| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| ln Vitro |
Derenofylline (100 μM, 72 h) prevents myofibroblast transformation brought on by TGF-β1 while maintaining cell viability [2].
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|---|---|
| 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].
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| 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.
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| Molecular Formula |
C18H20N4O
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|---|---|
| Molecular Weight |
308.385
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| Exact Mass |
308.164
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| CAS # |
251945-92-3
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| PubChem CID |
9953065
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
3.413
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
379
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C=C1)C2=NC3=C(C=CN3)C(=N[C@H]4CC[C@@H](CC4)O)N2
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| InChi Key |
RBZNJGHIKXAKQE-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
4-[(2-phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclohexan-1-ol
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| Synonyms |
SLV 320; SLV-320; SLV320
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~324.28 mM)
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|---|---|
| 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. View More
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. |
| 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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