1. GPCR/G Protein
  2. LPL Receptor
  3. SLF1081851

SLF1081851 is a Spns2 inhibitor, inhibits S1P release (IC50=1.93 μM). SLF1081851 plays a key role in development and immune system.

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SLF1081851 Chemical Structure

SLF1081851 Chemical Structure

CAS No. : 2763730-97-6

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Based on 1 publication(s) in Google Scholar

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1 Publications Citing Use of MCE SLF1081851

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Description

SLF1081851 is a Spns2 inhibitor, inhibits S1P release (IC50=1.93 μM). SLF1081851 plays a key role in development and immune system[1][2].

IC50 & Target

Spns2 (spinster homologue 2)[1]

In Vitro

Sphingosine 1-phosphate (S1P) is a pleiotropic signaling molecule, and Spns2 exerts the functions to maintain lymph S1P[1].
SLF1081851 (compound 16d) (0-5 μM; 18-20 h) inhibits S1P release with an IC50 value of 1.93 μM in Hela cells[1].
SLF1081851 (0-30 μM; 20 min) inhibits mSphK1 (recombinant mouse SphK) (10 μM) and mSphK2 (5 μM) in a dose-dependent manner and suggests at least 15-fold selectivity (SphK1 IC50≥30 μM; SphK2 IC50≈30 μM)[1].

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

In Vivo

SLF1081851 (20 mg/kg; i.p., 4 h postdose) significantly inhibits circulating lymphocytes and plasma S1P, and recapitulates the genetic phenotype of Spns2 null mice[1].

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

Animal Model: C57BL/6 mice[1]
Dosage: 20 mg/kg
Administration: Intraperitoneal injection; blood was drawn 4 h postdose
Result: Significantly decreased circulating lymphocyte count and plasma S1P concentration.
Animal Model: SpragueDawley mice (4-week-old)[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; single dose; measured at 0, 0.5, 1, 2, 4, 6, and 24 h postdose
Result: Reached a maximum concentration of 5 μM in blood at 2 h with drug levels sustained at ≥ 2 μM for at least 24 h, proved a half-life of over 8 h in rats. The appearance of SPNS2-IN-1 in circulation correlated with a maximal decrease in lymphocyte count at 4 h (25% lower compared to time =0).
Molecular Weight

343.51

Formula

C21H33N3O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NCCCC1=NC(C2=CC=C(CCCCCCCCCC)C=C2)=NO1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

Ethanol : 10 mg/mL (29.11 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9111 mL 14.5556 mL 29.1112 mL
5 mM 0.5822 mL 2.9111 mL 5.8222 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% EtOH    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1 mg/mL (2.91 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  50% PEG300    50% Saline

    Solubility: 6.67 mg/mL (19.42 mM); Suspended solution; Need ultrasonic

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

Dosage

mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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 (protect from light). 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
Ethanol 1 mM 2.9111 mL 14.5556 mL 29.1112 mL 72.7781 mL
5 mM 0.5822 mL 2.9111 mL 5.8222 mL 14.5556 mL
10 mM 0.2911 mL 1.4556 mL 2.9111 mL 7.2778 mL
15 mM 0.1941 mL 0.9704 mL 1.9407 mL 4.8519 mL
20 mM 0.1456 mL 0.7278 mL 1.4556 mL 3.6389 mL
25 mM 0.1164 mL 0.5822 mL 1.1644 mL 2.9111 mL
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SLF1081851 Related Classifications

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  • Do most proteins show cross-species activity?

    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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SLF1081851
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