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  • DC Chemicals Limited
  • China
  • Product Name: Rolofylline
  • Price: $Inquiry/100mg $Inquiry/250mg $Inquiry/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao

136199-02-5

136199-02-5 structure
136199-02-5 structure
  • Name: KW 3902
  • Chemical Name: Rolofylline
  • CAS Number: 136199-02-5
  • Molecular Formula: C20H28N4O2
  • Molecular Weight: 356.46200
  • Catalog: Signaling Pathways GPCR/G Protein Adenosine Receptor
  • Create Date: 2017-01-28 07:31:12
  • Modify Date: 2024-01-07 10:00:59
  • 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].

Name Rolofylline
Synonyms KW 3902
MK-7418
1,3-Dnax
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].
Related Catalog
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.

[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.

Density 1.262g/cm3
Boiling Point 578ºC at 760mmHg
Molecular Formula C20H28N4O2
Molecular Weight 356.46200
Flash Point 303.4ºC
Exact Mass 356.22100
PSA 72.68000
LogP 2.78400
Vapour Pressure 2.33E-13mmHg at 25°C
Index of Refraction 1.605
Hazard Statements H413
RIDADR NONH for all modes of transport

~99%

136199-02-5 structure

136199-02-5

Literature: Kyowa Hakko Kogyo Co., Ltd. Patent: US5290782 A1, 1994 ; US 5290782 A

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136199-02-5 structure

136199-02-5

Literature: Synthesis, , # 7 p. 1123 - 1126

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136199-02-5 structure

136199-02-5

Literature: Journal of Medicinal Chemistry, , vol. 35, # 5 p. 924 - 930

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136199-02-5 structure

136199-02-5

Literature: Journal of Medicinal Chemistry, , vol. 35, # 5 p. 924 - 930

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136199-02-5 structure

136199-02-5

Literature: Synthesis, , # 7 p. 1123 - 1126
Precursor  4

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