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Chemical Structure| 1415716-58-3 Chemical Structure| 1415716-58-3

Structure of TG6-10-1
CAS No.: 1415716-58-3

Chemical Structure| 1415716-58-3

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TG6-10-1 is an antagonist of prostaglandin E2 receptor subtype EP2.

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Product Details of TG6-10-1

CAS No. :1415716-58-3
Formula : C23H23F3N2O4
M.W : 448.43
SMILES Code : O=C(NCCN1C(C(F)(F)F)=CC2=C1C=CC=C2)/C=C/C3=CC(OC)=C(OC)C(OC)=C3
MDL No. :MFCD29472234
InChI Key :WUYOECAJFJFUFC-CMDGGOBGSA-N
Pubchem ID :71499384

Safety of TG6-10-1

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H317
Precautionary Statements:P280-P305+P351+P338

Related Pathways of TG6-10-1

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
SFCOX-2 cells 10 µM 72 hours Induced cell cycle arrest and apoptosis Br J Pharmacol. 2019 Jun;176(11):1680-1699
LNCOX-2 cells 10 µM 72 hours Induced cell cycle arrest and apoptosis Br J Pharmacol. 2019 Jun;176(11):1680-1699
SF767 cells 10 µM 96 hours Inhibition of GBM cell proliferation Br J Pharmacol. 2019 Jun;176(11):1680-1699
LN229 cells 10 µM 96 hours Inhibition of GBM cell proliferation Br J Pharmacol. 2019 Jun;176(11):1680-1699
SH-SY5Y cells 20 µM 24 hours Inhibited 6-OHDA-induced cytotoxicity Sci Rep. 2017 Aug 25;7(1):9459.
Neuro-2a cells 10 or 20 µM 24 hours Inhibited 6-OHDA-induced cytotoxicity Sci Rep. 2017 Aug 25;7(1):9459.
C6 glioma (C6G) cells 0.01, 0.1, 1, or 10 µM 10 min pretreatment followed by 40 min PGE2 stimulation To evaluate TG6-10-1's antagonism of EP2 receptor. Results showed competitive antagonism with KB = 17.8 nM Proc Natl Acad Sci U S A. 2013 Feb 26;110(9):3591-6
Rat primary hippocampal neuron-glia mixed cultures 10 µM Overnight To evaluate the neuroprotective effects of TG6-10-1 against NMDA/glycine-induced excitotoxicity. Results showed that TG6-10-1 at 10 μM reduced NMDA/glycine-induced LDH release to 72%. ACS Pharmacol Transl Sci. 2020 Jun 25;3(4):635-643

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Athymic nude mice Subcutaneous tumor model Oral 10 mg/kg Twice daily for 4 weeks Inhibited subcutaneous tumor growth Br J Pharmacol. 2019 Jun;176(11):1680-1699
Mice LPS-induced systemic inflammation model Intraperitoneal injection 10 mg/kg 0.5 and 3.5 hours after LPS injection EP2 antagonist TG6-10-1 promotes the recovery of body weight, mitigates neuroinflammation, prevents the loss of synaptic proteins, and ameliorates depression-like behavior in the sucrose preference test as well as memory loss in the novel object recognition test. Brain Behav Immun Health. 2020 Aug 25;8:100132
Mice Endometriosis model Intraperitoneal injection 10 mg/kg Single dose, tested at 45 minutes post administration To test the effect of TG6-10-1 on reversing mechanical allodynia in mice with endometriosis. Results showed that TG6-10-1 significantly reversed abdominal mechanical allodynia (p < 0.05) at 45 mins post administration, but the effect on hind paw did not reach statistical significance. Sci Rep. 2017 Mar 10;7:44169
Mice Kainate-induced status epilepticus model Intraperitoneal injection 5 mg/kg Twice daily for three consecutive days To evaluate the effects of EP2 receptor inhibition on neuronal inflammation and injury following kainate-induced status epilepticus. Results showed that TG6-10-1 treatment accelerated functional recovery, reduced cytokine induction and reactive gliosis, prevented blood-brain barrier impairment, and reduced hippocampal neuronal injury. Neuropharmacology. 2019 May 1;149:149-160
C57BL/6 mice Pilocarpine-induced status epilepticus (SE) model Intraperitoneal injection 5 mg/kg Administered at 4, 21, and 30 hours post-SE onset To assess TG6-10-1's effects on delayed mortality, weight recovery, brain inflammation, blood-brain barrier disruption, and hippocampal neurodegeneration post-SE. Results showed significant reduction in mortality (from 60% to 90%), accelerated weight recovery, attenuated brain inflammation, prevented blood-brain barrier opening, and reduced hippocampal neuronal damage, without affecting acute seizures Proc Natl Acad Sci U S A. 2013 Feb 26;110(9):3591-6
Mice Status epilepticus model Intraperitoneal injection 5 mg/kg Twice daily for 2 days To evaluate the effects of TG6-10-1 on delayed mortality and functional recovery after status epilepticus. Results showed that TG6-10-1 significantly improved survival rates, accelerated weight recovery, and enhanced functional recovery. Neurobiol Dis. 2015 Apr;76:126-136
Sprague-Dawley rats DFP-induced status epilepticus model Intraperitoneal injection 5 mg/kg Six doses, first at 80-150 min after onset of DFP-induced status epilepticus, followed by doses at 5-6 h, 9-21 h, 24 h, 31-42 h, and 48 h To evaluate the effect of EP2 receptor inhibition on DFP-induced neuropathologies. Results showed that TG6-10-1 significantly reduced hippocampal neurodegeneration, blunted the inflammatory cytokine burst, reduced microglial activation, and decreased weight loss in the days after status epilepticus. Neuropharmacology. 2015 Jun;93:15-27
Sprague-Dawley rats DFP-induced status epilepticus model Intraperitoneal injection 5 mg/kg Six injections (1.5, 6, 21, 30, 45–47, and 52–55 hours after SE onset) To test whether TG6-10-1 alters DFP-induced seizure characteristics or improves cognitive function after DFP. The results showed that TG6-10-1 is not an acute anticonvulsant and does not prevent the development of seizures or SE, decrease the intensity of SE or shorten the duration of SE. TG6-10-1 treatment restored the ability to form new memories after SE. Neuropharmacology. 2016 Nov;110(Pt A):419-430
C57BL/6 mice Transient middle cerebral artery occlusion (MCAO) model Intraperitoneal injection 5 or 10 mg/kg Administered at 4.5, 12, and 24 hours after MCAO, lasting for 3 days To evaluate the effects of TG6-10-1 on neurological deficits and infarct volumes after transient MCAO. Results showed that TG6-10-1 treatment improved functional recovery, reduced cerebral infarct volumes, and downregulated the expression of proinflammatory cytokines in the brain. ACS Pharmacol Transl Sci. 2020 Jun 25;3(4):635-643
Rats Healthy rat model Intraperitoneal injection 50 mg/kg Single dose To evaluate the effect of TG6-10-1 on cardiovascular function, results showed that TG6-10-1 had no significant effect on cardiovascular parameters including heart rate (HR), systolic blood pressure (SBP), diastolic blood pressure (DBP), mean arterial pressure (MAP), pulse pressure (PP), and body temperature (BT) in rats. Biomed Pharmacother. 2022 Mar;147:112646

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.23mL

0.45mL

0.22mL

11.15mL

2.23mL

1.12mL

22.30mL

4.46mL

2.23mL

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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