GSK-356278
- Product Name
- GSK-356278
- CAS No.
- 720704-34-7
- Chemical Name
- GSK-356278
- Synonyms
- GSK-356278;GSK356278,anti-inflammatory,Phosphodiesterase (PDE),anxiolytic,cognition,Inhibitor,phosphodiesterase,PDE4,inhibit;5-(5-((2,4-Dimethylthiazol-5-yl)methyl)-1,3,4-oxadiazol-2-yl)-1-ethyl-N-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-b]pyridin-4-amine;5-[5-[(2,4-dimethyl-5-thiazolyl)methyl]-1,3,4-oxadiazol-2-yl]-1-ethyl-N-(tetrahydro-2H-pyran-4-yl)-1H-Pyrazolo[3,4-b]pyridin-4-amine;1H-Pyrazolo[3,4-b]pyridin-4-amine, 5-[5-[(2,4-dimethyl-5-thiazolyl)methyl]-1,3,4-oxadiazol-2-yl]-1-ethyl-N-(tetrahydro-2H-pyran-4-yl)-
- CBNumber
- CB73032890
- Molecular Formula
- C21H25N7O2S
- Formula Weight
- 439.53
- MOL File
- 720704-34-7.mol
GSK-356278 Property
- Boiling point:
- 683.6±65.0 °C(Predicted)
- Density
- 1.50±0.1 g/cm3(Predicted)
- storage temp.
- -20°C, stored under nitrogen
- solubility
- Chloroform: 30 mg/ml
- form
- A crystalline solid
- pka
- 3.33±0.10(Predicted)
- color
- White to off-white
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Danger
- Hazard statements
-
H301Toxic if swalloed
H372Causes damage to organs through prolonged or repeated exposure
- Precautionary statements
-
P260Do not breathe dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.
P314Get medical advice/attention if you feel unwell.
P321Specific treatment (see … on this label).
P330Rinse mouth.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- 30412
- Product name
- GSK356278
- Packaging
- 5mg
- Price
- $57
- Updated
- 2024/03/01
- Product number
- 30412
- Product name
- GSK356278
- Packaging
- 10mg
- Price
- $95
- Updated
- 2024/03/01
- Product number
- 30412
- Product name
- GSK356278
- Packaging
- 25mg
- Price
- $208
- Updated
- 2024/03/01
- Product number
- 30412
- Product name
- GSK356278
- Packaging
- 50mg
- Price
- $384
- Updated
- 2024/03/01
- Product number
- CS-0024611
- Product name
- GSK356278
- Purity
- ≥98.0%
- Packaging
- 5mg
- Price
- $150
- Updated
- 2021/12/16
GSK-356278 Chemical Properties,Usage,Production
Uses
GSK356278 is a potent, selective, orally bioavailable and brain-penetrant inhibitor of phosphodiesterase 4 (PDE4), with pIC50s of 8.6, 8.8, and 8.7 for human PDE4A, PDE4B, and PDE4D, respectively. GSK356278 has anti-inflammatory activity, and exhibits anxiolytic and cognition-enhancing effects[1].
in vivo
GSK356278 (0.003-30 mg/kg; p.o.) shows anti-inflammatory activity in rodents at exposures that does not induce pica feeding[1].
GSK356278 (0.1-0.1 mg/kg; p.o.) demonstrates efficacy in a nonhuman primate model of anxiety at exposures that do not induce emesis[1].
GSK356278 (4 doses at 0.03, 0.1, 0.3, and 1.0 mg/kg for 6 weeks; p.o.) enhances performance in a nonhuman primate object retrieval test[1]. GSK356278 exhibits oral bioavailability (rat 91%, monkey 23%) and Cmax (rat 205, monkey 41 nM) following oral administration (rat 1, monkey 0.2 mg/kg)[1].
GSK356278 exhibits terminal elimination half-lives (rat 2.2, monkey 1.5 h) due to moderate blood clearance (rat 40, monkey 16 mL/min/kg) combined with volumes of distribution (rat 6.3, monkey 2.1 L/kg) following intravenous administration (rat 1, monkey 0.2 mg/kg)[1].
| Animal Model: | Male Lewis rats (320-400 g) are treated with lipopolysaccharide (LPS)[1] |
| Dosage: | 0.003-3 mg/kg |
| Administration: | P.o. administration 30 minutes prior to the LPS challenge |
| Result: | Reduced the level of neutrophilia in a dose-dependent manner, with an ED50 of 0.09 mg/kg. |
| Animal Model: | Male CD rats[1] |
| Dosage: | 1 mg/kg (Pharmacokinetic Analysis) |
| Administration: | I.v. and p.o. administration |
| Result: | Oral bioavailability (91%), Cmax (205 nM), T1/2 (2.2 h). |
IC 50
PDE4A: 8.6 (pIC50); PDE4B: 8.8 (pIC50); PDE4D: 8.7 (pIC50)
References
[1] Rutter AR, et, al. GSK356278, a potent, selective, brain-penetrant phosphodiesterase 4 inhibitor that demonstrates anxiolytic and cognition-enhancing effects without inducing side effects in preclinical species. J Pharmacol Exp Ther. 2014 Jul;350(1):153-63. DOI:10.1124/jpet.114.214155
GSK-356278 Preparation Products And Raw materials
Raw materials
Preparation Products
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