1. SMases D-IN-1

SMases D-IN-1 是一种 Loxosceles (​棕色隐士蜘蛛) 鞘磷脂酶 D (SMase D) 抑制剂,Ki 值为 0.54 μM。SMases D-IN-1 可抑制重组及天然 SMases D 对鞘磷脂底物的水解作用,降低 SMases D 与人红细胞的结合能力,并阻止人红细胞表面血型糖蛋白 C 的脱落。SMases D-IN-1 可部分抑制 Loxosceles 毒液诱导的人角质形成细胞死亡,还能抑制 Loxosceles 毒液引发的全身反应。SMases D-IN-1 可用于隐士蜘蛛毒中毒的相关研究。

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SMases D-IN-1

SMases D-IN-1 Chemical Structure

CAS No. : 849020-48-0

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SMases D-IN-1 is an inhibitor of SMase D (sphingomyelinase D) from Loxosceles, with a Ki value of 0.54 μM. SMases D-IN-1 inhibits the hydrolysis of sphingomyelin substrates by recombinant and native SMases D, reduces the binding ability of SMases D to human red blood cells, and prevents the shedding of glycophorin C from the surface of human red blood cells. SMases D-IN-1 partially inhibits Loxosceles venom-induced death of human keratinocytes and also suppresses systemic reactions triggered by Loxosceles venom. SMases D-IN-1 can be used in studies related to recluse spider envenomation[1].

体外研究
(In Vitro)

SMases D-IN-1 (Compound 1) (20 μg; 30 min) 可降低 SMase D 与人红细胞的结合,并完全阻止毒液诱导的血型糖蛋白 C 从人红细胞表面裂解[1]
SMases D-IN-1 (5 μg;72 h) 可部分减轻 L. laeta 毒液诱导的人 HaCaT 角质形成细胞死亡[1]
SMases D-IN-1 (20 μg; 2 h at 37 °C) 不会降低 SMase D 与人 HaCaT 角质形成细胞膜的结合[1]
SMases D-IN-1 (5 μg;72 h) 可使暴露于 L. laeta 毒液的人 HaCaT 角质形成细胞中 MMP-2MMP-9 的分泌恢复正常[1]

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

Cell Viability Assay[1]

Cell Line: human HaCaT keratinocytes
Concentration: 5 μg
Incubation Time: 72 h
Result: Partially prevented L.
laeta venom-induced HaCaT cell death.
体内研究
(In Vivo)

SMases D-IN-1 (1 mg;皮内注射;单次给药) 对新西兰白化兔由 Loxosceles laeta 毒液诱导的皮肤坏死及相关组织病理学损伤无显著抑制作用[1]

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

Animal Model: Albino New Zealand (male, 3 kg)[1]
Dosage: 1 mg
Administration: i.d.; single dose
Result: Had no significant effect on the development of venom-induced dermonecrotic lesions over 72 hours.
Showed persistent haemorrhagic areas, dense inflammatory infiltrate, collagen disorganisation, and adjacent muscle layer injury in skin samples, similar to venom-only controls.
分子量

412.49

Formula

C19H16N4O3S2

CAS 号
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

SMases D-IN-1 相关分类

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产品名称:
SMases D-IN-1
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HY-182413
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