[1]。

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

SARM1-IN-10 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route CL CLunbound Vd T1/2 Bioavailability
Mice[1] 2 mg/kg i.v. 50 mL/min/kg 417 mL/min/kg 5.0 L/kg 1.1 h /
Mice[1] 5 mg/kg p.o. / / / / 34 %
体内研究
(In Vivo)

SARM1-IN-10 (Compound 19) (25-100 mg/kg；口服；每日 2 次共 4 次) 在小鼠模型中发挥神经退行性病变保护作用，但低剂量下会升高神经退行性病变相关标志物水平[1]。

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

Animal Model: C57BL/6 (male, 6-to-8 weeks old, spared sciatic nerve injury model)[1]
Dosage: 25 mg/kg; 50 mg/kg; 100 mg/kg
Administration: p.o.; twice daily for 4
doses
Result: Reduced plasma NfL concentrations to levels comparable to the sham group at 50 mg/kg and 100 mg/kg BID.
Increased plasma NfL concentrations relative to the vehicle group at 25 mg/kg BID.
Achieved terminal plasma concentrations of 285 ng/mL at 30 hours (6 hours post-final dose) in the 25 mg/kg group.
Achieved terminal plasma concentrations of 903 ng/mL at 30 hours (6 hours post-final dose) in the 50 mg/kg group.
Achieved terminal plasma concentrations of 3028 ng/mL at 30 hours (6 hours post-final dose) in the 100 mg/kg group.
分子量

454.50

Formula

C25H23FN8
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

SARM1-IN-10 相关分类

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  • 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:

SARM1-IN-10Toll-like Receptor (TLR)mouse SNI modelSARM1 TIR domainW662NAD+rat DRG axonsSARM1hiPSC-derived cortical neuronsHEK293 cellsmouse DRG axonsperipheral nerve degenerationInhibitorinhibitorinhibit

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