We provide robust and sensitive in vitro screening and characterization platforms for accelerating the discovery and screening of potential therapies for immunosuppression. Our services offer comprehensive evaluation of candidate compounds, focusing on their ability to modulate immune cell signaling, receptor activity, and downstream effector functions. Key targets for immunosuppression include arrestin-mediated signaling pathways, G protein-coupled receptor (GPCR) activity, and cancer cell immune interactions. We can assess pathological processes such as immune cell activation, signal transduction alterations, and tumor-induced immune evasion.
Our in vitro testing suite employs a diverse range of cellular and molecular assays to evaluate immunosuppressive activity. These methods enable precise characterization of drug candidates' mechanisms of action and potency by measuring receptor engagement, signaling events, and functional cellular outcomes.
Arrestin protease recruitment assay: Measures the recruitment of arrestin proteins to activated receptors, providing insights into GPCR signaling modulation and arrestin-biased signaling relevant to immune regulation.
Bioluminescence resonance energy transfer (BRET) assay: Quantifies real-time protein-protein interactions and receptor activation in live cells, allowing detailed analysis of signaling cascades implicated in immunosuppression.
LLC Lewis murine lung carcinoma cells: Utilizes a cancer cell line model to evaluate the immunomodulatory effects of compounds on tumor-immune interactions, supporting translational relevance for immunosuppressive therapies.
[35S]-GTPgammaS binding assay: Assesses G-protein activation by measuring the binding of radiolabeled GTP analog, enabling quantification of receptor-mediated signal transduction critical for immune cell function.
We quantify critical pharmacological parameters that characterize compound efficacy, potency, and minimal effective or detectable concentrations. These metrics help to define dose-response relationships, optimize candidate selection, and support translational assessment for immunosuppressive drug development.
MEC (Minimum Effective Concentration): The lowest concentration of a compound that produces a measurable biological effect, crucial for determining starting doses and therapeutic windows.
MED (Minimum Effective Dose): The smallest dose required to achieve a significant pharmacological response, informing dosing strategies and safety margins.
pEC-50: The negative logarithm of the EC50 value, representing compound potency; a higher pEC-50 indicates greater potency, aiding in the comparison and ranking of candidate agents.
The Cd80 molecule plays a pivotal role in T cell activation and immune regulation, making it a crucial target in immunosuppression drug development. Our Cd80 testing service utilizes LLC Lewis murine lung carcinoma cells to evaluate drug effects on Cd80-mediated pathways. Key parameters assessed include Minimum Effective Concentration (MEC), enabling precise measurement of a compound’s immunosuppressive efficacy, essential for optimizing therapeutic candidates.
| Pharmacological Activity | Material | Method | Parameter |
|---|---|---|---|
| Integrin CD80 expression, induction | Dendritic cells (bone marrow-derived), mouse (CD11c+) (granulocyte/macrophage colony-stimulating factor-stimulated) | LLC Lewis murine lung carcinoma cells | MEC |
The Cd86 molecule is a critical costimulatory protein involved in T cell activation and immune response modulation, making it a key target in immunosuppression drug development. Testing Cd86 expression using LLC Lewis murine lung carcinoma cells enables precise evaluation of drug effects on immune pathways. The primary parameter assessed is the Minimum Effective Concentration (MEC), providing essential data for optimizing immunosuppressive therapies.
| Pharmacological Activity | Material | Method | Parameter |
|---|---|---|---|
| Integrin CD86 expression, induction | Dendritic cells (bone marrow-derived), mouse (CD11c+) (granulocyte/macrophage colony-stimulating factor-stimulated) | LLC Lewis murine lung carcinoma cells | MEC |
Our Sphingosine-1-Phosphate Receptor 1 (S1PR1) testing service supports immunosuppression drug development by evaluating compounds targeting S1PR1, a key regulator of lymphocyte trafficking and immune response. Using advanced methods—including Bioluminescence Resonance Energy Transfer (BRET) assay, [35S]-GTPγS binding assay, and arrestin protease recruitment assay—we assess functional activity. Main parameters measured are pEC50 (potency) and MED (minimal effective dose), enabling precise characterization of candidate drugs.
