G1421

GW405833 hydrochloride

≥98% (HPLC), solid

• Synonyme(s) : 1-(2,3-Dichlorobenzoyl)-5-methoxy-2-methyl-(3-(morpholin-4-yl)ethyl)-1H-indole hydrochloride
• Formule empirique (notation de Hill): C₂₃H₂₄Cl₂N₂O₃ · HCl
• Numéro CAS: 180002-83-9
• Poids moléculaire : 483.82
• Numéro MDL: MFCD09832650
• Code UNSPSC : 12352200
• ID de substance PubChem : 329799842
• Nomenclature NACRES : NA.77

Propriétés

• Pureté: ≥98% (HPLC)
• Forme: solid
• Contrôle du médicament: regulated under CDSA - not available from Sigma-Aldrich Canada
• Conditions de stockage: desiccated
• Couleur: white to pink
• Solubilité: DMSO: soluble >10 mg/mL; H₂O: insoluble <2 mg/mL
• Température de stockage: 2-8°C
• Chaîne SMILES: Cl.COc1ccc2n(c(C)c(CCN3CCOCC3)c2c1)C(=O)c4cccc(Cl)c4Cl
• InChI: 1S/C23H24Cl2N2O3.ClH/c1-15-17(8-9-26-10-12-30-13-11-26)19-14-16(29-2)6-7-21(19)27(15)23(28)18-4-3-5-20(24)22(18)25;/h3-7,14H,8-13H2,1-2H3;1H
• Clé InChI: JIQYDHDVNNFPMU-UHFFFAOYSA-N

Description

Application

GW405833 hydrochloride has been used as a lysosomal transient receptor potential mucolipin 1 (TRPML1) specific inhibitor to validate if TRPML1 mediates tau release in neurons and also to verify if it mediates the release of lysosomal tau. It has also been used as a TRPML channel blocker to study the effect of mucolipin transient receptor potential cation channel 3 (MCOLN3/TRPML3) function and trafficking on autophagy in HeLa cells.

Actions biochimiques/physiologiques

GW405833 hydrochloride, also known as ML-SI1, is a cell-permeable lysosomal transient receptor potential cation channel, mucolipin subfamily (TRPML) blocker.

GW405833 is a selective cannabanoid CB2 receptor agonist; analgesic. GW405833 binds with high affinity at both human and rat CB2 receptors (Ki′s 3.9 and 3.6 nM); acts as a partial agonist (50% inhibition of forskolin-stimulated cAMP formation compared to full agonist CP55,940). GW405833 has potent analgesic activity in rat models of inflammatory, neuropathic and incisional pain; devoid of CNS effects common with CB1 agonists.

Caractéristiques et avantages

This compound is featured on the Cannabinoid Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Informations sur la sécurité

• Pictogrammes: GHS06
• Mention d'avertissement: Danger
• Mentions de danger: H301,H413
• Conseils de prudence: P264 - P270 - P273 - P301 + P310 - P405 - P501
• Classification des risques: Acute Tox. 3 Oral - Aquatic Chronic 4
• Code de la classe de stockage: 6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable
• Équipement de protection individuelle: Eyeshields, Faceshields, Gloves, type P2 (EN 143) respirator cartridges