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

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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

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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..…

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 30412
Product name: GSK356278
Packaging: 5mg
Price: $57
Updated: 2024/03/01

Cayman Chemical

Product number: 30412
Product name: GSK356278
Packaging: 10mg
Price: $95
Updated: 2024/03/01

Cayman Chemical

Product number: 30412
Product name: GSK356278
Packaging: 25mg
Price: $208
Updated: 2024/03/01

Cayman Chemical

Product number: 30412
Product name: GSK356278
Packaging: 50mg
Price: $384
Updated: 2024/03/01

ChemScene

Product number: CS-0024611
Product name: GSK356278
Purity: ≥98.0%
Packaging: 5mg
Price: $150
Updated: 2021/12/16

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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 C_max (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%), C_max (205 nM), T_1/2 (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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GSK-356278 Suppliers

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720704-34-7, GSK-356278Related Search:

GSK-356278

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

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

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)-

GSK356278,anti-inflammatory,Phosphodiesterase (PDE),anxiolytic,cognition,Inhibitor,phosphodiesterase,PDE4,inhibit

720704-34-7