| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg | |||
| Other Sizes |
| Targets |
SPPL2a (signal peptide peptidase-like 2a). SPL-410 is a selective, hydroxyethylamine-based SPPL2a inhibitor (antagonist) that blocks the proteolytic activity of SPPL2a, a member of the signal peptide peptidase family involved in immune cell development and function.
|
|---|---|
| ln Vitro |
SPL-410 inhibits SPPL2a with an IC₅0 of 9 nM. The compound demonstrates high potency and selectivity for SPPL2a over other related proteases. It is an orally active hydroxyethylamine-based inhibitor with applications in studying immune regulation.
|
| ln Vivo |
In vivo, SPL-410 is orally bioactive and expected to demonstrate efficacy in models of immune-mediated diseases. By inhibiting SPPL2a, the compound modulates immune cell development and function. Efficacy would be assessed in models of autoimmunity, inflammation, and cancer immunotherapy where SPPL2a plays a role.
|
| Enzyme Assay |
SPPL2a enzymatic activity is measured using a fluorogenic peptide substrate assay. Recombinant SPPL2a or membrane preparations containing SPPL2a are incubated with a peptide substrate and serial dilutions of test compound. Cleavage of the substrate generates a fluorescent signal, and IC₅0 values are calculated from dose-response curves.
|
| Cell Assay |
Cells (e.g., immune cells, B cells, or dendritic cells) are treated with SPL-410 at various concentrations. SPPL2a substrate cleavage is assessed by measuring the accumulation of uncleaved substrates or the production of cleavage products. Cell viability, proliferation, and immune function (e.g., cytokine production, antigen presentation) are evaluated.
|
| Animal Protocol |
Mouse models of immune-mediated diseases (e.g., autoimmune, inflammatory, or tumor models) are administered SPL-410 orally. Disease progression is monitored by clinical scores, histopathology, and biomarker analysis. Immune cell populations in blood, spleen, and lymph nodes are characterized by flow cytometry. Efficacy is determined by disease amelioration and survival.
|
| ADME/Pharmacokinetics |
SPL-410 has a molecular weight of 500.57 g/mol and formula C24H31F3N2O4S. As an orally active compound, it is expected to have favorable oral bioavailability. Standard PK parameters would be determined in rodent studies following PO and IV administration. The compound is formulated in suitable vehicles for oral gavage.
|
| Toxicity/Toxicokinetics |
Toxicology data for SPL-410 are not publicly available. Standard preclinical safety assessment would include cytotoxicity assays, hERG channel inhibition testing, and repeat-dose toxicology studies in rodents. Given SPPL2a's role in immune function, potential immunomodulatory effects would be carefully evaluated.
|
| Additional Infomation |
SPL-410 is a research compound for studying SPPL2a biology and immune function. It is not clinically approved. The compound's hydroxyethylamine-based structure provides potent and selective SPPL2a inhibition. SPL-410 is useful for investigating the role of SPPL2a in immune cell development, autoimmunity, and cancer immunotherapy.
|
| Molecular Formula |
C24H31F3N2O4S
|
|---|---|
| Molecular Weight |
500.574156045914
|
| Exact Mass |
500.195
|
| CAS # |
2351886-00-3
|
| Related CAS # |
2351886-00-3;
|
| PubChem CID |
138911346
|
| Appearance |
White to off-white solid powder
|
| LogP |
4.8
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
34
|
| Complexity |
746
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
CC(C)(C)C1=CC=C(C=C1)S(=O)(=O)N(C[C@@H]([C@H](C2=CC=C(C=C2)OC(F)(F)F)N)O)C3CCC3
|
| InChi Key |
KEEHEUGOPCFXAV-VXKWHMMOSA-N
|
| InChi Code |
InChI=1S/C24H31F3N2O4S/c1-23(2,3)17-9-13-20(14-10-17)34(31,32)29(18-5-4-6-18)15-21(30)22(28)16-7-11-19(12-8-16)33-24(25,26)27/h7-14,18,21-22,30H,4-6,15,28H2,1-3H3/t21-,22-/m0/s1
|
| Chemical Name |
N-[(2S,3S)-3-amino-2-hydroxy-3-[4-(trifluoromethoxy)phenyl]propyl]-4-tert-butyl-N-cyclobutylbenzenesulfonamide
|
| 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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), 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)
|
| Solubility (In Vitro) |
DMSO : ~190 mg/mL (~379.57 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 4.75 mg/mL (9.49 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 47.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9977 mL | 9.9886 mL | 19.9772 mL | |
| 5 mM | 0.3995 mL | 1.9977 mL | 3.9954 mL | |
| 10 mM | 0.1998 mL | 0.9989 mL | 1.9977 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
