KW 3902

Modify Date: 2024-01-07 10:00:59

KW 3902 Structure
KW 3902 structure
Common Name KW 3902
CAS Number 136199-02-5 Molecular Weight 356.46200
Density 1.262g/cm3 Boiling Point 578ºC at 760mmHg
Molecular Formula C20H28N4O2 Melting Point N/A
MSDS Chinese USA Flash Point 303.4ºC

 Use of KW 3902


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].

 Names

Name Rolofylline
Synonym More Synonyms

 KW 3902 Biological Activity

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.

 Chemical & Physical Properties

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

 Safety Information

Hazard Statements H413
RIDADR NONH for all modes of transport

 Synthetic Route

~99%

KW 3902 Structure

KW 3902

CAS#:136199-02-5

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

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KW 3902 Structure

KW 3902

CAS#:136199-02-5

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

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KW 3902 Structure

KW 3902

CAS#:136199-02-5

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

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KW 3902 Structure

KW 3902

CAS#:136199-02-5

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

~%

KW 3902 Structure

KW 3902

CAS#:136199-02-5

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

 Articles26

More Articles
The effects of multiple doses of rolofylline on the single-dose pharmacokinetics of midazolam in healthy subjects.

Am. J. Ther. 17(1) , 53-60, (2010)

Rolofylline is a potent, selective adenosine A1 receptor antagonist that was under development for the treatment of patients with acute decompensated heart failure and renal function impairment. This ...

The disconnect between phase II and phase III trials of drugs for heart failure.

Nat. Rev. Cardiol. 10(2) , 85-97, (2013)

Hospitalization for heart failure (HF) is a clinical entity associated with high postdischarge morbidity and mortality, yet few therapies are available to improve outcomes in patients with this condit...

Design and rationale of the PROTECT study: a placebo-controlled randomized study of the selective A1 adenosine receptor antagonist rolofylline for patients hospitalized with acute decompensated heart failure and volume overload to assess treatment effect on congestion and renal function.

J. Card. Fail. 16(1) , 25-35, (2010)

Current treatment for acute decompensated heart failure (ADHF) is associated with incomplete resolution of symptoms and signs, recurrent symptoms of heart failure in-hospital and after discharge and h...

 Synonyms

KW 3902
MK-7418
1,3-Dnax