SLM6031434 - CAS:1897379-33-7

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SLM6031434

目录号 : KCM12237 CAS No. : 1897379-33-7 纯度 : ≥98%

Data Sheet 产品使用指南

SLM6031434 is an inhibitor of sphingosine kinase 2 (SPHK2) (K = 0.4 μM for the recombinant mouse enzyme). It is selective for SPHK2 over SPHK1 (Ks = >20 μM). It decreases sphingosine-1-phosphate (S1P; ) and increases sphingosine levels in U937 monocytic leukemia cells in a concentration-dependent manner. SLM6031434 (5 mg/kg) reduces blood S1P levels in Sphk1, but not Sphk2, mice. SLM6031434 also increases blood S1P levels in wild-type mice and rats.

规格	价格	是否有货	数量
1mg		In-stock
5mg		In-stock
10mg		In-stock
25mg		In-stock

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Other Forms of Rapamycin:

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SLM6031434 (hydrochloride) In-stock
SLM6031434 In-stock
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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).

体外研究

SLM6031434 (3 μM, 16 h) reduces the expression of TGFβ-induced profibrotic markers (Col1, FN-1, CTGF) in primary mouse renal fibroblasts.
SLM6031434 (0.3-10 μM, 16 h) increased Smad7 protein expression in primary mouse renal fibroblasts in a dose-dependent manner.
SLM6031434 (1 μM, 20 h) significantly increased the ceramide levels in human podocytes.
SLM6031434 (1 μM, 24 h) upregulates the protein and mRNA expression of nephrin and Wilms tumor suppressor gene 1 (WT1) in wild-type human podocytes.

体内研究

SLM6031434 (5 mg/kg, intraperitoneal injection, daily for 9 days) alleviates unilateral ureteral obstruction-induced renal interstitial fibrosis in mice.

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
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.

分子式

C₂₂H₃₀F₃N₅O₂

分子量

453.50

CAS号

1897379-33-7

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

纯度： ≥98%

Data Sheet

产品使用指南

Schwalm S, et al. Validation of highly selective sphingosine kinase 2 inhibitors SLM6031434 and HWG-35D as effective anti-fibrotic treatment options in a mouse model of tubulointerstitial fibrosis. Cell Signal. 2021 Mar;79:109881.

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Other Forms of Rapamycin:

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