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TG6-10-1

Cat. No. M8900
TG6-10-1 Structure
Synonym:

TP-6101

Size Price Availability Quantity
10mg USD 200 In stock
50mg USD 850 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

TG6-10-1 is an EP2 antagonist, shows low-nanomolar antagonist activity against only EP2, >300-fold selectivity over human EP3, EP4, and IP receptors, 100-fold selectivity over EP1 receptors.

In vitro: TG6-10-1, an analog of TG4-155 (a prostaglandin receptor EP2 antagonist, with a relatively short plasma half-life (0.6 h) and low brain: plasma ratio (0.3) after systemic administration in mice), which has a superior pharmacokinetic profile making it suitable for more extensive testing. TG6-10-1 had negligible effect on a panel of 40 enzymes, ion channels, receptors, and neurotransmitter transporters (IC50s > 10 μM), except that TG6-10-1 weakly inhibited the serotonin 5-hydroxytryptamine 2B (5-HT2B) receptor with IC50 = 7.5 μM. At a high concentration (10 μM), TG6-10-1 had little or no effect on the enzymatic activity of COX-1 (7% inhibition) and COX-2 (14% inhibition), and inhibited the leukotriene B4 (LTB4) receptor BLT1 by 1%. TG6-10-1 has a competitive mechanism of antagonism of the EP2 receptor with an equilibrium dissociation constant for the antagonist-receptor complex (KB) of 17.8 nM.

In vivo: TG6-10-1 displayed a plasma half-life of 1.6 h and a brain: plasma ratio of 1.6 after systemic administration (5 mg/kg, i.p.) in mice.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 448.43
Formula C23H23F3N2O4
CAS Number 1415716-58-3
Purity >98%
Solubility DMSO 10 mM
Storage at -20°C
References

Inhibition of the prostaglandin EP2 receptor is neuroprotective and accelerates functional recovery in a rat model of organophosphorus induced status epilepticus.
Rojas A, et al. Neuropharmacology. 2015 Jun;93:15-27. PMID: 25656476.

Inhibition of the prostaglandin receptor EP2 following status epilepticus reduces delayed mortality and brain inflammation.
Jiang J, et al. Proc Natl Acad Sci U S A. 2013 Feb 26;110(9):3591-6. PMID: 23401547.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: TG6-10-1, TP-6101 supplier, 5-HT Receptor, inhibitors

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