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BW-A 78U

Names

[ CAS No. ]:
101155-02-6

[ Name ]:
BW-A 78U

[Synonym ]:
bw-a 78u

Biological Activity

[Description]:

BW-A 78U is a PDE4 inhibitor with an IC50 of 3 μM.

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE)
Research Areas >> Inflammation/Immunology

[Target]

PDE4:3 μM (IC50)


[In Vitro]

BW-A 78U is a PDE4 inhibitor with an IC50 of 3 μM. BW-A 78U fails to significantly inhibit arachidonate release. BW-A 78U is ineffective to inhibit the lipopolysaccharide (LPS)-induced TNF-α release[1].

[Cell Assay]

Mononuclear cells are incubated for 30 min with BW-A 78U at the concentration of 10 nM to 10 μM. The cells are then stimulated with lipopolysaccharide (10 μg/mL) overnight at 37°C in an atmosphere of 5% CO2 at 100% humidity. Cell-free supernatants are collected, centrifuged (2000 g), and stored frozen at -20°C before TNF-α determination. TNF-α concentrations in cell culture supernatants are determined by specific ELISA using a commercial kit. Sensitivity of the assay is 1 pg/mL. The absorbance at 450 nm is assessed with an ELISA reader[1].

[References]

[1]. Boichot E, et al. Anti-inflammatory activities of a new series of selective phosphodiesterase 4 inhibitors derivedfrom 9-benzyladenine. J Pharmacol Exp Ther. 2000 Feb;292(2):647-53.


[Related Small Molecules]

3-Isobutyl-1-methylxanthine | rolipram | PF-04957325 | AN-2728 | GLPG1690 | BAY-60-7550 | Icariin | Ibudilast | PF-8380 | TAK-063 | Dipyridamole | Cilostazol | GSK256066 | Cialis | Pentoxifylline

Chemical & Physical Properties

[ Density]:
1.36g/cm3

[ Boiling Point ]:
477.9ºC at 760mmHg

[ Molecular Formula ]:
C13H12FN5

[ Molecular Weight ]:
257.26600

[ Flash Point ]:
242.8ºC

[ Exact Mass ]:
257.10800

[ PSA ]:
55.63000

[ LogP ]:
2.12840

[ Vapour Pressure ]:
2.69E-09mmHg at 25°C

[ Storage condition ]:
2-8℃

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
UO7440800
CHEMICAL NAME :
9H-Purin-6-amine, 9-((2-fluorophenyl)methyl)-N-methyl-
CAS REGISTRY NUMBER :
101155-02-6
LAST UPDATED :
199612
DATA ITEMS CITED :
3
MOLECULAR FORMULA :
C13-H12-F-N5
MOLECULAR WEIGHT :
257.30

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>1 gm/kg
TOXIC EFFECTS :
Behavioral - ataxia
REFERENCE :
JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 29,1133,1986
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>1 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JHTCAD Journal of Heterocyclic Chemistry. (Hetero Corporation, POB 16000 MH, Tampa, FL 33687) Vol.1- 1964- Volume(issue)/page/year: 25,1255,1988
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
120 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JHTCAD Journal of Heterocyclic Chemistry. (Hetero Corporation, POB 16000 MH, Tampa, FL 33687) Vol.1- 1964- Volume(issue)/page/year: 25,1255,1988

Related Compounds