SLV 320

Potent and selective A1 antagonist CAS# 251945-92-3

SLV 320

2D Structure

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SLV 320

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Chemical Properties of SLV 320

Cas No. 251945-92-3 SDF Download SDF
PubChem ID 9953065 Appearance Powder
Formula C18H20N4O M.Wt 308.38
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in DMSO and to 50 mM in ethanol
Chemical Name 4-[(2-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclohexan-1-ol
SMILES C1CC(CCC1NC2=NC(=NC3=C2C=CN3)C4=CC=CC=C4)O
Standard InChIKey RBZNJGHIKXAKQE-UHFFFAOYSA-N
Standard InChI 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)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of SLV 320

DescriptionPotent and selective adenosine A1 receptor antagonist (Ki values are 1, 200, 398 and 3981 nM at human A1, A3, A2A and A2B receptors respectively). Suppresses cardiac fibrosis and attenuates albuminuria, without effect on blood pressure in animal models of chronic renal failure. Orally active.

SLV 320 Dilution Calculator

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SLV 320 Molarity Calculator

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Preparing Stock Solutions of SLV 320

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.2428 mL 16.2138 mL 32.4275 mL 64.855 mL 81.0688 mL
5 mM 0.6486 mL 3.2428 mL 6.4855 mL 12.971 mL 16.2138 mL
10 mM 0.3243 mL 1.6214 mL 3.2428 mL 6.4855 mL 8.1069 mL
50 mM 0.0649 mL 0.3243 mL 0.6486 mL 1.2971 mL 1.6214 mL
100 mM 0.0324 mL 0.1621 mL 0.3243 mL 0.6486 mL 0.8107 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on SLV 320

The adenosine A1 receptor antagonist SLV320 reduces myocardial fibrosis in rats with 5/6 nephrectomy without affecting blood pressure.[Pubmed:17558436]

Br J Pharmacol. 2007 Aug;151(7):1025-32.

BACKGROUND AND PURPOSE: 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 rats with 5/6 nephrectomy. EXPERIMENTAL APPROACH: Male Sprague-Dawley rats were allocated to 4 groups of 12 rats each: 5/6 nephrectomy (5/6 NX), 5/6 NX plus SLV320 (10 mg kg(-1) d(-1) mixed with food), sham and sham plus SLV320. Study duration was 12 weeks, blood pressure was assessed repeatedly. At study end kidney function was assessed, blood samples and hearts were taken for histology/immunohistochemistry. Pharmacological properties of SLV320 were assessed using receptor binding and enzyme assays and in vivo. KEY RESULTS: SLV320 is a selective and potent adenosine A(1) antagonist in vitro (Ki=1 nM) with a selectivity factor of at least 200 versus other adenosine receptor subtypes. Functional A(1) antagonism was demonstrated in vivo. In rats with 5/6 NX SLV320 significantly decreased albuminuria by about 50%, but did not alter glomerular filtration rate (GFR). SLV320 normalized cardiac collagen I+III contents in 5/6 NX rats. SLV320 prevented nephrectomy-dependent rise in plasma levels of creatinine kinase (CK), ALT and AST. Blood pressure did not differ between study groups. CONCLUSION: SLV320 suppresses cardiac fibrosis and attenuates albuminuria without affecting blood pressure in rats with 5/6 nephrectomy, indicating that selective A(1) receptor antagonists may be beneficial in uraemic cardiomyopathy.

Description

Derenofylline (SLV 320) is a potent, selective and orally active adenosine A1 receptor antagonist, with Ki values of 1 nM, 200 nM and 398 nM for human A1, A3 and A2A receptors respectively. Derenofylline suppresses cardiac fibrosis and attenuates albuminuria without affecting blood pressure in rats.

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