成人免费xx,国产又黄又湿又刺激不卡网站,成人性视频app菠萝网站,色天天天天

  2. Membrane Transporter/Ion Channel
  3. OAT URAT1
  4. Lesinurad

Lesinurad  (Synonyms: 雷西那德; RDEA594)

目錄號: HY-15258 純度: 99.96%
COA 產(chǎn)品使用指南

Lesinurad 是一種 URAT1 和 OAT 抑制劑，用作腎轉(zhuǎn)運蛋白OAT1 和OAT3 的底物，Km值分別為 0.85 和 2 μM。

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

我們將采用定制合成服務(wù)的方式為您快速提供所需產(chǎn)品和技術(shù)服務(wù)

Lesinurad Chemical Structure

Lesinurad Chemical Structure

CAS No. : 878672-00-5

1.  客戶無需承擔(dān)相應(yīng)的運輸費用。

2.  同一機構(gòu)（單位）同一產(chǎn)品試用裝僅限申領(lǐng)一次，同一機構(gòu)（單位）一年內(nèi)

     可免費申領(lǐng)三個不同產(chǎn)品的試用裝。

3.  試用裝只面向終端客戶。

規(guī)格 價格 是否有貨 數(shù)量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ￥605
In-stock
5 mg ￥550
In-stock
10 mg ￥700
In-stock
50 mg ￥1900
In-stock
100 mg ￥2300
In-stock
200 mg   詢價  
500 mg   詢價  

* Please select Quantity before adding items.

Customer Review

Other Forms of Lesinurad:

MCE 顧客使用本產(chǎn)品發(fā)表的 2 篇科研文獻

  • 生物活性

  • 實驗參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

Lesinurad is a URAT1 and OAT inhibitor, is determined to be a substrate for the kidney transporters OAT1 and OAT3 with Km values of 0.85 and 2 μM, respectively.

IC50 & Target

Km: 0.85 μM (OAT1), 2 μM (OAT3)[1]
細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
15.1 μM
Compound: (-)-lesinurad
Inhibition of human URAT1 expressed in HEK293 cells assessed as inhibition of [14C]uric acid uptake preincubated for 15 mins followed by [14C]uric acid addition measured after 10 mins by liquid scintillation counting method
Inhibition of human URAT1 expressed in HEK293 cells assessed as inhibition of [14C]uric acid uptake preincubated for 15 mins followed by [14C]uric acid addition measured after 10 mins by liquid scintillation counting method
[PMID: 28337320]
HEK293 IC50
2.03 μM
Compound: 12
Inhibition of human OAT4 expressed in HEK293 cells by assessed as [14C]urate uptake preincubated for 5 mins followed by [14C]urate addition and measured after 10 mins by liquid scintillation counting method
Inhibition of human OAT4 expressed in HEK293 cells by assessed as [14C]urate uptake preincubated for 5 mins followed by [14C]urate addition and measured after 10 mins by liquid scintillation counting method
[PMID: 31774679]
HEK293 IC50
4.4 μM
Compound: (+)-lesinurad
Inhibition of human URAT1 expressed in HEK293 cells assessed as inhibition of [14C]uric acid uptake preincubated for 15 mins followed by [14C]uric acid addition measured after 10 mins by liquid scintillation counting method
Inhibition of human URAT1 expressed in HEK293 cells assessed as inhibition of [14C]uric acid uptake preincubated for 15 mins followed by [14C]uric acid addition measured after 10 mins by liquid scintillation counting method
[PMID: 28337320]
HEK293 IC50
7.3 μM
Compound: (+/-)-Lesinurad
Inhibition of human URAT1 expressed in HEK293 cells assessed as inhibition of [14C]uric acid uptake preincubated for 15 mins followed by [14C]uric acid addition measured after 10 mins by liquid scintillation counting method
Inhibition of human URAT1 expressed in HEK293 cells assessed as inhibition of [14C]uric acid uptake preincubated for 15 mins followed by [14C]uric acid addition measured after 10 mins by liquid scintillation counting method
[PMID: 28337320]
體外研究
(In Vitro)

Lesinurad 是一種新型選擇性尿酸重吸收抑制劑 (SURI)。Lesinurad 被確定為腎臟轉(zhuǎn)運蛋白有機陰離子轉(zhuǎn)運蛋白 (OAT1) 和 OAT3 的底物，Km 值分別為 0.85 和 2 μM[1]。Lesinurad (RDEA594) 是一種 URAT1 和 OAT 抑制劑，可增加近端腎小管尿酸鹽排泄[2]。Lesinurad (RDEA594) 是一種潛在的尿酸降低劑，通過抑制尿酸再攝取，表現(xiàn)出良好的 p450 特征，抑制 CYP2C9 和 CYP2C8，IC50 分別為 14.4 μM 和 16.2 μM。Lesinurad 對 CYP1A2、CYP2C19 和 CYP2D6 的 IC50 均高于 100 μM[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

