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Merck
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JN0006

Sigma-Aldrich

Draflazine

≥98% (HPLC)

Sinônimo(s):

(-)-1-[2-(4-Amino-2,6-dichloro-anilino)-2-oxo-ethyl]-4-[5,5-bis(4-fluorophenyl)pentyl]piperazine-2-carboxamide, (-)-R 75,231, (-)-R 75231, (-)-R-75231, (-)-R75231, (S)-2-(Aminocarbonyl)-N-(4-amino-2,6-dichlorophenyl)-4-[5,5-bis(4-fluorophenyl)pentyl]-1-piperazineacetamide, (S)-R 75,231, (S)-R 75231, (S)-R-75231, (S)-R75231, R 88,021, R 88021, R-88021, R88021

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About This Item

Fórmula empírica (Notação de Hill):
C30H33Cl2F2N5O2
Número CAS:
138681-29-5
Peso molecular:
604.52
Código UNSPSC:
12352200
NACRES:
NA.77

Ensaio

≥98% (HPLC)

forma

powder

atividade óptica

[α]/D -23 to -29°, c = 0.5 in ethanol

cor

white to beige

solubilidade

DMSO: 2 mg/mL, clear

temperatura de armazenamento

room temp

InChI

1S/C30H33Cl2F2N5O2/c31-25-15-23(35)16-26(32)29(25)37-28(40)18-39-14-13-38(17-27(39)30(36)41)12-2-1-3-24(19-4-8-21(33)9-5-19)20-6-10-22(34)11-7-20/h4-11,15-16,24,27H,1-3,12-14,17-18,35H2,(H2,36,41)(H,37,40)

chave InChI

IWMYIWLIESDFRZ-UHFFFAOYSA-N

Ações bioquímicas/fisiológicas

Draflazine (R88021; (-)-R75231), is a potent nucleoside transporter ENT1 (SLC29A1) inhibitor with 370-fold selectivity over ENT2 (SLC29A2). R88021 exhibits 30- and 40-times higher affinity as (+)-R75231 (R88016) using calf lung membrane preparation (by [3H]R75231 & [3H]NBI displacement) and intact human erythrocytes (by [3H]NBMPR displacement), respectively. Draflazine is 20-times more potent as R88016 in enhancing adenosine potency against ADP-induced aggregation in human whole blood (IC50 = 0.5 μM vs 10 μM with 1 μM respective inhibitor), Draflazine and R75231, but not R88016, show cardioprotective efficacy against catecholamines infusion in rabbits in vivo.

Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 3

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable

Certificados de análise (COA)

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H Van Belle et al.
Cardiovascular research, 27(1), 111-115 (1993-01-01)
R 75,231, a potent and specific nucleoside transport inhibitor, largely prevents cardiac damage and death in catecholamine challenged rabbits. The major biochemical effect of nucleoside transport inhibition in ischaemic and reperfused myocardium is a prolonged accumulation of adenosine. The cardioprotection
Nucleoside and nucleobase transport systems of mammalian cells.
D A Griffith et al.
Biochimica et biophysica acta, 1286(3), 153-181 (1996-10-29)
M W Beukers et al.
European journal of pharmacology, 266(1), 57-62 (1994-01-01)
In this study, we determined whether R75231, (+/-)-2-(aminocarbonyl)-N-(4-amino-2,6-dichlorophenyl)-4-[5,5-bis( 4-fluoro- phenyl)pentyl]-1-piperazineacetamide, and its two enantiomers, all nucleoside transport inhibitors, could play a role as anti-aggregatory agents. First, we determined the binding characteristics of [3H]nitrobenzylthioinosine, also a nucleoside transport inhibitor, on intact
J R Hammond
Naunyn-Schmiedeberg's archives of pharmacology, 361(4), 373-382 (2000-04-14)
The equilibrative nucleoside transporters of mammalian cells play an important role in the regulation of extracellular adenosine concentrations, and inhibition of these transporters potentiates the biological effects of adenosine. Two subtypes of equilibrative transporters have been defined by their differential
A P IJzerman et al.
Naunyn-Schmiedeberg's archives of pharmacology, 345(5), 558-563 (1992-05-01)
The tritiated analogue of R75231 ((+-)-2-(aminocarbonyl)-N-(4-amino-2,6-dichlorophenyl)-4-[5,5-bis (4-fluorophenyl)pentyl]-1-piperazineacetamide) has been examined as a new radioligand for (nitrobenzylthioinosine sensitive) nucleoside transport proteins. [3H]R75231 was prepared in two steps from R69064 ((+-)-4-[5,5-bis[4-fluorophenyl)-4-pentenyl]-2-piperazinecarboxamide+ ++ dihydrochloride) with a specific activity of 0.23 TBq/mmol (6.3 Ci/mmol).

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