1. Immunology/Inflammation
  2. SphK
  3. SLM6031434 hydrochloride

SLM6031434 hydrochloride is the hydrochloride salt form of SLM6031434 (HY-120268). 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 hydrochloride

SLM6031434 hydrochloride Chemical Structure

CAS No. : 1897379-34-8

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Based on 1 publication(s) in Google Scholar

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Description

SLM6031434 hydrochloride is the hydrochloride salt form of SLM6031434 (HY-120268). 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.
Molecular Weight

489.96

Formula

C22H31ClF3N5O2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

N=C(N1[C@H](C2=NC(C(C=C3)=CC(C(F)(F)F)=C3OCCCCCCCC)=NO2)CCC1)N.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

H2O : 40 mg/mL (81.64 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.1%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 2.0410 mL 10.2049 mL 20.4098 mL 51.0246 mL
5 mM 0.4082 mL 2.0410 mL 4.0820 mL 10.2049 mL
10 mM 0.2041 mL 1.0205 mL 2.0410 mL 5.1025 mL
15 mM 0.1361 mL 0.6803 mL 1.3607 mL 3.4016 mL
20 mM 0.1020 mL 0.5102 mL 1.0205 mL 2.5512 mL
25 mM 0.0816 mL 0.4082 mL 0.8164 mL 2.0410 mL
30 mM 0.0680 mL 0.3402 mL 0.6803 mL 1.7008 mL
40 mM 0.0510 mL 0.2551 mL 0.5102 mL 1.2756 mL
50 mM 0.0408 mL 0.2041 mL 0.4082 mL 1.0205 mL
60 mM 0.0340 mL 0.1701 mL 0.3402 mL 0.8504 mL
80 mM 0.0255 mL 0.1276 mL 0.2551 mL 0.6378 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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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Product Name:
SLM6031434 hydrochloride
Cat. No.:
HY-120268A
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