BW-A 78U
Names
Biological Activity
[Description]:
BW-A 78U is a PDE4 inhibitor with an IC50 of 3 μM.
[Related Catalog]:
[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]
[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