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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- CAS. Nr.: 1897379-33-7
- Formel: C22H30F3N5O2
- Molecular Weight:453.50
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Help & FAQs
Biologische Aktivität
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SphK2 0.4 μM (IC50) |
SphK1 16 μM (IC50) |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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]
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Dosage:5 mg/kg
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Administration:i.p., daily, 9 days
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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.
Chemical Information
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CAS. Nr. 1897379-33-7
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Molecular Weight 453.50
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Formel C22H30F3N5O2
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SMILES
N=C(N1[C@H](C2=NC(C3=CC=C(OCCCCCCCC)C(C(F)(F)F)=C3)=NO2)CCC1)N
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. 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. [Content Brief]
[2]. Imeri F, et al. Loss of sphingosine kinase 2 enhances Wilm's tumor suppressor gene 1 and nephrin expression in podocytes and protects from streptozotocin-induced podocytopathy and albuminuria in mice. Matrix Biol. 2021 Apr;98:32-48. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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