| Pharmacological Activity | Material | Method | Parameter |
|---|---|---|---|
| G-Protein (alpha-i1 subunit) activation, induction | CHO Chinese hamster ovary cells transfected with human (C206A-mutated) S1P1 receptor | Bioluminescence resonance energy transfer (BRET) assay | pEC-50 |
| G-Protein (alpha-i1 subunit) activation, induction | CHO Chinese hamster ovary cells transfected with human (E294A-mutated) S1P1 receptor | Bioluminescence resonance energy transfer (BRET) assay | pEC-50 |
| G-Protein (alpha-i1 subunit) activation, induction | CHO Chinese hamster ovary cells transfected with human (F125A-mutated) S1P1 receptor | Bioluminescence resonance energy transfer (BRET) assay | pEC-50 |
| G-Protein (alpha-i1 subunit) activation, induction | CHO Chinese hamster ovary cells transfected with human (F210A-mutated) S1P1 receptor | Bioluminescence resonance energy transfer (BRET) assay | pEC-50 |
| G-Protein (alpha-i1 subunit) activation, induction | CHO Chinese hamster ovary cells transfected with human (K34A-mutated) S1P1 receptor | Bioluminescence resonance energy transfer (BRET) assay | pEC-50 |
| G-Protein (alpha-i1 subunit) activation, induction | CHO Chinese hamster ovary cells transfected with human (L128A-mutated) S1P1 receptor | Bioluminescence resonance energy transfer (BRET) assay | pEC-50 |
| G-Protein (alpha-i1 subunit) activation, induction | CHO Chinese hamster ovary cells transfected with human (L174A-mutated) S1P1 receptor | Bioluminescence resonance energy transfer (BRET) assay | pEC-50 |
| G-Protein (alpha-i1 subunit) activation, induction | CHO Chinese hamster ovary cells transfected with human (L195A-mutated) S1P1 receptor | Bioluminescence resonance energy transfer (BRET) assay | pEC-50 |
| G-Protein (alpha-i1 subunit) activation, induction | CHO Chinese hamster ovary cells transfected with human (L272A-mutated) S1P1 receptor | Bioluminescence resonance energy transfer (BRET) assay | pEC-50 |
| G-Protein (alpha-i1 subunit) activation, induction | CHO Chinese hamster ovary cells transfected with human (L297A-mutated) S1P1 receptor | Bioluminescence resonance energy transfer (BRET) assay | pEC-50 |
| G-Protein (alpha-i1 subunit) activation, induction | CHO Chinese hamster ovary cells transfected with human (M124A-mutated) S1P1 receptor | Bioluminescence resonance energy transfer (BRET) assay | pEC-50 |
| G-Protein (alpha-i1 subunit) activation, induction | CHO Chinese hamster ovary cells transfected with human (R120A-mutated) S1P1 receptor | Bioluminescence resonance energy transfer (BRET) assay | pEC-50 |
| G-Protein (alpha-i1 subunit) activation, induction | CHO Chinese hamster ovary cells transfected with human (S105A-mutated) S1P1 receptor | Bioluminescence resonance energy transfer (BRET) assay | pEC-50 |
| G-Protein (alpha-i1 subunit) activation, induction | CHO Chinese hamster ovary cells transfected with human (S129A-mutated) S1P1 receptor | Bioluminescence resonance energy transfer (BRET) assay | pEC-50 |
| G-Protein (alpha-i1 subunit) activation, induction | CHO Chinese hamster ovary cells transfected with human (T109A-mutated) S1P1 receptor | Bioluminescence resonance energy transfer (BRET) assay | pEC-50 |
| G-Protein (alpha-i1 subunit) activation, induction | CHO Chinese hamster ovary cells transfected with human (V194A-mutated) S1P1 receptor | Bioluminescence resonance energy transfer (BRET) assay | pEC-50 |
| G-Protein (alpha-i1 subunit) activation, induction | CHO Chinese hamster ovary cells transfected with human (W269A-mutated) S1P1 receptor | Bioluminescence resonance energy transfer (BRET) assay | pEC-50 |
| G-Protein (alpha-i1 subunit) activation, induction | CHO Chinese hamster ovary cells transfected with human (Y29A-mutated) S1P1 receptor | Bioluminescence resonance energy transfer (BRET) assay | pEC-50 |
