Rolofylline
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity: 99.68%
- CAS No.: 136199-02-5
- Formula: C20H28N4O2
- Molecular Weight:356.46
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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All Adenosine Receptor Isoforms
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Biological Activity
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 136199-02-5
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Appearance Solid
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Molecular Weight 356.46
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Formula C20H28N4O2
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Color White to off-white
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SMILES
O=C(N1CCC)N(CCC)C2=C(N=C(C34CC(C5)CC3CC5C4)N2)C1=O
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Synonyms
KW-3902
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Stroh M, et al. Simultaneous pharmacokinetic model for rolofylline and both M1-trans and M1-cis metabolites. AAPS J. 2013 Apr;15(2):498-504. [Content Brief]
[2]. Dennissen FJ, et al. Adenosine A1 receptor antagonist rolofylline alleviates axonopathy caused by human Tau ΔK280. Proc Natl Acad Sci U S A. 2016 Oct 11;113(41):11597-11602. Epub 2016 Sep 26. [Content Brief]
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 |
Rolofylline Related Classifications
HY-10965 Related Classifications
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