KRN5|cas:1800465-47-7|西域试剂

KRN5,98.58%

产品编号：Bellancom-112126| CAS NO：1800465-47-7| 分子式：C₂₇H₂₂FNO₅| 分子量：459.47

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-112126	￥900.00	杭州北京（现货）
Bellancom-112126	￥1500.00	杭州北京（现货）
Bellancom-112126	￥3100.00	杭州北京（现货）
Bellancom-112126	￥5500.00	杭州北京（现货）
Bellancom-112126	￥9900.00	杭州北京（现货）

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KRN5

产品介绍

KRN5 是 KRN2 的衍生物，是具有口服活性的 T 细胞激活核因子 (NFAT5) 的抑制剂，IC₅₀ 值为 750 nM。KRN5 有潜力用于 NFAT5-介导的慢性关节炎的研究。

生物活性

KRN5, a derivative of KRN2, is an oral active Nuclear factor of activated T cells 5 (NFAT5) suppressor, with an IC₅₀ of 750 nM. KRN5 has potential to treat NFAT5-mediated Chronic Arthritis.

体外研究

KRN5 is less toxic than BBR as determined by a cytotoxicity assay, hERG K+ channel assay, cytochrome inhibition assay, and liver microsomal metabolic stability test, which makes it a potential drug candidate.
KRN5 at a concentration of 1 μM inhibits the expressions of NFAT5, IL-6,MCP-1, and GM-CSF,which are NFAT5 target molecules, in RAW264.7 macrophages stimulated with LPS.

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

体内研究

Oral feeding of KRN5 (15 mg/kg and 60 mg/kg) every other day for 3 weeks from day 21 dose-dependently mitigates arthritis severity.
The concentration of serum anti-type II collagen IgG also significantly decreases in the sera of KRN5-treated mice. TNF-α and IL-6 production by LPS-stimulated splenocytes are significantly lower in KRN5-treated CIA mice than in vehicle-treated mice.

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

Animal Model:	8-week-old DBA/1Jmice immunized with bovine type II collagen.
Dosage:	15 mg/kg and 60 mg/kg.
Administration:	Orally on alternate days (every other day) for 3 weeks.
Result:	Dose-dependently mitigated arthritis severity.

体内研究

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

Animal Model:	8-week-old DBA/1Jmice immunized with bovine type II collagen.
Dosage:	15 mg/kg and 60 mg/kg.
Administration:	Orally on alternate days (every other day) for 3 weeks.
Result:	Dose-dependently mitigated arthritis severity.

性状

Solid

溶解性数据

In Vitro:

DMSO : 5 mg/mL (10.88 mM; ultrasonic and warming and heat to 80°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1764 mL	10.8821 mL	21.7642 mL
5 mM	0.4353 mL	2.1764 mL	4.3528 mL
10 mM	0.2176 mL	1.0882 mL	2.1764 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: 0.5 mg/mL (1.09 mM); Suspended solution; Need ultrasonic

此方案可获得 0.5 mg/mL (1.09 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 5.0 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: 0.5 mg/mL (1.09 mM); Suspended solution; Need ultrasonic

此方案可获得 0.5 mg/mL (1.09 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 5.0 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