GSK356278|cas:720704-34-7|西域试剂

GSK356278,99.89%

产品编号：Bellancom-106003| CAS NO：720704-34-7| 分子式：C₂₁H₂₅N₇O₂S| 分子量：439.53

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货号	价格	库存与货期
Bellancom-106003	￥700.00	杭州北京（现货）
Bellancom-106003	￥1100.00	杭州北京（现货）
Bellancom-106003	￥3900.00	杭州北京（现货）
Bellancom-106003	￥6200.00	杭州北京（现货）

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GSK356278

产品介绍

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 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.

体外研究

GSK356278 competes with [³H]rolipram for the high affinity rolipram binding site (HARBS) with a pK_i 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 pK_is 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Lewis rats (320-400 g) are treated with lipopolysaccharide (LPS)
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
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).

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Lewis rats (320-400 g) are treated with lipopolysaccharide (LPS)
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
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).

性状

Solid

溶解性数据

In Vitro:

DMSO : 2.5 mg/mL (5.69 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2752 mL	11.3758 mL	22.7516 mL
5 mM	0.4550 mL	2.2752 mL	4.5503 mL
10 mM	---	---	---

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 1.25 mg/mL (2.84 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (2.84 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1.25 mg/mL (2.84 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (2.84 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 1.25 mg/mL (2.84 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (2.84 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。