Lesinurad (RDEA594) 顯示出比其前藥 RDEA806 更好的藥代動力學(xué)。100 mg 劑量的 Lesinurad 表現(xiàn)出的藥理作用范圍與 300 mg 至 800 mg 單劑量 RDEA806 產(chǎn)生的藥理作用相同[3]。

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

404.28

Formula

C17H14BrN3O2S
CAS 號
性狀

固體

顏色

White to off-white

中文名稱

雷西那德
運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
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)胞實驗： 

DMSO 中的溶解度 : 100 mg/mL (247.35 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.4735 mL 12.3677 mL 24.7353 mL
5 mM 0.4947 mL 2.4735 mL 4.9471 mL
查看完整儲備液配制表

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

  • 摩爾計算器

  • 稀釋計算器

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

動物實驗：

請根據(jù)您的 實驗動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，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

    請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.18 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 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

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

    Solubility: ≥ 2.5 mg/mL (6.18 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

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

    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。
動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動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。
計算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，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，請謹(jǐn)慎選擇該方案。
請確保第一步儲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: 99.96%

參考文獻
Cell Assay
[1]

Validated oocytes, HEK293, MDCK-II, Caco-2 or MDCK-MDR1 cell systems are used to study the interaction of Lesinurad with membrane transporters localized to the kidney (OAT1, OAT3, OCT2, MATE1, and MATE2K) or liver (P-gp, BCRP, OATP1B1, OATP1B3, and OCT1). Xenopus laevis oocytes are injected with OAT1 or OAT3 cRNA or control (water) while HEK293 cells are stably transfected with MATE1, MATE2K, or vector and MDCK-II cells with hOATP1B1, hOATP1B3, hOCT1, hOCT2, or vector. The MDCKII cell line is stably transfected with the human MDR1 gene to create a P-gp cell line. The interaction of Lesinurad with BCRP relied on the endogenous expression in Caco-2 cells. All cells are cultured with growth medium according to standard methodology. In order to determine whether Lesinurad is a substrate for a transporter, cells are incubated with [14C]-labeled Lesinurad at various concentrations and the amount of Lesinurad taken up by the cells determined by subtracting the uptake in vector cells from that in the transfected cells. The uptake of a [3H]-labeled known substrate of the transporter served as the positive control. Inhibition of a transporter by Lesinurad is determined by incubating cells with a fixed concentration of [3H]-labeled known substrate and various concentrations of unlabeled Lesinurad. Inhibition by a known inhibitor of each transporter served as the positive control. Cells are incubated for the appropriate amount of time. All reactions are terminated by the addition of ice-cold medium. The cells are then rinsed with medium and lysed[1].

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

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1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 2.4735 mL 12.3677 mL 24.7353 mL 61.8383 mL
5 mM 0.4947 mL 2.4735 mL 4.9471 mL 12.3677 mL
10 mM 0.2474 mL 1.2368 mL 2.4735 mL 6.1838 mL
15 mM 0.1649 mL 0.8245 mL 1.6490 mL 4.1226 mL
20 mM 0.1237 mL 0.6184 mL 1.2368 mL 3.0919 mL
25 mM 0.0989 mL 0.4947 mL 0.9894 mL 2.4735 mL
30 mM 0.0825 mL 0.4123 mL 0.8245 mL 2.0613 mL
40 mM 0.0618 mL 0.3092 mL 0.6184 mL 1.5460 mL
50 mM 0.0495 mL 0.2474 mL 0.4947 mL 1.2368 mL
60 mM 0.0412 mL 0.2061 mL 0.4123 mL 1.0306 mL
80 mM 0.0309 mL 0.1546 mL 0.3092 mL 0.7730 mL
100 mM 0.0247 mL 0.1237 mL 0.2474 mL 0.6184 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    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.

您最近查看的產(chǎn)品:

Your information is safe with us. * Required Fields.

   產(chǎn)品名稱：

  

* 需求量：

* 客戶姓名：

 

* Email：

* 電話：

 

* 公司或機構(gòu)名稱：

   留言給我們：

Bulk Inquiry

Inquiry Information

產(chǎn)品名稱：
Lesinurad
目錄號：
HY-15258
需求量：