SCH28080|cas:76081-98-6|西域试剂

SCH28080,99.0%

产品编号：Bellancom-103261| CAS NO：76081-98-6| 分子式：C₁₇H₁₅N₃O| 分子量：277.32

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-103261		￥600.00	杭州北京（现货）

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SCH28080

产品介绍

SCH28080 是一种可逆的，K⁺ 竞争性的胃 H,K-ATPase 抑制剂，K_i 值为 0.12 μM。SCH28080 在体内是有效的酸分泌抑制剂，具有抗溃疡作用。

生物活性

SCH28080 is a reversible, K⁺-competitive inhibitor of the gastric H,K-ATPase, with a K_i of 0.12 μM. SCH28080 is an effective inhibitor of acid secretion in vivo and with anti-gastric ulcer activity.

体外研究

SCH28080 competitively inhibits the K⁺-stimulated hydrolysis of ATP, with a K_i of 0.12 μM .
SCH28080 inhibits histamine-induced ^[14C]aminopyrine uptake into isolated rabbit parietal cells with an IC₅₀ of 0.029 μM.
SCH28080 causes a dose-dependent reduction in cell viability with IC₅₀ values of 22.9 µM and 15.3 µM after 2 h and 24 h treatments, respectively, and cell viability was below 10% at 100 µM already after 2 h treatment.
SCH28080 induces apoptosis and is cytotoxic at higher doses.
SCH28080 inhibits insulin secretion by activation of IK ATP and inhibition of L-type voltage-gated Ca²⁺ channels, reduces cell viability and dose-dependently induces apoptosis/necrosis.

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

Cell Viability Assay

Cell Line:	INS-1E cell
Concentration:	3.1 μM, 6.25 μM, 12.5 μM, 25 μM, 50 μM, 100 μM
Incubation Time:	2 hours, 24 hours
Result:	Caused a dose-dependent reduction in cell viability.

体内研究
(In Vivo)

SCH28080 (20 mg/kg; i.p.) inhibits gastric ulcers induced by pylorusligation in rats.

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

Animal Model:	Male Wistar rat (280-350 g), the Shay rat model
Dosage:	20 mg/kg
Administration:	Intraperitoneal injection
Result:	Showed 91% inhibition on gastric ulcers induced by pylorusligation in rats.

体内研究

SCH28080 (20 mg/kg; i.p.) inhibits gastric ulcers induced by pylorusligation in rats.

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

Animal Model:	Male Wistar rat (280-350 g), the Shay rat model
Dosage:	20 mg/kg
Administration:	Intraperitoneal injection
Result:	Showed 91% inhibition on gastric ulcers induced by pylorusligation in rats.

体内研究

SCH28080 (20 mg/kg; i.p.) inhibits gastric ulcers induced by pylorusligation in rats.

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

Animal Model:	Male Wistar rat (280-350 g), the Shay rat model
Dosage:	20 mg/kg
Administration:	Intraperitoneal injection
Result:	Showed 91% inhibition on gastric ulcers induced by pylorusligation in rats.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (360.59 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.6059 mL	18.0297 mL	36.0594 mL
5 mM	0.7212 mL	3.6059 mL	7.2119 mL
10 mM	0.3606 mL	1.8030 mL	3.6059 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。-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 (9.01 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (9.01 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 (9.01 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (9.01 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