| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
Spns2 (Spinster homolog 2), a transporter that mediates sphingosine-1-phosphate (S1P) release from cells. By inhibiting Spns2, SLB1122168 reduces extracellular S1P levels, thereby affecting S1P receptor signaling and lymphocyte trafficking. The compound has an IC50 of 94 nM for Spns2-mediated S1P release.
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| ln Vitro |
SLB1122168 formic is a potent inhibitor of Spns2-mediated S1P release with an IC50 value of 94 nM. It shows high selectivity for Spns2 over other transporters. The compound demonstrates good solubility in DMSO (100 mg/mL) and has favorable physicochemical properties for in vitro studies. Its activity is measured using cell-based S1P release assays or biochemical transport assays.
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| ln Vivo |
The amount of circulating lymphocytes is reduced in a dose-dependent manner by SLB1122168 (33p; 10 mg/kg; i.p.; once) [1]. SLB1122168 (33p) in rats at a dose of 10 mg/kg had a half-life of 8 hours and a maximal concentration of 4 μM 2 hours after delivery, with concentrations ≥1 μM within 24 hours [1].
In vivo, SLB1122168 formic induces a dose-dependent reduction in circulating lymphocytes. In rats, a single intraperitoneal dose of 10 mg/kg resulted in a peak plasma concentration of 4 uM at 2 hours post-administration, with levels remaining ≥1 uM up to 24 hours. The compound has a plasma half-life of approximately 8 hours, indicating good pharmacokinetic properties for in vivo studies. |
| Enzyme Assay |
Spns2-mediated S1P release inhibition assay: Cells expressing Spns2 (e.g., HEK293-Spns2) are loaded with fluorescent S1P analog or incubated with 3H-S1P. Increasing concentrations of SLB1122168 formic (0-10 uM) are added for 30 min at 37degC. Extracellular S1P levels are measured by scintillation counting (for 3H-S1P) or fluorescence intensity. The IC50 (94 nM) is calculated by non-linear regression analysis of triplicate measurements. Non-specific release is determined using mock-transfected cells.
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| Cell Assay |
Cellular S1P release assay protocol: S1P-producing cells (e.g., RBCs or HEK293 cells expressing Spns2) are seeded in 96-well plates. Cells are treated with SLB1122168 formic (0-10 uM) for 1-4 hours at 37degC. Culture supernatants are collected and S1P concentrations are quantified by LC-MS/MS or commercial S1P ELISA kit. Percent inhibition is calculated relative to vehicle-treated controls. IC50 values are determined by non-linear regression using GraphPad Prism.
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| Animal Protocol |
Pharmacokinetic and pharmacodynamic study protocol: Male Sprague-Dawley rats (n=3-4 per group) receive a single intraperitoneal injection of SLB1122168 formic at 10 mg/kg. Blood samples are collected at 0, 0.5, 1, 2, 4, 6, 8, 12, 24 hours post-dose via tail vein. Plasma concentrations of SLB1122168 are measured by LC-MS/MS. For lymphocyte counting, blood samples are collected in EDTA tubes and analyzed using automated hematology analyzer. PK parameters are calculated by non-compartmental analysis.
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| ADME/Pharmacokinetics |
SLB1122168 formic shows favorable PK properties in rats. After intraperitoneal administration at 10 mg/kg, the compound reaches a peak plasma concentration (Cmax) of 4 uM at 2 hours (Tmax). Plasma levels remain ≥1 uM for up to 24 hours post-dose. The compound has a terminal half-life (t½) of approximately 8 hours. These properties support its use in in vivo efficacy studies requiring sustained target inhibition.
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| Toxicity/Toxicokinetics |
Toxicology data for SLB1122168 formic are limited. In rat studies at 10 mg/kg (i.p., single dose), the compound was generally well tolerated with no acute adverse effects reported. The primary pharmacodynamic effect is a dose-dependent reduction in circulating lymphocytes, which is the intended on-target effect of Spns2 inhibition. The compound is intended for research use only and not for human therapeutic applications.
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| References | |
| Additional Infomation |
SLB1122168 formic is a research compound targeting the Spns2-S1P axis for studying immune cell trafficking. S1P signaling plays a critical role in lymphocyte egress from lymph nodes, and Spns2 inhibition represents a novel approach for immunomodulation distinct from direct S1P receptor modulators. The compound has not entered clinical trials or received regulatory approval. It should be stored as powder at -20degC for long-term stability.
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| Molecular Formula |
C23H37N3O3
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| Related CAS # |
SLB1122168
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| Appearance |
Off-white to light yellow solid-liquid Mixture
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| SMILES |
CCCCCCCCCCC1=CC=C2C(OC(NC[C@@H]3CNCC3)=N2)=C1.OC=O
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~247.8 mM; with ultrasonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.19 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.19 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (6.19 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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