GW 791343 hydrochloride - CAS 1019779-04-4
Catalog number:
1019779-04-4
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C20H24F2N4O.3HCl
Molecular Weight:
483.81
COA:
Inquire
Targets:
P2X Receptor
Description:
The hydrochlorie salt form of GW791343 that is a non-competitive inhibitor of human P2X7 receptors amd it seems to show species-specific activity which is probably negative allosteric modulators of the human P2X7 receptor and the agonist of the same recep
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Purity:
>99 %
Appearance:
White solid
Synonyms:
GW791343 (dihydrochloride); 1019779-04-4; 2-((3,4-Difluorophenyl)amino)-N-(2-methyl-5-(piperazin-1-ylmethyl)phenyl)acetamide dihydrochloride; GW 791343; 3075AH
Solubility:
DMSO: 42 mg/ml
Storage:
-20ºC Freeze
MSDS:
Inquire
Application:
The hydrochlorie salt form of GW791343 that is a non-competitive inhibitor of human P2X7 receptors.
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Quantity:
Milligrams-Grams
InChIKey:
WSBRAHWNJBXXJM-UHFFFAOYSA-N
InChI:
InChI=1S/C20H24F2N4O.3ClH/c1-14-2-3-15(13-26-8-6-23-7-9-26)10-19(14)25-20(27)12-24-16-4-5-17(21)18(22)11-16;;;/h2-5,10-11,23-24H,6-9,12-13H2,1H3,(H,25,27);3*1H
Canonical SMILES:
CC1=C(C=C(C=C1)CN2CCNCC2)NC(=O)CNC3=CC(=C(C=C3)F)F.Cl.Cl.Cl
1.A randomized double-blind, placebo-controlled efficacy and safety study of ALO-02 (extended-release oxycodone surrounding sequestered naltrexone) for moderate-to-severe chronic low back pain treatment.
Rauck RL1, Hale ME, Bass A, Bramson C, Pixton G, Wilson JG, Setnik B, Meisner P, Sommerville KW, Malhotra BK, Wolfram G. Pain. 2015 Sep;156(9):1660-9. doi: 10.1097/j.pain.0000000000000230.
The objective of this multicenter, double-blind, placebo-controlled, randomized withdrawal study was to evaluate the efficacy and safety of ALO-02, an abuse-deterrent formulation containing pellets of extended-release oxycodone hydrochloride (HCl) surrounding sequestered naltrexone HCl, compared with placebo in the treatment of moderate-to-severe chronic low back pain. An open-label titration period in which all patients received ALO-02 was followed by a double-blind treatment period where patients meeting treatment response criteria were randomized to either a fixed dose of ALO-02 or placebo. Daily average low back pain was assessed using an 11-point numeric rating scale (NRS)-Pain. Of the 663 patients screened, 410 received ALO-02 during the open-label conversion and titration period and 281 patients were randomized to the double-blind treatment period (n = 134, placebo; n = 147, ALO-02). Change in the mean NRS-Pain score from randomization baseline to the final 2 weeks of the treatment period was significantly different favoring ALO-02 compared with placebo (P = 0.
2.Gateways to clinical trials.
Tomillero A1, Moral MA. Methods Find Exp Clin Pharmacol. 2008 May;30(4):313-31.
11D10, 9vPnC-MnCc; Adalimumab, Adefovir dipivoxil, Alefacept, ALN-RSV01, AME-133, AMG-317, Aminolevulinic acid methyl ester, Amlodipine besylate/atorvastatin calcium, Anisodamine, Anti-IL-5 receptor antibody, Apremilast, Aripiprazole, Atacicept, Atazanavir sulfate, Atrasentan; Banoxantrone, Bevacizumab, BIBW-2992, Binodenoson, BMS-387032; cAC10, Caldaret hydrate, CD-NP, Ceftobiprole medocaril, Celivarone fumarate, Certolizumab pegol, Cholesteryl hydrophobized polysaccharide-Her2 protein complex, Choline fenofibrate, Cilengitide, Cinaciguat, Curcumin, Custirsen sodium, Cypher, CYT-6091; Dalcetrapib, Deforolimus, Desvenlafaxine succinate, DHA-paclitaxel, DP6-001; E-7010, E75, Ecogramostim, EGF-P64K, EnvPro, Enzastaurin hydrochloride, Escitalopram oxalate, Ezetimibe, Ezetimibe/simvastatin; Fenretinide; Gefitinib, Golimumab, Green