LOC14|cas:877963-94-5|西域试剂

LOC14,98.0%

产品编号：Bellancom-100432| CAS NO：877963-94-5| 分子式：C₁₆H₁₉N₃O₂S| 分子量：317.41

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-100432	￥1000.00	杭州北京（现货）
Bellancom-100432	￥1700.00	杭州北京（现货）
Bellancom-100432	￥3400.00	杭州北京（现货）
Bellancom-100432	￥5500.00	杭州北京（现货）
Bellancom-100432	￥6600.00	杭州北京（现货）

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LOC14

产品介绍

LOC14 是蛋白质二硫键异构酶 (PDI) 抑制剂 (EC₅₀=500 nM; K_d=62 nM)。LOC14 在小鼠肝微粒体和血浆中表现出高稳定性，低内在微粒体清除率和低血浆蛋白结合。LOC14 抑制 PDIA3 活性，降低肺上皮细胞中 HA 的分子内二硫键和随后的寡聚化。

生物活性

LOC14 is a potent Protein disulfide isomerase (PDI) inhibitor with EC₅₀ and K_d values of 500 nM and 62 nM, respectively. LOC14 exhibits high stability in mouse liver microsomes and blood plasma, low intrinsic microsome clearance, and low plasma-protein binding. LOC14 inhibits PDIA3 activity, decreases intramolecular disulfide bonds and subsequent oligomerization (maturation) of HA in lung epithelial cells.

体外研究

LOC14 (0.01-100 μM; 24 hours) exhibits the capacity to inhibit recombinant (r)PDIA3 at an IC50 of approximately 5 μM.

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

Cell Viability Assay

Cell Line:	MTEC cells
Concentration:	0.01 μM; 0.1 μM; 0.5 μM; 1 μM; 5 μM; 10 μM; 100 μM
Incubation Time:	24 hours
Result:	Inhibited recombinant (r)PDIA3 activity.

体内研究
(In Vivo)

LOC14 (orally administered by gavage; 20 mg/kg; once daily; 12-28 weeks) significantly improves motor function, attenuated brain atrophy and extended survival in the N171–82Q HD mice.

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

Animal Model:	Male N171–82Q HD mice
Dosage:	20 mg/kg
Administration:	Orally administered by gavage; 20 mg/kg; once daily; 12-28 weeks
Result:	Improved motor function in HD mice.

体内研究

LOC14 (orally administered by gavage; 20 mg/kg; once daily; 12-28 weeks) significantly improves motor function, attenuated brain atrophy and extended survival in the N171–82Q HD mice.

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

Animal Model:	Male N171–82Q HD mice
Dosage:	20 mg/kg
Administration:	Orally administered by gavage; 20 mg/kg; once daily; 12-28 weeks
Result:	Improved motor function in HD mice.

体内研究

LOC14 (orally administered by gavage; 20 mg/kg; once daily; 12-28 weeks) significantly improves motor function, attenuated brain atrophy and extended survival in the N171–82Q HD mice.

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

Animal Model:	Male N171–82Q HD mice
Dosage:	20 mg/kg
Administration:	Orally administered by gavage; 20 mg/kg; once daily; 12-28 weeks
Result:	Improved motor function in HD mice.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (157.52 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.1505 mL	15.7525 mL	31.5050 mL
5 mM	0.6301 mL	3.1505 mL	6.3010 mL
10 mM	0.3150 mL	1.5752 mL	3.1505 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；该产品在溶液状态不稳定，建议您现用现配，即刻使用。

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: ≥ 2.08 mg/mL (6.55 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.55 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (6.55 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.55 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (6.55 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.55 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。