SML1958

Sigma-Aldrich

BAY 60-6583

≥98% (HPLC)

Sinónimos:
BAY 606583, 2-[[6-Amino-3,5-dicyano-4-[4-(cyclopropylmethoxy)phenyl]-2-pyridinyl]thio]-acetamide, BAY606583, BAY 60–6,583, BR 4887, BR4887
Empirical Formula (Hill Notation):
C19H17N5O2S
Número de CAS:
Peso molecular:
379.44
MDL number:
En este momento no podemos mostrarle ni los precios ni la disponibilidad

Quality Level

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 20 mg/mL, clear

storage temp.

2-8°C

SMILES string

NC1=C(C#N)C(C2=CC=C(OCC3CC3)C=C2)=C(C#N)C(SCC(N)=O)=N1

Biochem/physiol Actions

BAY 60-6583 is a potent adenosine receptor A2b (A2bR) partial agonist (Ki against 0.3 nM [3H]PSB-603 for binding human/mouse/rat A2bR = 114/136/100 nM) that selectively induces cAMP-dependent transcription activity in CHO transfectants expressing human A2bR (EC50 ~100 nM), but not A1R or A2aR, while exhibiting no affinity toward human/rat/mouse A2aR. BAY 60-6583 also displays low-affinity antagonistic activity toward A1R (Ki against 1 nM [3H]CCPA for binding human/mouse/rat A1R = 387/351/514 nM; IC50 = 7.4 μM against 100 nM CCPA-induced hA1R β-arrestin recruitment) and A3R (Ki against 10 nM [3H]NECA for binding human/mouse/rat A3R = 223/3920/2750 nM; IC50 = 6.7 μM against 30 nM Cl-IB-MECA-induced hA3R β-arrestin recruitment). BAY 60-6583 is widely administered in animals in vivo via i.p. (0.1-80 mg/kg) or i.v. (0.2-2 mg/kg) for studying A2bR-mediated biological responses.

RIDADR

NONH for all modes of transport

WGK Germany

WGK 3

Flash Point F

Not applicable

Flash Point C

Not applicable

Atsushi Kuno et al.
Journal of molecular and cellular cardiology, 43(3), 262-271 (2007-07-17)
Although protein kinase C (PKC) plays a key role in ischemic preconditioning (IPC), the actual mechanism of that protection is unknown. We recently found that protection from IPC requires activation of adenosine receptors during early reperfusion. We, therefore, hypothesized that...
Tobias Eckle et al.
Circulation, 115(12), 1581-1590 (2007-03-14)
Ecto-5'-nucleotidase (CD73)-dependent adenosine generation has been implicated in tissue protection during acute injury. Once generated, adenosine can activate cell-surface adenosine receptors (A1 AR, A2A AR, A2B AR, A3 AR). In the present study, we define the contribution of adenosine to...
Mohamad Wessam Alnouri et al.
Purinergic signalling, 11(3), 389-407 (2015-07-02)
Adenosine receptors (ARs) have emerged as new drug targets. The majority of data on affinity/potency and selectivity of AR ligands described in the literature has been obtained for the human species. However, preclinical studies are mostly performed in mouse or...
Vanessa D'Antongiovanni et al.
Cells, 9(5) (2020-05-24)
The role played by adenosine A2B receptors (A2BRs) in the regulation of enteric glial cell (EGC) functions remains unclear. This study was aimed at investigating the involvement of A2BRs in the control of EGC functions in a model of obesity....

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