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SLB1122168 formic

Cat No.:V76507 Purity: ≥98%
SLB1122168 formic is a potent inhibitor of Spns2-mediated S1P release with IC50 of 94 nM.
SLB1122168 formic
SLB1122168 formic Chemical Structure Product category: LPL Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
50mg
Other Sizes

Other Forms of SLB1122168 formic:

  • SLB1122168
  • (R)-SLB1122168 free base
  • SLB1122168 free base
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
SLB1122168 formic is a potent inhibitor of Spns2-mediated S1P release with IC50 of 94 nM.
SLB1122168 formic is a potent small-molecule inhibitor targeting Spns2-mediated sphingosine-1-phosphate (S1P) release. It exhibits an IC50 value of 94 nM against this target. The compound functions as an LPL receptor modulator and is used in research studying immune cell trafficking and inflammatory diseases. The molecular formula is C23H37N3O3 with a molecular weight of 403.56, and purity is reported at 99.91%.
Biological Activity I Assay Protocols (From Reference)
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.
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.
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.
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.
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.
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.
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.
References

[1]. 2-Aminobenzoxazole Derivatives as Potent Inhibitors of the Sphingosine-1-Phosphate Transporter Spinster Homolog 2 (Spns2). J Med Chem. 2023 Apr 27;66(8):5873-5891.

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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C23H37N3O3
Related CAS #
SLB1122168
Appearance
Off-white to light yellow solid-liquid Mixture
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
Solubility (In Vivo)
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

Injection Formulations
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO 400 μLPEG300 50 μL Tween 80 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).
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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO 900 μL (20% SBE-β-CD in saline)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL Saline)


Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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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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