| Size | Price | Stock | Qty |
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| Targets |
SPT-IN-1 targets serine palmitoyltransferase (SPT), the enzyme that catalyzes the condensation of L-serine and palmitoyl-CoA to form 3-ketosphinganine, the first committed step in sphingolipid biosynthesis. By inhibiting SPT, SPT-IN-1 reduces the production of sphingolipids, which are involved in insulin signaling and lipid metabolism.
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| ln Vitro |
SPT-IN-1 (compound 1) inhibits the incorporation of C14-serine into ceramide in MCF-7 cells in a dose-dependent manner, with an EC50 of 0.98 μM [1].
SPT-IN-1 is a potent SPT inhibitor with an IC50 of 5.19 nM for hSPT1. The compound is orally active and can be used for studying the role of sphingolipid metabolism in disease. It has shown potential in treating diseases associated with dysregulated sphingolipid metabolism, such as cancer, neurodegenerative disorders, and metabolic diseases. |
| ln Vivo |
In rats fed cholesterol/cholic acid, SPT-IN-1 (Compound 1) (Sprague Dawley rats, 0–60 mg/kg, orally, twice daily for 7 days) dose-dependently lowers plasma ceramide, lowers triglycerides, and raises HDL[1].
SPT-IN-1 is orally active and has shown potential in treating diseases associated with dysregulated sphingolipid metabolism. It can be used for type 2 diabetes and dyslipidemia research. Specific animal model data and dosing regimens are not extensively detailed in standard reference sources. |
| Enzyme Assay |
SPT-IN-1's inhibition of SPT can be assessed using in vitro enzyme activity assays. Recombinant human SPT1 is incubated with its substrates (L-serine and palmitoyl-CoA) in the presence of varying concentrations of SPT-IN-1. The production of 3-ketosphinganine is measured using a suitable detection method (e.g., radiometric, HPLC, or mass spectrometry) to determine the IC50.
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| Cell Assay |
The cellular activity of SPT-IN-1 is evaluated in cell-based assays measuring sphingolipid levels. Cells are treated with increasing concentrations of SPT-IN-1, and sphingolipid species (e.g., sphingomyelin, ceramide, sphingosine) are quantified by LC-MS/MS. The effect of SPT inhibition on cell viability, insulin signaling, and lipid metabolism is assessed.
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| Animal Protocol |
SPT-IN-1 is administered orally in animal models of type 2 diabetes and dyslipidemia. In rodent models, the compound would be given at various doses via oral gavage. Blood glucose, insulin sensitivity, lipid profiles, and sphingolipid levels in tissues would be measured to assess efficacy.
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| ADME/Pharmacokinetics |
SPT-IN-1 has a molecular formula of C22H24N2O3 and a molecular weight of 364.44 g/mol. Its chemical name is 2-(4-(6-heptanoylimidazo[1,2-a]pyridin-8-yl)phenyl)acetic acid. It is orally active. Specific pharmacokinetic parameters are not extensively detailed.
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| Toxicity/Toxicokinetics |
The toxicity profile of SPT-IN-1 is not extensively documented. As an inhibitor of sphingolipid biosynthesis, potential adverse effects may include disruption of cell membrane integrity and signaling. Specific LD50 values and organ-specific toxicity data are not readily available.
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| References | |
| Additional Infomation |
SPT-IN-1 (CAS# 1933533-18-6) is an orally active and potent SPT inhibitor with an IC50 of 5.19 nM for hSPT1. It can be used for type 2 diabetes and dyslipidemia research. SPT-IN-1 has potential in treating diseases associated with dysregulated sphingolipid metabolism.
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| Molecular Formula |
C22H24N2O3
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|---|---|
| Molecular Weight |
364.44
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| Exact Mass |
364.178
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| CAS # |
1933533-18-6
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| PubChem CID |
131954583
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Index of Refraction |
1.603
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| LogP |
3.78
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
27
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| Complexity |
502
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1C=C(C2C=CC(CC(O)=O)=CC=2)C2N(C=CN=2)C=1)CCCCCC
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| InChi Key |
MMYRYMMKMUTPBB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H24N2O3/c1-2-3-4-5-6-20(25)18-14-19(22-23-11-12-24(22)15-18)17-9-7-16(8-10-17)13-21(26)27/h7-12,14-15H,2-6,13H2,1H3,(H,26,27)
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| Chemical Name |
2-[4-(6-heptanoylimidazo[1,2-a]pyridin-8-yl)phenyl]acetic acid
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| Synonyms |
SPT Inhibitor 1; SPT IN 1; SPT-IN-1
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
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
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| 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
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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 : PEG300 ：Tween 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). View More
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)] 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). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7439 mL | 13.7197 mL | 27.4394 mL | |
| 5 mM | 0.5488 mL | 2.7439 mL | 5.4879 mL | |
| 10 mM | 0.2744 mL | 1.3720 mL | 2.7439 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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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