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Chemical Structure| 934369-14-9 Chemical Structure| 934369-14-9

Structure of TY-52156
CAS No.: 934369-14-9

Chemical Structure| 934369-14-9

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TY-52156 is a potent S1P3 receptor antagonist in a competitive manner, and the Ki value is estimated to be 110 nM for S1P3 receptor.

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Product Details of TY-52156

CAS No. :934369-14-9
Formula : C18H19Cl2N3O
M.W : 364.27
SMILES Code : ClC1=CC=C(/N=C(NNC2=CC=C(Cl)C=C2)/C(C(C)(C)C)=O)C=C1
MDL No. :MFCD28396419
InChI Key :XONRRGIRSGNWFP-UHFFFAOYSA-N
Pubchem ID :16046248

Safety of TY-52156

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of TY-52156

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
MNNG-HOS 10 μM TY52156 combined with methotrexate inhibited the proliferation and promoted the apoptosis of osteosarcoma cells PMC6412077
U-2OS 10 μM TY52156 combined with methotrexate inhibited the proliferation and promoted the apoptosis of osteosarcoma cells PMC6412077
TSC2-deficient cells 2 μM 24 hours TY52156 significantly reduced the viability of TSC2-deficient cells and induced cell death. PMC9772321
Bone marrow-derived macrophages (BMDMs) 0, 1, 5, 10 μM 3.5 hours To investigate the effect of TY-52156 on ATP-induced NLRP3 inflaμMasome activation, results showed that TY-52156 significantly inhibited caspase-1 cleavage and IL-1β maturation. PMC9927198
Human umbilical vein endothelial cells (HUVECs) 10 μM 48 hours TY-52156 significantly attenuated the LPS-induced increase in the percentage of apoptotic cells and decreased the levels of IL-6 and TNF-α in the supernatant and cell contents. Additionally, TY-52156 enhanced cell migration and invasion. PMC11151509
Human Pulmonary Endothelial Cells (PECs) 0.1 µM, 1 µM, 10 µM 24 hours TY-52156 was able to dose-dependently rescue the barrier-enhancing cellular response towards S1P in S1PR3 OE cells. PMC10671260
mouse renal interstitial fibroblast-like cells 10 µM 24 hours inhibition of S1P1 and S1P3 receptors, preventing sphingosine-induced HIF-2α and Epo protein increase PMC9180811
FAIK F3-5 cells 10 µM 6 hours TY-52156 completely reduced S1P-stimulated Epo mRNA expression, indicating the role of S1P 3 receptor in Epo expression PMC8430949
EpCAM CAR-T cells 10 µM 24 hours TY-52156 significantly increased CAR-T cell cytokine release of IFN-γ, IL-2, and TNF-α upon antigen stimulation. PMC10441059
4T1 cells 10 µM 24 hours TY-52156 significantly increased CAR-T cell cytokine release of IFN-γ, IL-2, and TNF-α upon antigen stimulation. PMC10441059
MC38 cells 10 µM 24 hours TY-52156 significantly increased CAR-T cell cytokine release of IFN-γ, IL-2, and TNF-α upon antigen stimulation. PMC10441059

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
nude mice subcutaneous xenograft model intraperitoneal injection 200 mg/kg Single injection TY52156 combined with methotrexate inhibited the growth of osteosarcoma PMC6412077
SCID mice TSC2-deficient cell xenograft model intraperitoneal injection 5 mg/kg twice daily for 3 days, followed by 4 days of rest, for a total of 3 cycles TY52156 significantly suppressed the growth of TSC2-deficient cell xenograft tumors and induced autophagy and apoptosis. PMC9772321
C57BL/6 mice Cecal ligation and puncture (CLP)-induced sepsis model Intraperitoneal injection 3 mg/kg every 4 days for 20 days To investigate the effect of TY-52156 on septic mice, results showed that TY-52156 increased pulmonary edema, bacterial loads, and mortality. PMC9927198
C57BL/6 mice LPS-induced acute respiratory distress syndrome (ARDS) model Intraperitoneal injection 2 mg/kg four times per week for 6 weeks TY-52156 significantly alleviated LPS-induced lung inflammation, reduced neutrophil infiltration, and decreased the levels of IL-6 and TNF-α in serum and bronchoalveolar lavage fluid. Additionally, TY-52156 restored endothelial barrier function and reduced vascular leakage. PMC11151509
C57/B6 mice Ventilator-Induced Lung Injury (VILI) model Intraperitoneal injection 10 mg/kg Single dose, 48 hours TY-52156 effectively attenuated VILI-induced increases in bronchoalveolar lavage cell counts and protein concentration, suppressed the release of pro-inflammatory cytokines, and inhibited lung inflammation as assessed via a histological evaluation. PMC10671260
mice MC38 colon cancer and 4T1 breast tumor models oral 10 mg/kg Single dose, duration of 4 hours TY-52156 significantly enhanced the antitumor activity of EpCAM CAR-T cells and prolonged the survival of mice. PMC10441059

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.75mL

0.55mL

0.27mL

13.73mL

2.75mL

1.37mL

27.45mL

5.49mL

2.75mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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