| G-Protein (alpha-i1 subunit) activation, induction | CHO Chinese hamster ovary cells transfected with human S1P1 receptor | Bioluminescence resonance energy transfer (BRET) assay | pEC-50 |
| G-Protein (receptor-linked) activation, induction | CHO Chinese hamster ovary cells transfected with human (C206A-mutated) S1P1 receptor | Arrestin protease recruitment assay | pEC-50 |
| G-Protein (receptor-linked) activation, induction | CHO Chinese hamster ovary cells transfected with human (E294A-mutated) S1P1 receptor | Arrestin protease recruitment assay | pEC-50 |
| G-Protein (receptor-linked) activation, induction | CHO Chinese hamster ovary cells transfected with human (F210A-mutated) S1P1 receptor | Arrestin protease recruitment assay | pEC-50 |
| G-Protein (receptor-linked) activation, induction | CHO Chinese hamster ovary cells transfected with human (K34A-mutated) S1P1 receptor | Arrestin protease recruitment assay | pEC-50 |
| G-Protein (receptor-linked) activation, induction | CHO Chinese hamster ovary cells transfected with human (L174A-mutated) S1P1 receptor | Arrestin protease recruitment assay | pEC-50 |
| G-Protein (receptor-linked) activation, induction | CHO Chinese hamster ovary cells transfected with human (L195A-mutated) S1P1 receptor | Arrestin protease recruitment assay | pEC-50 |
| G-Protein (receptor-linked) activation, induction | CHO Chinese hamster ovary cells transfected with human (L297A-mutated) S1P1 receptor | Arrestin protease recruitment assay | pEC-50 |
| G-Protein (receptor-linked) activation, induction | CHO Chinese hamster ovary cells transfected with human (S105A-mutated) S1P1 receptor | Arrestin protease recruitment assay | pEC-50 |
| G-Protein (receptor-linked) activation, induction | CHO Chinese hamster ovary cells transfected with human (S129A-mutated) S1P1 receptor | Arrestin protease recruitment assay | pEC-50 |
| G-Protein (receptor-linked) activation, induction | CHO Chinese hamster ovary cells transfected with human (T109A-mutated) S1P1 receptor | Arrestin protease recruitment assay | pEC-50 |
| G-Protein (receptor-linked) activation, induction | CHO Chinese hamster ovary cells transfected with human (V194A-mutated) S1P1 receptor | Arrestin protease recruitment assay | pEC-50 |
| G-Protein (receptor-linked) activation, induction | CHO Chinese hamster ovary cells transfected with human (Y29A-mutated) S1P1 receptor | Arrestin protease recruitment assay | pEC-50 |
| G-Protein (receptor-linked) activation, induction | CHO Chinese hamster ovary cells transfected with human S1P1 receptor | Arrestin protease recruitment assay | pEC-50 |
| G-Protein (receptor-linked) activation, inhibition | Amygdala, mouse (male) (SEW2871-treated) | [35S]-GTPgammaS binding assay | MED |
| G-Protein (receptor-linked) activation, inhibition | Amygdala, mouse (male) (chronic constriction injury) (SEW2871-treated) | [35S]-GTPgammaS binding assay | MED |
| G-Protein (receptor-linked) activation, inhibition | Amygdala, mouse (male) (chronic constriction injury) (sphingosine 1-phosphate-treated) | [35S]-GTPgammaS binding assay | MED |
| G-Protein (receptor-linked) activation, inhibition | Amygdala, mouse (male) (sphingosine 1-phosphate-treated) | [35S]-GTPgammaS binding assay | MED |
| G-Protein (receptor-linked) activation, inhibition | Caudate, mouse (male) (SEW2871-treated) | [35S]-GTPgammaS binding assay | MED |
| G-Protein (receptor-linked) activation, inhibition | Caudate, mouse (male) (chronic constriction injury) (SEW2871-treated) | [35S]-GTPgammaS binding assay | MED |
| G-Protein (receptor-linked) activation, inhibition | Caudate, mouse (male) (chronic constriction injury) (sphingosine 1-phosphate-treated) | [35S]-GTPgammaS binding assay | MED |
| G-Protein (receptor-linked) activation, inhibition | Caudate, mouse (male) (sphingosine 1-phosphate-treated) | [35S]-GTPgammaS binding assay | MED |
| G-Protein (receptor-linked) activation, inhibition | Cerebellum, mouse (male) (SEW2871-treated) | [35S]-GTPgammaS binding assay | MED |
