G1421

GW405833 -hydrochlorid

≥98% (HPLC), solid

• Synonym(e): 1-(2,3-Dichlorobenzoyl)-5-methoxy-2-methyl-(3-(morpholin-4-yl)ethyl)-1H-indole -hydrochlorid
• Empirische Formel (Hill-System): C₂₃H₂₄Cl₂N₂O₃ · HCl
• CAS-Nummer: 180002-83-9
• Molekulargewicht: 483.82
• MDL-Nummer: MFCD09832650
• UNSPSC-Code: 12352200
• PubChem Substanz-ID: 329799842
• NACRES: NA.77

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥98% (HPLC)
• Form: solid
• Arzneimittelkontrolle: regulated under CDSA - not available from Sigma-Aldrich Canada
• Lagerbedingungen: desiccated
• Farbe: white to pink
• Löslichkeit: DMSO: soluble >10 mg/mL; H₂O: insoluble <2 mg/mL
• Lagertemp.: 2-8°C
• SMILES String: 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
• InChIKey: JIQYDHDVNNFPMU-UHFFFAOYSA-N

Beschreibung

Anwendung

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.

Biochem./physiol. Wirkung

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.

Leistungsmerkmale und Vorteile

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.

Sicherheitshinweise

• Piktogramme: GHS06
• Signalwort: Danger
• H-Sätze: H301 - H413
• P-Sätze: P264 - P270 - P273 - P301 + P310 - P405 - P501
• Gefahreneinstufungen: Acute Tox. 3 Oral - Aquatic Chronic 4
• Lagerklassenschlüssel: 6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable
• Persönliche Schutzausrüstung: Eyeshields, Faceshields, Gloves, type P2 (EN 143) respirator cartridges