GSK143 dihydrochloride|cas:2341796-81-2|西域试剂

GSK143 dihydrochloride,99.73%

产品编号：Bellancom-12736A| CAS NO：2341796-81-2| 分子式：C₁₇H₂₄Cl₂N₆O₂| 分子量：415.32

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货号	价格	库存与货期
Bellancom-12736A	￥1500.00	杭州北京（现货）
Bellancom-12736A	￥2500.00	杭州北京（现货）
Bellancom-12736A	￥5400.00	杭州北京（现货）
Bellancom-12736A	￥9200.00	杭州北京（现货）

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GSK143 dihydrochloride

产品介绍

GSK143 dihydrochloride 是一种具有口服活性，高选择性的脾酪氨酸激酶 (SYK) 抑制剂，pIC₅₀ 为 7.5。GSK143 dihydrochloride 抑制 Erk 磷酸化 (pErk: pIC₅₀=7.1)。GSK143 dihydrochloride 可以减轻炎症，并防止小鼠肠道肌层中免疫细胞的募集。

生物活性

GSK143 dihydrochloride is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC₅₀ of 7.5. GSK143 dihydrochloride inhibits phosphorylated Erk (pErk: pIC₅₀=7.1). GSK143 dihydrochloride reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice.

体外研究

GSK143 dihydrochloride (compound 20) inhibits ZAP-70 (pIC₅₀=4.7), LCK (pIC₅₀=5.3), LYN (pIC₅₀=5.4), JAK1/2/3 (pIC₅₀=5.8/5.8/5.7), Aurora B (pIC₅₀=4.8), hWB (pIC₅₀=6.6), hERG (pIC₅₀=4.7).
GSK143 dihydrochloride (10-10000 nM; every 24 hours for 3 days) has an IC₅₀ of 323 nM in CLL cells. GSK 143 dihydrochloride (1 μM; 30 mins) abrogates early signalling events including SYK phosphorylation and calcium flux.
GSK143 dihydrochloride (0.1-10 μM; for 30 min) reduces cytokine expression in bone marrow derived macrophages in a concentration-dependent manner.

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

Cell Viability Assay

Cell Line:	Chronic lymphocytic leukaemia (CLL) cells
Concentration:	10, 100, 1000, 10000 nM
Incubation Time:	Every 24 hours for 3 days
Result:	Had an IC₅₀ of 323 nM.

体内研究
(In Vivo)

GSK143 (0.1-10 mg/kg; orally; 1.5 hours) reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis of 1 mg/kg.
GSK143 (3, 10, 30, 100 mg/kg; oral; 1 hour before ovalbumin challenge) reduces the cutaneous reverse passive Arthus reaction in a dose dependent manner by approximately 50% and 70% at 10 mg/kg and 30 mg/kg, respectively.
GSK143 (iv of 1 mg/kg; po of 3 mg/kg) has a T_1/2 of 4.2 hours, low clearance (16 mL/min/kg), moderate bioavailability of 30% and a V_ss of 4.1 L/kg in rats.

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

Animal Model:	Wild type C57NL/BL6 mice, 10-12 weeks old
Dosage:	0.1, 1, 3, 10 mg/kg
Administration:	Orally; 1.5 hours before intestinal manipulation (IM)
Result:	Reduced inflammation and prevented recruitment of immune cells in the intestinal muscularis.

Animal Model:	Male CD rats (175-200 g)
Dosage:	1 mg/kg of iv; 3 mg/kg of po (Pharmacokinetic Analysis)
Administration:	IV or PO
Result:	Had a T_1/2 of 4.2 hours, low clearance (16 mL/min/kg), moderate bioavailability of 30% and a V_ss of 4.1 L/kg.

体内研究

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

Animal Model:	Wild type C57NL/BL6 mice, 10-12 weeks old
Dosage:	0.1, 1, 3, 10 mg/kg
Administration:	Orally; 1.5 hours before intestinal manipulation (IM)
Result:	Reduced inflammation and prevented recruitment of immune cells in the intestinal muscularis.

Animal Model:	Male CD rats (175-200 g)
Dosage:	1 mg/kg of iv; 3 mg/kg of po (Pharmacokinetic Analysis)
Administration:	IV or PO
Result:	Had a T_1/2 of 4.2 hours, low clearance (16 mL/min/kg), moderate bioavailability of 30% and a V_ss of 4.1 L/kg.

体内研究

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

Animal Model:	Wild type C57NL/BL6 mice, 10-12 weeks old
Dosage:	0.1, 1, 3, 10 mg/kg
Administration:	Orally; 1.5 hours before intestinal manipulation (IM)
Result:	Reduced inflammation and prevented recruitment of immune cells in the intestinal muscularis.

Animal Model:	Male CD rats (175-200 g)
Dosage:	1 mg/kg of iv; 3 mg/kg of po (Pharmacokinetic Analysis)
Administration:	IV or PO
Result:	Had a T_1/2 of 4.2 hours, low clearance (16 mL/min/kg), moderate bioavailability of 30% and a V_ss of 4.1 L/kg.

性状

Solid

溶解性数据

In Vitro:

H₂O : 100 mg/mL (240.78 mM; Need ultrasonic)

DMSO : ≥ 50 mg/mL (120.39 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4078 mL	12.0389 mL	24.0778 mL
5 mM	0.4816 mL	2.4078 mL	4.8156 mL
10 mM	0.2408 mL	1.2039 mL	2.4078 mL

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 (sealed storage, away from moisture and light)。-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: ≥ 2.5 mg/mL (6.02 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.02 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (6.02 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.02 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (6.02 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.02 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。