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Merck
모든 사진(1)

주요 문서

SML1931

Sigma-Aldrich

SLV320

≥98% (HPLC)

동의어(들):

4-[(4-trans-Hydroxycyclohexyl)amino]-2-phenyl-7H-pyrrolo[2,3-d]pyrimidine, Derenofylline, SLV 320, SLV-320, trans-4-[(2-Phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclohexanol

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About This Item

실험식(Hill 표기법):
C18H20N4O
CAS Number:
Molecular Weight:
308.38
UNSPSC 코드:
12352200
NACRES:
NA.77

Quality Level

분석

≥98% (HPLC)

형태

powder

색상

white to beige

solubility

DMSO: 2 mg/mL, clear

저장 온도

2-8°C

SMILES string

O[C@H]1CC[C@@H](CC1)NC2=NC(C3=CC=CC=C3)=NC4=C2C=CN4

InChI

1S/C18H20N4O/c23-14-8-6-13(7-9-14)20-18-15-10-11-19-17(15)21-16(22-18)12-4-2-1-3-5-12/h1-5,10-11,13-14,23H,6-9H2,(H2,19,20,21,22)

InChI key

RBZNJGHIKXAKQE-UHFFFAOYSA-N

생화학적/생리학적 작용

SLV320 is an orally active, high-affinity adenosine receptor A1 antagonist (pKi = 9.0 against 3H-DPCPX for binding human A1R and 8.6 against 3H-CCPA for binding rat A1R) that exhibits higher A1R-selectivity than DPCPX over other adenosine receptor subtypes (Fold-selectivity/subtypes = 200/hA3, 398/hA2a, 3981/hA2b). SLV320 displays much reduced or little affinity toward a panel of 94 other receptors and no inhibitory activity against PDE1-6 (IC50 ≥1 μM). SLV320 selectively reduces A1R-mediated bradycardia (ED50 = 0.49 mg/kg via p.o. or 0.25 mg/kg via i.v. 10 min prior to 100 μg/kg adenosine i.v. challenge), but not A2R-dependent hypotension (up to 2 mg/kg) among adenosin-challenged rats. When administered via food intake, SLV320 efficacy is demonstrated in experimental models of chronic renal failure (CRF; 10 mg/kg/day) and liver cirrhosis (5.1 mg/kg/day p.o.) in rats in vivo.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


시험 성적서(COA)

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문서 라이브러리 방문

Berthold Hocher et al.
PloS one, 6(3), e17891-e17891 (2011-03-23)
Liver cirrhosis is often complicated by an impaired renal excretion of water and sodium. Diuretics tend to further deteriorate renal function. It is unknown whether chronic selective adenosine A(1) receptor blockade, via inhibition of the hepatorenal reflex and the tubuloglomerular
Jian Zhou et al.
American journal of respiratory cell and molecular biology, 48(3), 299-305 (2012-12-12)
Epithelial injury and airway hyperresponsiveness are prominent features of asthma. We have previously demonstrated that laser ablation of single epithelial cells immediately induces global airway constriction through Ca(2+)-dependent smooth muscle shortening. The response is mediated by soluble mediators released from
P Kalk et al.
British journal of pharmacology, 151(7), 1025-1032 (2007-06-15)
Myocardial fibrosis is an unwanted effect associated with chronic renal failure. The adenosine system is involved in cardiac and renal function. Therefore, we investigated the novel selective adenosine A(1) receptor antagonist SLV320 focusing on its potential in preventing cardiomyopathy in

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