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Chemical Structure| 1672665-49-4 Chemical Structure| 1672665-49-4

Structure of PT-2385
CAS No.: 1672665-49-4

Chemical Structure| 1672665-49-4

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PT-2385 is a selective HIF-2α inhibitor with a Ki of less than 50 nM.

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Product Details of PT-2385

CAS No. :1672665-49-4
Formula : C17H12F3NO4S
M.W : 383.34
SMILES Code : N#CC1=CC(F)=CC(OC2=CC=C(S(=O)(C)=O)C3=C2CC(F)(F)[C@H]3O)=C1
MDL No. :MFCD28963916
InChI Key :ONBSHRSJOPSEGS-INIZCTEOSA-N
Pubchem ID :91754484

Safety of PT-2385

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of PT-2385

epigenetics

Isoform Comparison

Biological Activity

Description
PT-2385 is a selective inhibitor of HIF-2α, with a Ki value of less than 50 nM[1][2].

In Vitro:

Cell Line
Concentration Treated Time Description References
RA FLS 5, 10, 20 μM 24 hours Inhibition of HIF-2α significantly reduced CD70 expression and ROS levels in RA FLS PMC8877612
HepG2 20 μM 48 hours PT-2385 significantly enhanced sorafenib efficacy to suppress HCC cell invasion PMC5680567
SKhep1 20 μM 48 hours PT-2385 significantly enhanced sorafenib efficacy to suppress HCC cell invasion PMC5680567
pituitary tumor (GH3) cells 3 µM 1 minute PT-2385 inhibited the delayed rectifier potassium current (IK(DR)) in GH3 cells, manifested as a reduction in current amplitude and an increase in inactivation rate. PMC8398179
human 13-06-MG glioma cells 3 µM 1 minute PT-2385 inhibited the delayed rectifier potassium current (IK(DR)) in human 13-06-MG glioma cells, manifested as a reduction in current amplitude. PMC8398179
HCT116 cells 10 μM 24 hours PT2385 treatment completely abolished the induction of Neu3 under hypoxia, accompanied by decreased expression of the HIF-2α target gene DMT1 and DCYTB mRNAs. PMC6410352
SμMC7721 10 μM PT2385 inhibited the proliferation of SμMC7721 cells PMC6859620

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Oxygen-Induced Retinopathy (OIR) Model Oral Gavage 2 mg/kg (1st week) and 1 mg/kg (2nd week) daily for 2 weeks Inhibiting HIF-2α expression, reducing retinal neovascularization PMC8890718
Nude mice Intrahepatic injection of SKhep1-luc cells in nude mice Intraperitoneal injection 30 mg/kg Once daily for 5 consecutive days PT-2385 combined with sorafenib significantly increased efficacy by suppressing HIF-2α and increasing AR PMC5680567
mice Irp2−/− mice intraperitoneally 10 mg/kg/day daily for 40 days To investigate the effect of PT-2385 on neurodegenerative symptoms in Irp2?/? mice, it was found that PT-2385 significantly improved behavioral performance, alleviated neurodegenerative symptoms, and reversed the shift of energy metabolism from glycolysis to oxidative phosphorylation. PMC8525628
mice high-fat diet-induced obesity and hepatic steatosis mouse model oral 0.4 mg/kg every other day for 1 month PT2385 substantially prevented HFD-induced body-weight increase and insulin resistance in Hif2afl/fl mice, but not in Hif2aΔIE mice. PMC6410352
mice subcutaneous xenograft model oral 20 mg/kg once daily for 4 weeks PT2385 significantly inhibited tumor growth and was dependent on YTHDF2 expression PMC6859620
Mice OIR model Oral 2 mmol/L, 30 μL/kg Single administration 2 hours before SAH induction To investigate the inhibitory effect of PT2385 on retinal neovascularization in the OIR model in mice PMC8203455

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.61mL

0.52mL

0.26mL

13.04mL

2.61mL

1.30mL

26.09mL

5.22mL

2.61mL

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
Protocol 2

References

 

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