339303-87-6

339303-87-6 structure

Name: UCLA GP130 2
Chemical Name: N-(4-Fluorophenyl)-4-phenyl-1,3-thiazol-2-amine
CAS Number: 339303-87-6
Molecular Formula: C₁₅H₁₁FN₂S
Molecular Weight: 270.325
Catalog: Signaling Pathways Immunology/Inflammation Interleukin Related
Create Date: 2021-01-11 20:33:23
Modify Date: 2024-01-04 17:33:38
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].

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

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	Signaling Pathways >> Immunology/Inflammation >> Interleukin Related Research Areas >> Neurological Disease
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.

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

Hazard Codes	Xi

339303-87-6	82212-14-4
330196-02-6	110704-48-8
61165-31-9	52600-50-7
852569-36-9	119750-08-2
915402-30-1	191349-37-8