2. GPCR/G Protein Apoptosis
  3. Succinate Receptor 1 Apoptosis
  4. SUCNR1 antagonist-1

SUCNR1 antagonist-1 is an orally active SUCNR1 antagonist. SUCNR1 antagonist-1 forms stable, water-bridged hydrogen bonds with key residue Glu221.31 to stabilize binding conformation and modulates protein conformational flexibility. SUCNR1 antagonist-1 blocks succinate-mediated SUCNR1 signaling and induces cell apoptosis. SUCNR1 antagonist-1 can be used for the research of colorectal carcinoma.

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SUCNR1 antagonist-1

SUCNR1 antagonist-1 Chemical Structure

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SUCNR1 antagonist-1 Related Antibodies

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Description

SUCNR1 antagonist-1 is an orally active SUCNR1 antagonist. SUCNR1 antagonist-1 forms stable, water-bridged hydrogen bonds with key residue Glu221.31 to stabilize binding conformation and modulates protein conformational flexibility. SUCNR1 antagonist-1 blocks succinate-mediated SUCNR1 signaling and induces cell apoptosis. SUCNR1 antagonist-1 can be used for the research of colorectal carcinoma[1].

In Vitro

SUCNR1 antagonist-1 (Compound 26) potently and competitively inhibits SUCNR1 activity in transiently transfected HEK293 cells, with an IC50 of 11.7 nM in the Glosensor cAMP assay[1].
SUCNR1 antagonist-1 (18.0 nM; 6 h) inhibits succinate-mediated SUCNR1 signaling in transiently transfected HEK293 cells, with an IC50 of 18.0 nM in the CRE reporter assay[1].
SUCNR1 antagonist-1 (up to 30 μM; 72 h) exhibits no significant cytotoxicity toward HEK293 cells and THP-1 cells, with an IC50 >30 μM[1].
SUCNR1 antagonist-1 (0.1-10 μM; 12 h) dose-dependently inhibits succinate-induced expression of immunosuppression-related genes in THP-1 cells[1].
SUCNR1 antagonist-1 (10 μM; 72 h) reverses succinate-induced immunosuppression by THP-1 macrophages, restoring Jurkat T cell proliferation to 60.6% after 72 h coculture[1].
SUCNR1 antagonist-1 (10 μM; 5 days) remodels the immune landscape in patient-derived colorectal cancer ALI-PDTIOs, reducing immunosuppressive macrophages, expanding effector T cells, and inducing tumor cell apoptosis after 5 days of treatment[1].
SUCNR1 antagonist-1 forms stable, high-affinity interactions with SUCNR1, including unique water-bridged hydrogen bonds with Glu221.31, which enhances its binding affinity and antagonistic potency[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SUCNR1 antagonist-1 Related Antibodies

Real Time qPCR[1]

Cell Line: THP-1 human macrophage-like cells
Concentration: 0.1 μM; 1 μM; 10 μM
Incubation Time: 12 h
Result: Dose-dependently suppressed succinate-induced upregulation of multiple immunosuppression-related genes, including IL4, IL6, CHI3L1, MRC1, TREM2, CD274, IDO1, and NOS2.

Cell Proliferation Assay[1]

Cell Line: THP-1 macrophages, Jurkat T cells
Concentration: 10 μM
Incubation Time: 72 h
Result: Reversed succinate-mediated suppression of T cell proliferation, restoring proliferation from 11.7% (succinate-only treatment) to 60.6%.
Parmacokinetics
Species Dose Route Cmax Tmax T1/2 AUC0-t AUC0-∞ Vz CL MRT0-t MRT0-∞ F
Mice[1] 1.0 mg/kg i.v. 2003 ng/mL 0.08 h 1.78 h 674 ng·h/mL 683 ng·h/mL 3768 mL/kg 1467 mL/h/kg 0.39 h 0.52 h /
Mice[1] 5.0 mg/kg p.o. 2173 ng/mL 0.08 h 4.19 h 1092 ng·h/mL 1145 ng·h/mL / / 1.52 h 2.17 h 33.5 %
In Vivo

SUCNR1 antagonist-1 (Compound 26) (1.0-5.0 mg/kg; i.v., p.o.; single dose) exhibits favorable in vivo pharmacokinetic properties in male ICR mice, including an oral bioavailability of 33.5% and a half-life of 4.19 h after oral administration[1].
SUCNR1 antagonist-1 (100-300 mg/kg; p.o.; single dose) shows no significant acute toxicity in 6−8 week old C57BL/6 mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: ICR (male)[1]
Dosage: 1.0 mg/kg; 5.0 mg/kg
Administration: i.v. or p.o.; single dose
Result: Reached Cmax = 2003 ng/mL, Tmax = 0.08 h, t1/2 = 1.78 h, AUC0-t = 674 ng·h/mL, AUC0-∞ = 683 ng·h/mL, Vz = 3768 mL/kg, CL = 1467 mL/h/kg, MRT0-t = 0.39 h, MRT0-∞ = 0.52 h following i.v. administration.
Reached Cmax = 2173 ng/mL, Tmax = 0.08 h, t1/2 = 4.19 h, AUC0-t = 1092 ng·h/mL, AUC0-∞ = 1145 ng·h/mL, MRT0-t = 1.52 h, MRT0-∞ = 2.17 h, and oral bioavailability = 33.5% following p.o. administration.
Animal Model: C57BL/6 (6−8 weeks old)[1]
Dosage: 100 mg/kg; 300 mg/kg
Administration: p.o.; single dose
Result: Showed no significant alterations in body weight over 1 week post-administration.
Exhibited no noticeable morphological changes in major organs (heart, liver, spleen, lung, kidney) via H&E staining histological analysis.
Molecular Weight

411.45

Formula

C26H21NO4
SMILES

COC1=CC2=CC(C3=CC(C(NC4=CC=CC=C4CC(O)=O)=O)=CC=C3)=CC=C2C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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SUCNR1 antagonist-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SUCNR1 antagonist-1Succinate Receptor 1ApoptosisSUCNR1GPR91 cytotoxic T cellsHEK293 cellsmacrophagesTHP-1 cellsICR micesuccinateJurkat T cellGlu221.31colorectal carcinomaInhibitorinhibitorinhibit

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