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)

IC50&Target

SphK2                                           SphK1

0.4 μM (IC50)                                16 μM (IC50)

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。

The molarity calculator equation
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The dilution calculator equation
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This equation is commonly abbreviated as: C1V1 = C2V2
动物实验计算换算器
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计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,

体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。

配置后的溶液总体积:

1. 首先保证母液是澄清的;
           2. 一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。