Derenofylline (SLV 320) is a potent, selective, orally bioactive adenosine A1 receptor blocker (antagonist) with Kis of 1 nM, 200 nM and 398 for adenosine A1, A3 and A2A receptors respectively. nM. Derenofylline inhibits myocardial fibrosis and reduces proteinuria without affecting blood pressure in rats.

Physicochemical Properties

Molecular Formula	C18H20N4O
Molecular Weight	308.385
Exact Mass	308.164
CAS #	251945-92-3
PubChem CID	9953065
Appearance	Typically exists as solid at room temperature
LogP	3.413
Hydrogen Bond Donor Count	3
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	3
Heavy Atom Count	23
Complexity	379
Defined Atom Stereocenter Count	0
SMILES	C1=CC=C(C=C1)C2=NC3=C(C=CN3)C(=N[C@H]4CC[C@@H](CC4)O)N2
InChi Key	RBZNJGHIKXAKQE-UHFFFAOYSA-N
InChi Code	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)
Chemical Name	4-[(2-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclohexan-1-ol
Synonyms	SLV 320; SLV-320; SLV320
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	Derenofylline (100 μM, 72 h) prevents myofibroblast transformation brought on by TGF-β1 while maintaining cell viability [2].
ln Vivo	Adenosine-sensitive locus bradycardia is inhibited by derenofylline (0.3–10 mg/kg) when taken orally [1]. 10 mg/kg/d, PO, 12 weeks) 5/6 Derenofylline (0.1–5 mg/kg, IV) reduction in the renal transplantation diagram did not result in significant hemodynamic consequences (hypertension and myocardium) [1].
Animal Protocol	Animal/Disease Models: 5/6 nephrectomized rats [1] Doses: 10 mg/kg/d Route of Administration: Orally, mixed with food for 12 weeks. Experimental Results: Urinary proteinuria was diminished by about 50%. Inhibits the increase in plasma CK levels, ALT and AST levels in nephrectomized animals.
References	[1]. Kalk P, et al. The adenosine A1 receptor antagonist SLV320 reduces myocardial fibrosis in rats with 5/6 nephrectomy without affecting blood pressure. Br J Pharmacol. 2007 Aug;151(7):1025-32. [2]. Marta Mateus, et al. Understanding the Role of Adenosine Receptors in the Myofibroblast Transformation in Peyronie's Disease. J Sex Med. 2018 Jul;15(7):947-957.
Additional Infomation	Derenofylline has been used in trials studying the treatment of Congestive Heart Failure and Acute Decompensated Heart Failure; Renal Dysfunction.

Solubility Data

Solubility (In Vitro)

DMSO : ~100 mg/mL (~324.28 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 6.25 mg/mL (20.27 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 6.25 mg/mL (20.27 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 6.25 mg/mL (20.27 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.2426 mL	16.2132 mL	32.4265 mL
	5 mM	0.6485 mL	3.2426 mL	6.4853 mL
	10 mM	0.3243 mL	1.6213 mL	3.2426 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.