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GW791343 trihydrochloride

Catalog No. T6526 CAS 309712-55-8

Synonyms: GW791343 3HCl

GW791343 trihydrochloride (GW791343 3HCl) is aHCl salt form of GW791343, which is a non-competitive allosteric modulator of human P2X7 receptor inhibitor with pIC50 of 7.

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GW791343 trihydrochloride Chemical Structure

GW791343 trihydrochloride, CAS 309712-55-8

Pack Size	Availability	Price/USD
5 mg	6-8 weeks	$ 72.00
10 mg	6-8 weeks	$ 123.00
25 mg	6-8 weeks	$ 221.00
100 mg	6-8 weeks	$ 853.00
1 mL * 10 mM (in DMSO)	6-8 weeks	$ 87.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

Storage & Solubility Information

Description	GW791343 trihydrochloride (GW791343 3HCl) is aHCl salt form of GW791343, which is a non-competitive allosteric modulator of human P2X7 receptor inhibitor with pIC50 of 7.
Targets&IC50	P2X7:7（pIC50）
In vitro	Synephrine (0.1-30 μM) displays potent vasoconstrictive effects on isolated rat aorta in a dose dependent manner, which can be significantly inhibited by pretreatment with prazosin, BRL15572, and ketanserin but not by pretreatment with SB216641 and propranolol, indicating that Synephrine exerts the constrictive effects via adrenergic alpha(1)-receptors, serotonergic 5-HT(1D) receptors, and 5-HT(2A) receptors. [2] Although the Ki values of Synephrine, 1R,2S-norephedrine, and β-phenethylamine are same for all three subtypes, only Synephrine is a partial agonist of α1A-AR subtype stably expressed in HEK 293 cells with EC50 of 4 μM, giving a maximal response at 100 μM that is equal to 55.3 % of the L-phenylephrine maximum. Functional studies on the α2A- and α2C-AR subtypes stably expressed in CHO cells indicate that Synephrine may act as an antagonist rather than an agonist of the pre-synaptic α(2A)- and α(2C)-AR subtypes present in nerve terminals, although antagonist activity of synephrine is lower than its partial agonist potency. [3] Synephrine (~100 μM) treatment increases basal glucose consumption up to 50% over the control in a dose-dependent manner, without affecting the viability of L6 skeletal muscle cells. Synephrine significantly stimulates the basal- or insulin-stimulated lactic acid production as well as glucose consumption. Synephrine treatment stimulates the phosphorylation of AMPK but not Akt, and Synephrine-induced glucose consumption and the translocation of Glut4 from the cytoplasm to the plasma membrane are sensitive to the inhibition of AMPK but not to the inhibition of PI3 kinase. [4]

Synonyms	GW791343 3HCl
Molecular Weight	483.81
Formula	C20H24F2N4O·3HCl
CAS No.	309712-55-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 48.4 mg/mL(100 mM)

References and Literature

1. Michel AD, et al. Br J Pharmacol. 2009 Apr;156(8):1312-25. 2. Michel AD, et al. Br J Pharmacol. 2008 Nov;155(5):738-51.

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Keywords

GW791343 trihydrochloride 309712-55-8 Membrane transporter/Ion channel Neuroscience P2X Receptor GW791343 3HCl neurological disease P2XRs GW 791343 GW791343 Trihydrochloride GW 791343 Trihydrochloride Inhibitor inhibit GW-791343 Trihydrochloride GW-791343 trihydrochloride SCN cells depressive disorder GW791343 ATP GW-791343 inhibitor

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