| G-Protein (receptor-linked) activation, inhibition | Cerebellum, mouse (male) (chronic constriction injury) (SEW2871-treated) | [35S]-GTPgammaS binding assay | MED |
| G-Protein (receptor-linked) activation, inhibition | Cerebellum, mouse (male) (chronic constriction injury) (sphingosine 1-phosphate-treated) | [35S]-GTPgammaS binding assay | MED |
| G-Protein (receptor-linked) activation, inhibition | Cerebellum, mouse (male) (sphingosine 1-phosphate-treated) | [35S]-GTPgammaS binding assay | MED |
| G-Protein (receptor-linked) activation, inhibition | Corpus callosum, mouse (male) (SEW2871-treated) | [35S]-GTPgammaS binding assay | MED |
| G-Protein (receptor-linked) activation, inhibition | Corpus callosum, mouse (male) (chronic constriction injury) (SEW2871-treated) | [35S]-GTPgammaS binding assay | MED |
| G-Protein (receptor-linked) activation, inhibition | Corpus callosum, mouse (male) (chronic constriction injury) (sphingosine 1-phosphate-treated) | [35S]-GTPgammaS binding assay | MED |
| G-Protein (receptor-linked) activation, inhibition | Corpus callosum, mouse (male) (sphingosine 1-phosphate-treated) | [35S]-GTPgammaS binding assay | MED |
| G-Protein (receptor-linked) activation, inhibition | Cortex (cingulate), mouse (male) (SEW2871-treated) | [35S]-GTPgammaS binding assay | MED |
| G-Protein (receptor-linked) activation, inhibition | Cortex (cingulate), mouse (male) (chronic constriction injury) (SEW2871-treated) | [35S]-GTPgammaS binding assay | MED |
| G-Protein (receptor-linked) activation, inhibition | Cortex (cingulate), mouse (male) (chronic constriction injury) (sphingosine 1-phosphate-treated) | [35S]-GTPgammaS binding assay | MED |
| G-Protein (receptor-linked) activation, inhibition | Cortex (cingulate), mouse (male) (sphingosine 1-phosphate-treated) | [35S]-GTPgammaS binding assay | MED |
| G-Protein (receptor-linked) activation, inhibition | Fimbria, mouse (male) (SEW2871-treated) | [35S]-GTPgammaS binding assay | MED |
| G-Protein (receptor-linked) activation, inhibition | Fimbria, mouse (male) (chronic constriction injury) (SEW2871-treated) | [35S]-GTPgammaS binding assay | MED |
| G-Protein (receptor-linked) activation, inhibition | Fimbria, mouse (male) (chronic constriction injury) (sphingosine 1-phosphate-treated) | [35S]-GTPgammaS binding assay | MED |
| G-Protein (receptor-linked) activation, inhibition | Fimbria, mouse (male) (sphingosine 1-phosphate-treated) | [35S]-GTPgammaS binding assay | MED |
| G-Protein (receptor-linked) activation, inhibition | Hippocampus, mouse (male) (SEW2871-treated) | [35S]-GTPgammaS binding assay | MED |
| G-Protein (receptor-linked) activation, inhibition | Hippocampus, mouse (male) (chronic constriction injury) (SEW2871-treated) | [35S]-GTPgammaS binding assay | MED |
| G-Protein (receptor-linked) activation, inhibition | Hippocampus, mouse (male) (chronic constriction injury) (sphingosine 1-phosphate-treated) | [35S]-GTPgammaS binding assay | MED |
| G-Protein (receptor-linked) activation, inhibition | Hippocampus, mouse (male) (sphingosine 1-phosphate-treated) | [35S]-GTPgammaS binding assay | MED |
| G-Protein (receptor-linked) activation, inhibition | Midbrain periaqueductal gray, mouse (male) (SEW2871-treated) | [35S]-GTPgammaS binding assay | MED |
| G-Protein (receptor-linked) activation, inhibition | Midbrain periaqueductal gray, mouse (male) (chronic constriction injury) (SEW2871-treated) | [35S]-GTPgammaS binding assay | MED |
| G-Protein (receptor-linked) activation, inhibition | Midbrain periaqueductal gray, mouse (male) (chronic constriction injury) (sphingosine 1-phosphate-treated) | [35S]-GTPgammaS binding assay | MED |
| G-Protein (receptor-linked) activation, inhibition | Midbrain periaqueductal gray, mouse (male) (sphingosine 1-phosphate-treated) | [35S]-GTPgammaS binding assay | MED |
Make Order
Experimental Scheme
Implementation
Conclusion