1. Immunology/Inflammation
  2. SphK
  3. 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).

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SLM6031434

SLM6031434 Estructura química

No. CAS : 1897379-33-7

Tamaño Precio Stock Cantidad
1 mg Obtener un presupuesto 3 - 4 Weeks 4 - 5 Weeks 5 - 6 Weeks 2 - 3 weeks
5 mg Obtener un presupuesto 3 - 4 Weeks 4 - 5 Weeks 5 - 6 Weeks 2 - 3 weeks
10 mg Obtener un presupuesto 3 - 4 Weeks 4 - 5 Weeks 5 - 6 Weeks 2 - 3 weeks
50 mg   Obtener un presupuesto  
100 mg   Obtener un presupuesto  
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Descripciòn

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)

In Vitro

SLM6031434 (3 μM, 16 h) reduces TGFβ-induced expression of profibrotic markers (Col1, FN-1, CTGF) in primary mouse renal fibroblasts[1].
SLM6031434 (0.3-10 μM, 16 h) dose-dependently increases Smad7 protein expression in primary mouse renal fibroblasts[1].
SLM6031434 (1 μM, 20 h) significantly increases cellular sphingosine levels in human podocytes[2].
SLM6031434 (1 μM, 24 h) upregulates nephrin and Wilm’s tumor suppressor gene 1 (WT1) protein expressions and mRNA expressions in wildtype human podocytes[2].

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

In Vivo

SLM6031434 (5 mg/kg, i.p., daily, 9 days) attenuates unilateral ureteral obstruction (UUO)-induced renal interstitial fibrosis in mice[1].

MedChemExpress (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.
Peso molecular

453.50

Fòrmula

C22H30F3N5O2

No. CAS
SMILES

N=C(N1[C@H](C2=NC(C3=CC=C(OCCCCCCCC)C(C(F)(F)F)=C3)=NO2)CCC1)N

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.

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    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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Inquiry Information

Nombre del producto:
SLM6031434
Cat. No.:
HY-120268
Cantidad:
MCE Japan Authorized Agent: