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G1421

Sigma-Aldrich

GW405833 hydrochloride

≥98% (HPLC), solid

Szinonimák:

1-(2,3-Dichlorobenzoyl)-5-methoxy-2-methyl-(3-(morpholin-4-yl)ethyl)-1H-indole hydrochloride, 242 hydrochloride, L-768, L-768242 hydrochloride, L768242 hydrochloride, ML-SI1 hydrochloride

Bejelentkezésa Szervezeti és Szerződéses árazás megtekintéséhez
Összes fotó(1)

About This Item

Tapasztalati képlet (Hill-képlet):
C23H24Cl2N2O3 · HCl
CAS-szám:
180002-83-9
Molekulatömeg:
483.82
MDL-szám:
MFCD09832650
UNSPSC kód:
12352200
PubChem Substance ID:
329799842
NACRES:
NA.77

Minőségi szint

100

Teszt

≥98% (HPLC)

Forma

solid

gyógyszerellenőrzés

regulated under CDSA - not available from Sigma-Aldrich Canada

tárolási körülmény

desiccated

szín

white to pink

oldhatóság

DMSO: soluble >10 mg/mL
H2O: insoluble <2 mg/mL

tárolási hőmérséklet

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

Nemzetközi kémiai azonosító kulcs

JIQYDHDVNNFPMU-UHFFFAOYSA-N

Alkalmazás

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.

Biokémiai/fiziológiai hatások

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.

Tulajdonságok és előnyök

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.

Piktogramok

Skull and crossbones
GHS06

Figyelmeztetés

Danger

Figyelmeztető mondatok

H301,H413

Óvintézkedésre vonatkozó mondatok

P264 - P270 - P273 - P301 + P310 - P405 - P501

Veszélyességi osztályok

Acute Tox. 3 Oral - Aquatic Chronic 4

Tárolási osztály kódja

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

WGK

WGK 3

Lobbanási pont (F)

Not applicable

Lobbanási pont (C)

Not applicable

Egyéni védőeszköz

Eyeshields, Faceshields, Gloves, type P2 (EN 143) respirator cartridges

Válasszon a legfrissebb verziók közül:

Analitikai tanúsítványok (COA)

Lot/Batch Number
0000379873
0000379874
0000303351
0000379874
0000379873

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Dokumentumtár megtekintése

I Dando et al.
Cell death & disease, 4, e664-e664 (2013-06-15)
The anti-tumoral effects of cannabinoids have been described in different tumor systems, including pancreatic adenocarcinoma, but their mechanism of action remains unclear. We used cannabinoids specific for the CB1 (ACPA) and CB2 (GW) receptors and metabolomic analyses to unravel the
M Donadelli et al.
Cell death & disease, 2, e152-e152 (2011-04-29)
Gemcitabine (GEM, 2',2'-difluorodeoxycytidine) is currently used in advanced pancreatic adenocarcinoma, with a response rate of < 20%. The purpose of our work was to improve GEM activity by addition of cannabinoids. Here, we show that GEM induces both cannabinoid receptor-1
Charlotte Leser et al.
European journal of medicinal chemistry, 210, 112966-112966 (2020-11-15)
The members of the TRPML subfamily of non-selective cation channels (TRPML1-3) are involved in the regulation of important lysosomal and endosomal functions, and mutations in TRPML1 are associated with the neurodegenerative lysosomal storage disorder mucolipidosis type IV. For in-depth investigation
Bethan S Kilpatrick et al.
Journal of cell science, 129(20), 3859-3867 (2016-09-01)
Transient receptor potential (TRP) mucolipins (TRPMLs), encoded by the MCOLN genes, are patho-physiologically relevant endo-lysosomal ion channels crucial for membrane trafficking. Several lines of evidence suggest that TRPMLs mediate localised Ca2+ release but their role in Ca2+ signalling is not
Yin Xu et al.
Molecular psychiatry, 26(10), 5925-5939 (2020-05-06)
Neurofibrillary tangles (NFTs) composed of hyperphosphorylated and misfolded tau protein are a pathological hallmark of Alzheimer's disease and other tauopathy conditions. Tau is predominantly an intraneuronal protein but is also secreted in physiological and pathological conditions. The extracellular tau has
View All Related Papers

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