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  1. Metabolic Enzyme/Protease Immunology/Inflammation
  2. Dihydroorotate Dehydrogenase Interleukin Related FXR
  3. Vidofludimus

Vidofludimus  (Synonyms: 4sc-101; SC12267)

目錄號(hào): HY-14908 純度: 99.11%
COA 產(chǎn)品使用指南

Vidofludimus 是二氫乳清酸脫氫酶 (DHODH) 的抑制劑,也是法尼醇 X 受體 (FXR) 的新型調(diào)節(jié)劑,具有口服活性。Vidofludimus 作為一種免疫調(diào)節(jié)劑,可用于研究自身免疫性疾病,如炎癥性腸病 (IBD)。Vidofludimus 還可通過靶向 FXR 用于脂肪肝的研究。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào),我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Vidofludimus Chemical Structure

Vidofludimus Chemical Structure

CAS No. : 717824-30-1

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ¥700
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5 mg ¥900
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10 mg ¥1500
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50 mg ¥4500
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100 mg ¥5329
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Customer Review

Other Forms of Vidofludimus:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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[1][2][3].

IC50 & Target[1][2]

IL-17

 

體外研究
(In Vitro)

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[1].
Vidofludimus (0-8 μM) blocks nuclear translocation of p65 by suppressing IKK-IκB-NF-κB pathway[1].
Vidofludimus has inhibitory activity for human DHODH with an IC50 value of 160 nM[2].
Vidofludimus inhibits dihydro-orotate dehydrogenase and lymphocyte proliferation in vitro[3].
Vidofludimus inhibits interleukin (IL)-17 secretion in vitro independently of effects on lymphocyte proliferation[3].
Vidofludimus completely blocks IL-23 + IL-1β-stimulated secretion of IL-17 by colonic strips in ex vivo[3].

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

Western Blot Analysis[1]

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[1]

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.
體內(nèi)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[1].
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[3].

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

Animal Model: homozygous FXR deficient (FXR KO) mice[1]
(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[1]
(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[3]
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.
Clinical Trial
分子量

355.36

Formula

C20H18FNO4

CAS 號(hào)
性狀

固體

顏色

Light yellow to gray

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : ≥ 46 mg/mL (129.45 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
儲(chǔ)備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn):

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑:
——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用;
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (7.04 mM); 懸濁液; 超聲助溶

    此方案可獲得 2.5 mg/mL的均勻懸濁液,懸濁液可用于口服和腹腔注射。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請(qǐng)依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (7.04 mM); 懸濁液; 超聲助溶

    此方案可獲得 2.5 mg/mL的均勻懸濁液,懸濁液可用于口服和腹腔注射。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中,混合均勻。

    20% SBE-β-CD in Saline 的配制(4°C,儲(chǔ)存一周):2 g SBE-β-CD(磺丁基醚 β-環(huán)糊精)粉末定容于 10 mL 的生理鹽水中,完全溶解至澄清透明。
動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

由于實(shí)驗(yàn)過程有損耗,建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括:DMSO, ,均可在 MCE 網(wǎng)站選購。 ,Tween 80,均可在 MCE 網(wǎng)站選購。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。
您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測(cè)溶解度,以下方案僅供參考,如有需要,請(qǐng)與 MCE 中國技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液,加入 μL 。 μL ,混合均勻至澄清,再加 μL Tween 80,混合均勻至澄清,再加 μL 生理鹽水
連續(xù)給藥周期超過半月以上,請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.11%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8140 mL 14.0702 mL 28.1405 mL 70.3512 mL
5 mM 0.5628 mL 2.8140 mL 5.6281 mL 14.0702 mL
10 mM 0.2814 mL 1.4070 mL 2.8140 mL 7.0351 mL
15 mM 0.1876 mL 0.9380 mL 1.8760 mL 4.6901 mL
20 mM 0.1407 mL 0.7035 mL 1.4070 mL 3.5176 mL
25 mM 0.1126 mL 0.5628 mL 1.1256 mL 2.8140 mL
30 mM 0.0938 mL 0.4690 mL 0.9380 mL 2.3450 mL
40 mM 0.0704 mL 0.3518 mL 0.7035 mL 1.7588 mL
50 mM 0.0563 mL 0.2814 mL 0.5628 mL 1.4070 mL
60 mM 0.0469 mL 0.2345 mL 0.4690 mL 1.1725 mL
80 mM 0.0352 mL 0.1759 mL 0.3518 mL 0.8794 mL
100 mM 0.0281 mL 0.1407 mL 0.2814 mL 0.7035 mL
Help & FAQs
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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產(chǎn)品名稱:
Vidofludimus
目錄號(hào):
HY-14908
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