GSK356278|720704-34-7|-陌孚医药/Medlife

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GSK356278

目录号: PL09696 纯度: ≥99%

GSK356278 是一种有效，选择性，具有口服活性和可透过血脑屏障的磷酸二酯酶 4 (PDE4) 抑制剂，对人 PDE4A，PDE4B 和 PDE4D 的 pIC50 值分别为 8.6、8.8 和 8.7。GSK356278 具有抗炎活性，并具有抗焦虑和增强认知的作用。

CAS No. :720704-34-7

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PL09696-200mg	200mg	询价	询价
PL09696-500mg	500mg	询价	询价

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中文名称	GSK356278
中文别名	5-[5-[(2,4-二甲基-5-噻唑)甲基]-1,3,4-噁二唑-2-基]-1-乙基-n-(四氢-2H-吡喃-4-基)-1H-吡唑并[3,4-b]吡啶-4-胺
英文名称	GSK356278
英文别名	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-dimethyl-1,3-thiazol-5-yl)methyl]-1,3,4-oxadiazol-2-yl]-1-ethyl-N-(oxan-4-yl)pyrazolo[3,4-b]pyridin-4-amine;GSK356278;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;1QTA9P992C;GSK 356278;DB12542;SB16753;1H-Pyrazolo(3,4-b)pyridin-4-amine, 5-(5-((2,4-dimethyl-
Cas No.	720704-34-7
分子式	C₂₁H₂₅N₇O₂S
分子量	439.53
包装储存	-20°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

产品详情

GSK356278 是一种有效，选择性，具有口服活性和可透过血脑屏障的磷酸二酯酶 4 (PDE4) 抑制剂，对人 PDE4A，PDE4B 和 PDE4D 的 pIC₅₀ 值分别为 8.6、8.8 和 8.7。GSK356278 具有抗炎活性，并具有抗焦虑和增强认知的作用。

生物活性

GSK356278 is a potent, selective, orally bioavailable and brain-penetrant inhibitor of phosphodiesterase 4 (PDE4), with pIC 50 s 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.

性状

Solid

IC50 & Target[1][2]

PDE4A 8.6 (pIC50) PDE4B 8.8 (pIC50

体外研究(In Vitro)

GSK356278 competes with [H]rolipram for the high affinity rolipram binding site (HARBS) with a pKi of 8.6 in a competitive filtration-binding assay to the recombinant human PDE4B2B enzyme expressed in yeast membranes.
GSK356278 bounds to the HARBS in rats, mice, marmosets, and ferrets with pKis of 7.9, 7.8, 8.4, and 8.5, respectively.
GSK356278 inhibits LPS-induced release of TNF-α in human whole blood, with a pIC50 of 7.6. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

GSK356278 (0.003-30 mg/kg; p.o.) shows anti-inflammatory activity in rodents at exposures that does not induce pica feeding.
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.
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. 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).
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).

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

ClinicalTrial

参考文献

[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):153-6

溶解度数据	In Vitro: DMSO : 2.5 mg/mL (5.69 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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