Vidofludimus 4sc-101; SC12267|cas:717824-30-1|西域试剂

Vidofludimus 4sc-101; SC12267,99.06%

产品编号：Bellancom-14908| CAS NO：717824-30-1| 分子式：C₂₀H₁₈FNO₄| 分子量：355.36

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货号	价格	库存与货期
Bellancom-14908	￥900.00	杭州北京（现货）
Bellancom-14908	￥1500.00	杭州北京（现货）
Bellancom-14908	￥4500.00	杭州北京（现货）
Bellancom-14908	￥6400.00	杭州北京（现货）

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Vidofludimus 4sc-101; SC12267

产品介绍

Vidofludimus 是二氢乳清酸脱氢酶 (DHODH) 的抑制剂，也是法尼醇 X 受体 (FXR) 的新型调节剂，具有口服活性。Vidofludimus 作为一种免疫调节剂，可用于研究自身免疫性疾病，如炎症性肠病 (IBD)。Vidofludimus 还可通过靶向 FXR 用于脂肪肝的研究。

生物活性

Vidofludimus is an orally active inhibitor for dihydroorotate dehydrogenase (DHODH) and also is a novel modulator for farnesoid X receptor (FXR). Vidofludimus, as an immunomodulatory agent, can be used for the research of autoimmune disorders such as inflammatory bowel disease (IBD). Vidofludimus also can be used for the research of fatty liver by targeting FXR.

体外研究

Vidofludimus (0-1 µM) selectively activats FXR in a concentration dependent manner with an EC₅₀ value of about 450 nM in inducing the recruitment of various coactivator LXXLL motifs.
Vidofludimus (0-8 μM) blocks nuclear translocation of p65 by suppressing IKK-IκB-NF-κB pathway.
Vidofludimus has inhibitory activity for human DHODH with an IC₅₀ value of 160 nM.
Vidofludimus inhibits dihydro-orotate dehydrogenase and lymphocyte proliferation in vitro.
Vidofludimus inhibits interleukin (IL)-17 secretion in vitro independently of effects on lymphocyte proliferation.
Vidofludimus completely blocks IL-23 + IL-1β-stimulated secretion of IL-17 by colonic strips in ex vivo.

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

Western Blot Analysis

Cell Line:	HepG2 cells or MEFs
Concentration:	2, 8 μM
Incubation Time:	1 h
Result:	Inhibited of TNFα-induced IKKα/β phosphorylation and IκBα degradation.

RT-PCR

Cell Line:	HepG2 cells
Concentration:	5 μM
Incubation Time:	24 h
Result:	Inhibited the increase of NF-κB target genes MCP-1 and CXCL-2 upon TNFα stimulation.

体内研究
(In Vivo)

Vidofludimus (i.p.; once daily; for 14 days) exerts effects on dextran sodium sulfate (DSS) induced colitis in an FXR-dependent manner in vivo.
Vidofludimus (p.o; 60 mg/kg; for 6 days) effectively improves many parameters of TNBS-induced colitis in rats and has inhibitory effects on colonic STAT3 and IL-17.

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

Animal Model:	homozygous FXR deficient (FXR KO) mice (10-week-old, male)
Dosage:	20 mg/kg
Administration:	oral, 20 mg/kg/day
Result:	Revealed multifocal inflammatory cell infiltration and edema with crypt and epithelial cell destruction and ulceration.

Animal Model:	NAFLD Model (10-11 weeks old male obese Lepob/ob C57BL/6 (ob/ob) mice)
Dosage:	10 mg/kg
Administration:	intraperitoneally, once daily, for 14 days
Result:	Significantly reduced body weight loss, prevented colonic shortening, decreased histological scores, and disease activity index (DAI) scores in WT mice. Significantly decreased colonic mRNA expression of the pro-inflammatorygenes interleukin (IL)-1β, IL-6, IL-17, and prostaglandin-endoperoxide synthase 2 (COX-2).

Animal Model:	Wistar rats
Dosage:	60 mg/kg
Administration:	p.o., for 6 days
Result:	Effectively reduced macroscopic and histological pathology and the numbers of CD3+ T cells in vivo. Reduced nuclear signal transducer and activator of transcription 3 (STAT3) binding and IL-17 levels.

体内研究

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

Animal Model:	homozygous FXR deficient (FXR KO) mice (10-week-old, male)
Dosage:	20 mg/kg
Administration:	oral, 20 mg/kg/day
Result:	Revealed multifocal inflammatory cell infiltration and edema with crypt and epithelial cell destruction and ulceration.

Animal Model:	NAFLD Model (10-11 weeks old male obese Lepob/ob C57BL/6 (ob/ob) mice)
Dosage:	10 mg/kg
Administration:	intraperitoneally, once daily, for 14 days
Result:	Significantly reduced body weight loss, prevented colonic shortening, decreased histological scores, and disease activity index (DAI) scores in WT mice. Significantly decreased colonic mRNA expression of the pro-inflammatorygenes interleukin (IL)-1β, IL-6, IL-17, and prostaglandin-endoperoxide synthase 2 (COX-2).

Animal Model:	Wistar rats
Dosage:	60 mg/kg
Administration:	p.o., for 6 days
Result:	Effectively reduced macroscopic and histological pathology and the numbers of CD3+ T cells in vivo. Reduced nuclear signal transducer and activator of transcription 3 (STAT3) binding and IL-17 levels.

体内研究

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

Animal Model:	homozygous FXR deficient (FXR KO) mice (10-week-old, male)
Dosage:	20 mg/kg
Administration:	oral, 20 mg/kg/day
Result:	Revealed multifocal inflammatory cell infiltration and edema with crypt and epithelial cell destruction and ulceration.

Animal Model:	NAFLD Model (10-11 weeks old male obese Lepob/ob C57BL/6 (ob/ob) mice)
Dosage:	10 mg/kg
Administration:	intraperitoneally, once daily, for 14 days
Result:	Significantly reduced body weight loss, prevented colonic shortening, decreased histological scores, and disease activity index (DAI) scores in WT mice. Significantly decreased colonic mRNA expression of the pro-inflammatorygenes interleukin (IL)-1β, IL-6, IL-17, and prostaglandin-endoperoxide synthase 2 (COX-2).

Animal Model:	Wistar rats
Dosage:	60 mg/kg
Administration:	p.o., for 6 days
Result:	Effectively reduced macroscopic and histological pathology and the numbers of CD3+ T cells in vivo. Reduced nuclear signal transducer and activator of transcription 3 (STAT3) binding and IL-17 levels.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 46 mg/mL (129.45 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	2.8140 mL	14.0702 mL	28.1405 mL
5 mM	0.5628 mL	2.8140 mL	5.6281 mL
10 mM	0.2814 mL	1.4070 mL	2.8140 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 (7.04 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (7.04 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 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 (7.04 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (7.04 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 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 (7.04 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.04 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。