| Identification | Back Directory | [Name]
Slv320 | [CAS]
251945-92-3 | [Synonyms]
Slv320
SC-204288
Derenofylline
SLV320 >=98% (HPLC)
SLV320; SLV-320; SLV 320; DERENOFYLLINE
4-[(2-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclohexanol
trans-4-[(2-Phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclohexanol
(1R,4R)-4-(2-Phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)cyclohexanol
Cyclohexanol, 4-[(2-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]-, trans-
Cyclohexanol, 4-((2-phenyl-1H-pyrrolo(2,3-D)pyrimidin-4-yl)amino)-, trans- | [Molecular Formula]
C18H20N4O | [MOL File]
251945-92-3.mol | [Molecular Weight]
308.38 |
| Chemical Properties | Back Directory | [Boiling point ]
532.3±60.0 °C(Predicted) | [density ]
1.37±0.1 g/cm3(Predicted) | [storage temp. ]
Keep in dark place,Sealed in dry,2-8°C | [solubility ]
Soluble to 100 mM in DMSO and to 50 mM in ethanol | [form ]
Powder | [pka]
15.15±0.40(Predicted) | [color ]
White to off-white | [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) | [InChIKey]
RBZNJGHIKXAKQE-UHFFFAOYSA-N | [SMILES]
O[C@H]1CC[C@@H](CC1)NC2=NC(C3=CC=CC=C3)=NC4=C2C=CN4 |
| Hazard Information | Back Directory | [Description]
Derenofylline is an adenosine A1 receptor antagonist (Ki = 1 nM). It is selective for adenosine A1 over A2A, A2B, and A3 receptors (Kis = 398, 3,981, and 200 nM, respectively). It decreases adenosine A1 receptor-mediated adenosine-induced bradycardia in rats (ED50 = 0.49 mg/kg) but reduces A2 receptor-mediated adenosine-induced hypotension by only 44.6% when administered at an intravenous dose of 5 mg/kg. It prevents increases in heart levels of collagen I and III in nephrectomized rats when administered at a dose of 10 mg/kg per day. Derenofylline also reduces relative plaque counts in a Zika virus plaque-forming assay in A549 cells (IC50 = 58.6 nM) in an adenosine A1 receptor-independent manner without inducing cytotoxicity when used at concentrations less than 10 μM. | [Uses]
SLV 320 is an A1 antagonist. | [in vivo]
Derenofylline (0.3-10 mg/kg, oral administration) suppresses adenosine-induced bradycardia in rats[1].
Derenofylline (10 mg/kg/d, oral administration, 12 weeks) reduces myocardial fibrosis in 5/6 nephrectomy rats without affecting blood pressure[1].
Derenofylline (0.1-5mg/kg, intravenous injection) causes no major haemodynamic effects (heart rate and blood pressure)[1].
| Animal Model: | 5/6 nephrectomy rats[1] | | Dosage: | 10 mg/kg/d | | Administration: | Oral administration, mixed with food for 12 weeks | | Result: | Attenuated urinary albuminuria by about 50%.
Suppressed the increase in CK levels, ALT and AST plasma levels in nephrectomized animals.
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| [IC 50]
A1R: 1 nM (Ki); Adenosine A3 receptor: 200 nM (Ki); A2AR: 398 nM (Ki) | [storage]
Store at RT | [References]
[1] P KALK. The adenosine A1 receptor antagonist SLV320 reduces myocardial fibrosis in rats with 5/6 nephrectomy without affecting blood pressure[J]. British Journal of Pharmacology, 2009, 151 7: 1025-1032. DOI: 10.1038/sj.bjp.0707319
[2] EWA D. MICEWICZ . Identification of novel small-molecule inhibitors of Zika virus infection[J]. Bioorganic & Medicinal Chemistry Letters, 2018, 28 3: Pages 452-458. DOI: 10.1016/j.bmcl.2017.12.019 |
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https://www.bocsci.com |
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