tea catechins, GTI-2040, GW-406381; HPV16 E6 E7, HPV-16/18 AS04, HPV-6/11/16/18; ICC-1132, Immune globulin intravenous (human), Indacaterol, Intranasal insulin; Kahalalide F; Lactobacillus rhamnosus, Laromustine, Laropiprant, GTI-2040; MAb 3H1, Mepolizumab, Mifamurtide, Milataxel, MP4; Nebicapone, Nelarabine, Neuradiab; Oncolytic HSV; PCV7, PHX-1149, Pimecrolimus, Pralatrexate, Pramiconazole; Ranibizumab, Reolysin, Rilonacept, Rolofylline, Romidepsin; S-32865, Shigella dysenteriae 1 vaccine; Taranabant, Taxus, TZP-101; Ustekinumab; Vitespen; Zileuton, Zycure.
3.Inhibition of inducible nitric oxide synthase in respiratory diseases.
Hesslinger C1, Strub A, Boer R, Ulrich WR, Lehner MD, Braun C. Biochem Soc Trans. 2009 Aug;37(Pt 4):886-91. doi: 10.1042/BST0370886.
Nitric oxide (NO) is a key physiological mediator and disturbed regulation of NO release is associated with the pathophysiology of almost all inflammatory diseases. A multitude of inhibitors of NOSs (nitric oxide synthases) have been developed, initially with low or even no selectivity against the constitutively expressed NOS isoforms, eNOS (endothelial NOS) and nNOS (neuronal NOS). In the meanwhile these efforts yielded potent and highly selective iNOS (inducible NOS) inhibitors. Moreover, iNOS inhibitors have been shown to exert beneficial anti-inflammatory effects in a wide variety of acute and chronic animal models of inflammation. In the present mini-review, we summarize some of our current knowledge of inhibitors of the iNOS isoenzyme, their biochemical properties and efficacy in animal models of pulmonary diseases and in human disease itself. Moreover, the potential benefit of iNOS inhibition in animal models of COPD (chronic obstructive pulmonary disease), such as cigarette smoke-induced pulmonary inflammation, has not been explicitly studied so far.
4.Regulation of sphingomyelin phosphodiesterase acid-like 3A gene (SMPDL3A) by liver X receptors.
Noto PB1, Bukhtiyarov Y, Shi M, McKeever BM, McGeehan GM, Lala DS. Mol Pharmacol. 2012 Oct;82(4):719-27. Epub 2012 Jul 18.
Liver X receptor (LXR) α and LXRβ function as physiological sensors of cholesterol metabolites (oxysterols), regulating key genes involved in cholesterol and lipid metabolism. LXRs have been extensively studied in both human and rodent cell systems, revealing their potential therapeutic value in the contexts of atherosclerosis and inflammatory diseases. The LXR genome landscape has been investigated in murine macrophages but not in human THP-1 cells, which represent one of the frequently used monocyte/macrophage cell systems to study immune responses. We used a whole-genome screen to detect direct LXR target genes in THP-1 cells treated with two widely used LXR ligands [N-(2,2,2-trifluoroethyl)-N-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)-ethyl]phenyl]-benzenesulfonamide (T0901317) and 3-[3-[N-(2-chloro-3-trifluoromethylbenzyl)-(2,2-diphenylethyl)amino]propyloxy] phenylacetic acid hydrochloride (GW3965)]. This screen identified the sphingomyelin phosphodiesterase acid-like 3A (SMPDL3A) gene as a novel LXR-regulated gene, with an LXR response element within its promoter.
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CAS 1019779-04-4 GW 791343 hydrochloride

GW 791343 hydrochloride
(CAS: 1019779-04-4)

The hydrochlorie salt form of GW791343 that is a non-competitive inhibitor of human P2X7 receptors amd it seems to show species-specific activity which is proba...

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CAS 1019779-04-4 GW 791343 hydrochloride

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