C199

CGS-15943

Name: CGS-15943
Brand: SIGMA

≥98% (HPLC), Adenosine receptor antagonist, solid

Sinónimos:

9-Chloro-2-(2-furanyl)-[1,2,4]triazolo[1,5-c]quinazolin-5-amine

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Fórmula empírica (notación de Hill):

C₁₃H₈ClN₅O

Número CAS:

104615-18-1

Peso molecular:

285.69

UNSPSC Code:

12352202

PubChem Substance ID:

24277704

NACRES:

NA.77

MDL number:

MFCD01529897

Assay:

≥98% (HPLC)

Form:

solid

Quality level:

100

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Nombre del producto

CGS-15943, solid

assay

≥98% (HPLC)

Quality Level

100

form

solid

color

white

solubility

DMSO: >10 mg/mL, H₂O: insoluble

storage temp.

room temp

SMILES string

Nc1nc2ccc(Cl)cc2c3nc(nn13)-c4ccco4

InChI

1S/C13H8ClN5O/c14-7-3-4-9-8(6-7)12-17-11(10-2-1-5-20-10)18-19(12)13(15)16-9/h1-6H,(H2,15,16)

InChI key

MSJODEOZODDVGW-UHFFFAOYSA-N

Gene Information

human ... ADORA1(134), ADORA2A(135), ADORA2B(136), ADORA3(140)
rat ... Adora1(29290), Adora2a(25369), Adora2b(29316)

Categorías relacionadas

Bioactive Small Molecules

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Este artículo	S4568	S6451	Z0153
Sigma-Aldrich C199 CGS-15943	Sigma-Aldrich S4568 SCH 58261	Sigma-Aldrich S6451 SCH-442416	Sigma-Aldrich Z0153 ZM 241385
assay ≥98% (HPLC)	assay ≥98% (HPLC)	assay ≥98% (HPLC)	assay ≥98% (HPLC)
form solid	form solid	form powder	form powder
Quality Level 100	Quality Level 100	Quality Level 100	Quality Level 100
storage temp. room temp	storage temp. -	storage temp. 2-8°C	storage temp. room temp
solubility DMSO: >10 mg/mL, H₂O: insoluble	solubility DMSO: soluble >10 mg/mL, H₂O: insoluble	solubility DMSO: ≥20 mg/mL	solubility DMSO: >15 mg/mL
color white	color off-white	color light tan to tan	color white to tan

Application

CGS-15943 has been used as a non-selective adenosine receptor antagonist to study its effects on the proliferation of pancreatic ductal adenocarcinoma (PDAC) cells and hepatocellular carcinoma (HCC)[1]. It has also been used as a non-selective adenosine receptor antagonist to investigate the mechanism underlying adenosine inhibition on cholangiocarcinoma (CCA) cells.[2]

Biochem/physiol Actions

CGS-15943 is a potent and non-selective adenosine receptor antagonist. It exhibits anti-carcinogenic and anti-apoptotic activity.[1]

ppe

Eyeshields, Gloves, type N95 (US)

Clase de almacenamiento

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificados de análisis (COA)

Lot/Batch Number

0000364481

0000216290

0000209086

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The adenosine receptor antagonist CGS15943 reinstates cocaine-seeking behavior and maintains self-administration in baboons.

Elise M Weerts et al.

Psychopharmacology, 168(1-2), 155-163 (2003-04-02)

Caffeine and the adenosine A(1) and A(2A) receptor antagonist CGS15943 produce many behavioral effects that are similar to those produced by classic stimulant drugs (e.g. cocaine and amphetamines). The current study evaluated whether CGS15943 would maintain self-administration and reinstate extinguished

Modeling the adenosine receptors: comparison of the binding domains of A2A agonists and antagonists.

Soo-Kyung Kim et al.

Journal of medicinal chemistry, 46(23), 4847-4859 (2003-10-31)

A three-dimensional model of the human A(2A) adenosine receptor (AR) and its docked ligands was built by homology to rhodopsin and validated with site-directed mutagenesis and the synthesis of chemically complementary agonists. Different binding modes of A(2A)AR antagonists and agonists

Adenosine A2a receptors increase arterial endothelial cell nitric oxide.

J m Li et al.

The Journal of surgical research, 80(2), 357-364 (1999-01-08)

Adenosine is a potent vasodilator of vascular smooth muscle. Endothelium-derived nitric oxide (NO) elicits vasodilation. We have previously reported that adenosine stimulates the production of NO from porcine carotid arterial endothelial cells (PCAEC) via a receptor-mediated mechanism. This study was

Direct effects of caffeine and theophylline on p110 delta and other phosphoinositide 3-kinases. Differential effects on lipid kinase and protein kinase activities.

Lazaros C Foukas et al.

The Journal of biological chemistry, 277(40), 37124-37130 (2002-07-30)

We investigated the effects of methylxanthines on enzymatic activity of phosphoinositide 3-kinases (PI3Ks). We found that caffeine inhibits the in vitro lipid kinase of class I PI3Ks (IC(50) = 75 microm for p110 delta, 400 microm for p110 alpha and

Receptor subtypes mediating adenosine-induced dilation of cerebral arterioles.

A C Ngai et al.

American journal of physiology. Heart and circulatory physiology, 280(5), H2329-H2335 (2001-04-12)

The purpose of this study was to investigate the receptor subtypes that mediate the dilation of rat intracerebral arterioles elicited by adenosine. Penetrating arterioles were isolated from the rat brain, cannulated with the use of a micropipette system, and luminally

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SKU	GTIN
C199-25MG	04061833474914

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