G1421

GW405833 -hydrochlorid

≥98% (HPLC), Selective cannabinoid CB2 receptor agonist, 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
• UNSPSC Code: 12352200
• PubChem Substance ID: 329799842
• NACRES: NA.77
• MDL number: MFCD09832650
• Assay: ≥98% (HPLC)
• Form: solid
• Storage condition: desiccated

Eigenschaften

• Produktname: GW405833 -hydrochlorid, ≥98% (HPLC), solid
• assay: ≥98% (HPLC)
• form: solid
• drug control: regulated under CDSA - not available from Sigma-Aldrich Canada
• storage condition: desiccated
• color: white to pink
• solubility: DMSO: soluble >10 mg/mL, H₂O: insoluble <2 mg/mL
• storage temp.: 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
• InChI key: JIQYDHDVNNFPMU-UHFFFAOYSA-N

Beschreibung

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.[1] 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.[2]

Biochem/physiol Actions

GW405833 hydrochloride, also known as ML-SI1, is a cell-permeable[2] lysosomal transient receptor potential cation channel, mucolipin subfamily (TRPML) blocker.[3]

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.

Selective cannabinoid CB2 receptor agonist; analgesic.

Features and Benefits

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

• pictograms: GHS06
• signalword: Danger
• hcodes: H301,H413
• pcodes: P264 - P270 - P273 - P301 + P310 - P405 - P501
• Hazard Classifications: Acute Tox. 3 Oral - Aquatic Chronic 4
• Lagerklasse: 6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable
• ppe: Eyeshields, Faceshields, Gloves, type P2 (EN 143) respirator cartridges