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Merck

C5749

Sigma-Aldrich

CGP 52608

≥98%, solid

别名:

1-[3-Allyl-4-oxo-thiazolidine-2-ylidene]-4-methyl-thiosemicarbazone, N-Methyl-2-[4-oxo-3-(2-propen-1-yl)-2-thiazolidinylidene]-hydrazinecarbothioamide

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About This Item

经验公式(希尔记法):
C8H12N4OS2
CAS号:
分子量:
244.34
MDL號碼:
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77

品質等級

化驗

≥98%

形狀

solid

溶解度

DMSO: >30 mg/mL
H2O: insoluble

儲存溫度

−20°C

SMILES 字串

CNC(=S)N\N=C1/SCC(=O)N1CC=C

InChI

1S/C8H12N4OS2/c1-3-4-12-6(13)5-15-8(12)11-10-7(14)9-2/h3H,1,4-5H2,2H3,(H2,9,10,14)/b11-8-

InChI 密鑰

DDYJDIHOSRTMSE-FLIBITNWSA-N

應用

CGP 52608 has been used as a RAR related orphan receptor α (RORα) synthetic agonist in THP-1 macrophages, in human monocyte cells THP1 and somatic testicular cells.

生化/生理作用

CGP 52608 is a thiazolidine derivative and an antiarthritic compound. It possesses immunostimulatory functionality and elicits antiproliferative effect in colon tumors. It is cytotoxic towards neural cell lines. CGP 52608 induces apoptosis in tumor and also favors G0-G1 cell cycle phase accumulation in neural cell lines.
CGP 52608 is a specific activator of retinoic acid receptor-related orphan receptor α (RORA).

特點和優勢

This compound is featured on the Nuclear Receptors (Non-Steroids) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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P T Ram et al.
Cancer letters, 179(2), 141-150 (2002-03-13)
Two putative melatonin receptors have been described including the cell surface G-protein-linked receptors, mt1 and MT2, and the nuclear retinoic orphan receptor alpha (RORalpha). The mt1 receptor, but not the MT2 receptor, is expressed in human breast tumor cell lines
J E Roberts et al.
Journal of pineal research, 28(3), 165-171 (2000-03-30)
Previous work has demonstrated that melatonin inhibits growth of cultured human uveal melanoma cells. The goal of this study was to determine the expression of mRNA encoding the melatonin receptor subtypes and the effect of specific melatonin receptor agonists on
Andrea Balla et al.
Neuropharmacology, 56(5), 915-921 (2009-04-18)
Deficits in N-methyl-D-aspartate receptor (NMDAR)-mediated neurotransmission may underlie dopaminergic hyperactivity in schizophrenia. Dysregulation of the GABAergic system has also been implicated. In this study we investigated a role for GABA(B) receptors as an intermediate step in the pathway leading from
Antonio Carrillo-Vico et al.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 17(6), 755-757 (2003-02-21)
It is well known that melatonin plays a fundamental role in human neuro-immunomodulation. Thus, melatonin regulates the production of a large number of cytokines, including interleukin-2 (IL-2) in the human system. Both membrane and nuclear receptors for melatonin are present
M Karasek et al.
Biological signals and receptors, 8(1-2), 75-78 (1999-03-23)
The antiproliferative effects of melatonin and CGP 52608, an exogenous ligand for RZR/ROR receptors, are compared in the present paper. Both compounds exerted similar inhibitory effects on the proliferation of neoplastic cells in mouse colonic adenocarcinoma, DU 145 human prostate

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