1. Immunology/Inflammation
  2. SphK
  3. SLM6031434

SLM6031434 是一种高度选择性的鞘脂激酶 2 (SphK2) 抑制剂,对 SphK2IC50 值为 0.4 μM。SLM6031434 通过增加鞘脂积累和 Smad7 表达发挥抗纤维化作用。SLM6031434 在单侧输尿管梗阻 (UUO) 诱导的小鼠肾小管间质纤维化模型中显示出有效的抗纤维化疗效。SLM6031434 可用于蛋白尿性肾病或慢性肾病 (CKD) 的研究。

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SLM6031434

SLM6031434 Chemical Structure

CAS No. : 1897379-33-7

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1 mg ¥843
3 - 4 周
5 mg ¥2530
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10 mg ¥4048
3 - 4 周
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生物活性

SLM6031434 is a highly selective sphingosine kinase 2 (SphK2) inhibitor with an IC50 value of 0.4 μM for SphK2. SLM6031434 exerts anti-fibrotic effects by increasing sphingosine accumulation and Smad7 expression. SLM6031434 demonstrates effective anti-fibrotic efficacy in a unilateral ureteral obstruction (UUO)-induced tubulointerstitial fibrosis mouse model. SLM6031434 can be used for the study of proteinuric kidney diseases or chronic kidney disease (CKD)[1][2].

IC50 & Target[1]

SphK2

0.4 μM (IC50)

SphK1

16 μM (IC50)

体外研究
(In Vitro)

SLM6031434 (3 μM, 16 h) 降低原代小鼠肾成纤维细胞中 TGFβ 诱导的促纤维化标志物(Col1、FN-1、CTGF)的表达[1]
SLM6031434 (0.3-10 μM, 16 h) 以剂量依赖方式增加原代小鼠肾成纤维细胞中 Smad7 蛋白表达[1]
SLM6031434 (1 μM, 20 h) 显著增加人足细胞中的细胞鞘脂水平[2]
SLM6031434 (1 μM, 24 h) 在野生型人足细胞中上调 nephrin 和 Wilm 氏肿瘤抑制基因 1 (WT1) 的蛋白表达和 mRNA 表达[2]

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

体内研究
(In Vivo)

SLM6031434 (5 mg/kg,,腹腔注射,每日,9 天) 减轻小鼠单侧输尿管梗阻诱导的肾间质纤维化[1]

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

Animal Model: UUO-induced renal interstitial fibrosis mouse models were established by performing unilateral ureteral ligation surgery on 10-12 week-old adult male mice[1]
Dosage: 5 mg/kg
Administration: i.p., daily, 9 days
Result: Reduced collagen accumulation and ECM deposition.
Decreased α-SMA expression to reduce myofibroblast activation.
Downregulated mRNA and protein levels of Col1, FN-1, CTGF.
Increased sphingosine accumulation and Smad7 expression, while reduced Smad2 phosphorylation.
Reduced F4/80-positive macrophage infiltration and downregulated iNOS, Mcr1 mRNA.
分子量

453.50

Formula

C22H30F3N5O2

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
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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.

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产品名称:
SLM6031434
目录号:
HY-120268
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