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Merck
모든 사진(1)

주요 문서

SML2311

Sigma-Aldrich

BAY 60-7550

≥95% (HPLC)

동의어(들):

2-(3,4-Dimethoxybenzyl)-7-{(1R)-1-[(1R)-1-hydroxyethyl]-4-phenylbutyl}-5-methyllimidazo[5,1-f][1,2,4]triazin-4(3H)-one, BAY-60−7550, BAY60-7550

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About This Item

실험식(Hill 표기법):
C27H32N4O4
CAS Number:
Molecular Weight:
476.57
MDL number:
UNSPSC 코드:
12352200
NACRES:
NA.77

분석

≥95% (HPLC)

양식

powder

색상

white to light brown

solubility

DMSO: 2 mg/mL, clear

저장 온도

−20°C

InChI

1S/C27H32N4O4/c1-17-25-27(33)29-24(16-20-13-14-22(34-3)23(15-20)35-4)30-31(25)26(28-17)21(18(2)32)12-8-11-19-9-6-5-7-10-19/h5-7,9-10,13-15,18,21,32H,8,11-12,16H2,1-4H3,(H,29,30,33)/t18-,21+/m1/s1

InChI key

MYTWFJKBZGMYCS-NQIIRXRSSA-N

생화학적/생리학적 작용

BAY 60-7550 is an orally active, potent and selective cGMP-dependent phosphodiesterase PDE2 (PDE2A) inhibitor (human/bovine PDE2 IC50 = 4.7/2.0 nM; bovine PDE1 IC50 = 108 nM, human PDE5/5A/10A/4B IC50 = 240/580/704/940/1830 nM, human PDE3B/7B/8A/9A/11A IC50 >4 μM) with little activity (IC50 >10 μM) toward acetylcholinesterase, mAO-A/B, adenosine deaminase, and many receptor subtypes tested. Bay 60-7550 effectively upregulates cGMP and cAMP level in cultured rat and murine neurons (1 nM-1 μM) exposed to guanylyl cyclase (GC) or adenylyl cyclase (AC) stimulator (1 μM Bay 41-8543 or 2 μM forskolin), respectively, as well as exhibits learning and memory-improving efficacy in rats (0.6-3 mg/kg p.o.) and mice (0.3-1 mg/kg p.o.) in vivo.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


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시험 성적서(COA)

Lot/Batch Number

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문서 라이브러리 방문

Ligia Mendes Soares et al.
The European journal of neuroscience, 45(4), 510-520 (2016-11-05)
Cognitive and affective impairments are the most characterized consequences following cerebral ischemia. BAY 60-7550, a selective phosphodiesterase type 2 inhibitor (PDE2-I), presents memory-enhancing and anxiolytic-like properties. The behavioral effects of BAY 60-7550 have been associated with its ability to prevent
Stefania Monterisi et al.
eLife, 6 (2017-05-04)
cAMP/PKA signalling is compartmentalised with tight spatial and temporal control of signal propagation underpinning specificity of response. The cAMP-degrading enzymes, phosphodiesterases (PDEs), localise to specific subcellular domains within which they control local cAMP levels and are key regulators of signal
Remi Neviere et al.
International journal of molecular sciences, 17(12) (2016-12-16)
Adrenergic receptors couple to Gs-proteins leading to transmembrane adenylyl cyclase activation and cytosolic cyclic adenosine monophosphate (cAMP) production. Cyclic AMP is also produced in the mitochondrial matrix, where it regulates respiration through protein kinase A (PKA)-dependent phosphorylation of respiratory chain
Juen Zhang et al.
Cell, 166(3), 716-728 (2016-07-19)
Fear behaviors are regulated by adaptive mechanisms that dampen their expression in the absence of danger. By studying circuits and the molecular mechanisms underlying this adaptive response, we show that cholinergic neurons of the medial habenula reduce fear memory expression
Hege E Larsen et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 36(33), 8562-8573 (2016-08-19)
Hypertension is associated with impaired nitric oxide (NO)-cyclic nucleotide (CN)-coupled intracellular calcium (Ca(2+)) homeostasis that enhances cardiac sympathetic neurotransmission. Because neuronal membrane Ca(2+) currents are reduced by NO-activated S-nitrosylation, we tested whether CNs affect membrane channel conductance directly in neurons

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