SLM6031434 (hydrochloride)
目录号 : KCM12238 CAS No. : 1897379-34-8 纯度 : ≥98%
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
50mg 询价 In-stock

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生物活性

SLM6031434 (hydrochloride) is the hydrochloride salt form of SLM6031434. 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) dose-dependently increased Smad7 protein expression in primary mouse renal fibroblasts.
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, 9 days) alleviates renal interstitial fibrosis induced by unilateral ureteral obstruction 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.HCl
分子量
489.96
CAS号
1897379-34-8
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式

2-8°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO: 5 mg/mL (10.20 mM; Need ultrasonic)

配制储备液
                                           
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
                                                                                                                    
1 mM 2.0410 mL 10.2049 mL 20.4098 mL
5 mM 0.4082 mL 2.0410 mL 4.0820 mL
10 mM 0.2041 mL 1.0205 mL 2.0410 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

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