UCLA GP130 2

Modify Date: 2024-01-04 17:33:38

UCLA GP130 2 Structure
UCLA GP130 2 structure
Common Name UCLA GP130 2
CAS Number 339303-87-6 Molecular Weight 270.325
Density 1.3±0.1 g/cm3 Boiling Point 424.2±47.0 °C at 760 mmHg
Molecular Formula C15H11FN2S Melting Point N/A
MSDS N/A Flash Point 210.3±29.3 °C

 Use of UCLA GP130 2


GP130 receptor agonist-1 is a potent, brain-penetrant and orally active GP130 receptor agonist. GP130 receptor agonist-1 has a neuroprotective effect on NMDA-induced neurotoxicity[1].

 Names

Name N-(4-Fluorophenyl)-4-phenyl-1,3-thiazol-2-amine
Synonym More Synonyms

 UCLA GP130 2 Biological Activity

Description GP130 receptor agonist-1 is a potent, brain-penetrant and orally active GP130 receptor agonist. GP130 receptor agonist-1 has a neuroprotective effect on NMDA-induced neurotoxicity[1].
Related Catalog
In Vitro In SH-SY5Y cells, GP130 receptor agonist-1 (Compound 2) treatment showed a 2-fold increase in phosphorylation of STAT3 within 10 min at its regulatory Tyr705 site. In primary hippocampal neuronal cultures, the pSTAT3 levels are below levels of detection for GP130 receptor agonist-1 at all time points[1]. GP130 receptor agonist-1 treatment shows increases phosphorylation of AKT at its regulatory Thr308 site and phosphorylation of ERK1/2 at its regulatory Thr202/Tyr204 site in the serum free media condition in SH-SY5Y cells, and in primary cortical neurons[1].
In Vivo For GP130 receptor agonist-1 (Compound 2), mice are dosed orally at 10 or 30 mg/kg, or injected subcutaneously (SQ) at 10 mg/kg, and euthanized after 1, 2, 4, 6, and 8 h post dose. At 2 h after SQ delivery at 10 mg/kg the brain Cmax is 161 ng/g while dosing at 30 mg/kg orally, results in the brain Cmax of 156 ng/g (0.57 μM). The brain to plasma ratio for 2 is ∼4:1 for oral 30 mg/kg and ∼7.5:1 for 10 mg/kg SQ injection[1].
References

[1]. Mohammad Parvez Alam,et al. A Small Molecule Mimetic of the Humanin Peptide as a Candidate for Modulating NMDA-Induced Neurotoxicity. ACS Chem Neurosci. 2018 Mar 21;9(3):462-468.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 424.2±47.0 °C at 760 mmHg
Molecular Formula C15H11FN2S
Molecular Weight 270.325
Flash Point 210.3±29.3 °C
Exact Mass 270.062683
LogP 4.53
Vapour Pressure 0.0±1.0 mmHg at 25°C
Index of Refraction 1.660

 Safety Information

Hazard Codes Xi

 Synonyms

MFCD00784992
2-Thiazolamine, N-(4-fluorophenyl)-4-phenyl-
N-(4-Fluorophenyl)-4-phenyl-1,3-thiazol-2-amine