SPL-707|cas:2195361-33-0|西域试剂

SPL-707,99.28%

产品编号：Bellancom-111360| CAS NO：2195361-33-0| 分子式：C₂₇H₂₈FN₅O₄| 分子量：505.54

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-111360		￥9800.00	杭州北京（现货）
Bellancom-111360		￥18000.00	杭州北京（现货）

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SPL-707

产品介绍

SPL-707 是口服有效的，选择性的信号肽肽酶样 2a (SPPL2a) 抑制剂，对 hSPPL2a 的 IC₅₀ 为 77 nM。SPL-707 抑制 γ-分泌酶 (γ-secretase; IC₅₀=6.1 μM) 和 SPP (IC₅₀=3.7 μM)。SPL-707 具有靶向 B 细胞和树突状细胞的自身免疫疾病的研究潜力。

生物活性

SPL-707 is an orally active, selective signal peptide peptidase-like 2a (SPPL2a) inhibitor with an IC₅₀ of 77 nM for hSPPL2a. SPL-707 inhibits γ-secretase (IC₅₀=6.1 μM) and SPP (IC₅₀=3.7 μM). SPL-707 has the potential for autoimmune diseases research by targeting B cells and dendritic cells.

体外研究

SPL-707 (Compound 40) inhibits mouse SPPL2a (IC₅₀=0.18 μM), rat SPPL2a (IC₅₀=0.056 μM) and human SPPL2a (IC₅₀=0.16 μM), human SPPL2b (IC₅₀=0.43 μM) by a high content imaging assay (HCA).

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

体内研究

SPL-707 (Compound 40; 3-30 mg/kg; orally; b.i.d.; for 11 days) leads to a reduction in B cells and myeloid dendritic cells without affecting γ-secretase activity.
SPL-707 (3 mg/kg of po and 1 mg/kg of iv) has a CL of 6 mL/min•kg, and an AUC of 8787 h•nM.
SPL-707 (1, 3 mg/kg; b.i.d.; first dose at 0 h, second dose at 8 h) achieves full inhibition of CD74/p8 processing in spleen in female Lewis rats.

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

Animal Model:	Mice with 5-12 weeks of age
Dosage:	3, 10, and 30 mg/kg
Administration:	Orally; b.i.d. (with 8 and 16 h dosing intervals); for 11 days
Result:	Led to a reduction in B cells and myeloid dendritic cells without affecting γ-secretase activity.

Animal Model:	Female Sprague−Dawley rat
Dosage:	3 mg/kg of po and 1 mg/kg of iv (Pharmacokinetic Analysis)
Administration:	PO or IV
Result:	Had a CL of 6 mL/min•kg, and an AUC of 8787 h•nM.

体内研究

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

Animal Model:	Mice with 5-12 weeks of age
Dosage:	3, 10, and 30 mg/kg
Administration:	Orally; b.i.d. (with 8 and 16 h dosing intervals); for 11 days
Result:	Led to a reduction in B cells and myeloid dendritic cells without affecting γ-secretase activity.

Animal Model:	Female Sprague−Dawley rat
Dosage:	3 mg/kg of po and 1 mg/kg of iv (Pharmacokinetic Analysis)
Administration:	PO or IV
Result:	Had a CL of 6 mL/min•kg, and an AUC of 8787 h•nM.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (197.81 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9781 mL	9.8904 mL	19.7808 mL
5 mM	0.3956 mL	1.9781 mL	3.9562 mL
10 mM	0.1978 mL	0.9890 mL	1.9781 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: ≥ 5 mg/mL (9.89 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (9.89 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 50.0 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% corn oil
Solubility: ≥ 5 mg/mL (9.89 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (9.89 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 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。