2. GPCR/G Protein
  3. Adenosine Receptor
  4. Rolofylline

Rolofylline (KW-3902) is a potent, selective adenosine A1 receptor antagonist that is under development for the treatment of patients with acute congestive heart failure and renal impairment. Rolofylline is metabolized primarily to the pharmacologically active M1-trans and M1-cis metabolites by cytochrome P450 (CYP450). Rolofylline is alleviating the presynaptic dysfunction and restores neuronal activity as well as dendritic spine levels in vitro, is an interesting candidate to combat the hypometabolism and neuronal dysfunction associated with Tau-induced neurodegenerative diseases.

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Rolofylline Chemical Structure

Rolofylline Chemical Structure

CAS No. : 136199-02-5

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Description

Rolofylline (KW-3902) is a potent, selective adenosine A1 receptor antagonist that is under development for the treatment of patients with acute congestive heart failure and renal impairment. Rolofylline is metabolized primarily to the pharmacologically active M1-trans and M1-cis metabolites by cytochrome P450 (CYP450)[1]. Rolofylline is alleviating the presynaptic dysfunction and restores neuronal activity as well as dendritic spine levels in vitro, is an interesting candidate to combat the hypometabolism and neuronal dysfunction associated with Tau-induced neurodegenerative diseases[2].

Clinical Trial
Molecular Weight

356.46

Formula

C20H28N4O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1CCC)N(CCC)C2=C(N=C(C34CC(C5)CC3CC5C4)N2)C1=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (56.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8054 mL 14.0268 mL 28.0536 mL
5 mM 0.5611 mL 2.8054 mL 5.6107 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Purity & Documentation

Purity: 99.68%

Data Sheet (274 KB) SDS (393 KB)

COA (252 KB) HNMR (132 KB) RP-HPLC (247 KB) MS (106 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8054 mL 14.0268 mL 28.0536 mL 70.1341 mL
5 mM 0.5611 mL 2.8054 mL 5.6107 mL 14.0268 mL
10 mM 0.2805 mL 1.4027 mL 2.8054 mL 7.0134 mL
15 mM 0.1870 mL 0.9351 mL 1.8702 mL 4.6756 mL
20 mM 0.1403 mL 0.7013 mL 1.4027 mL 3.5067 mL
25 mM 0.1122 mL 0.5611 mL 1.1221 mL 2.8054 mL
30 mM 0.0935 mL 0.4676 mL 0.9351 mL 2.3378 mL
40 mM 0.0701 mL 0.3507 mL 0.7013 mL 1.7534 mL
50 mM 0.0561 mL 0.2805 mL 0.5611 mL 1.4027 mL
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Rolofylline Related Classifications

Keywords:

Rolofylline136199-02-5KW-3902KW3902KW 3902Adenosine ReceptorP1 receptorInhibitorinhibitorinhibit

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