2+ | mobilization | Inhibitor | inhibitor | inhibit"/>

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  2. GPCR/G Protein
  3. Urotensin Receptor
  4. SB-657510

SB-657510 是選擇性的 urotensin II (UII) receptor (UT) 拮抗劑。 對(duì)于人，猴，貓，大鼠和小鼠的受體的 Ki 值分別為 61、17、30、65 和 56 nM。SB-657510 通過(guò)抑制 UII 誘導(dǎo)的人類血管內(nèi)皮細(xì)胞中炎性介質(zhì)，如粘附分子，細(xì)胞因子和組織因子上調(diào)發(fā)揮抗炎作用。

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SB-657510 Chemical Structure

SB-657510 Chemical Structure

CAS No. : 474960-44-6

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥2615
In-stock
5 mg ￥2350
In-stock
10 mg ￥3750
In-stock
25 mg 現(xiàn)貨 詢價(jià)
50 mg   詢價(jià)  
100 mg   詢價(jià)  

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Customer Review

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

SB-657510 is a selective urotensin II (UII) receptor (UT) antagonist. The Ki values are 61, 17, 30, 65 and 56 nM for human, monkey, cat, rat and mouse receptors, respectively. SB-657510 exerts anti-inflammatory effects by inhibiting UII-induced upregulation of inflammatory mediators such as adhesion molecules, cytokines, and tissue factor in human vascular endothelial cells[1][2].

體外研究
(In Vitro)

SB-657510 dramatically blocks the UII-induced increase in adhesion between U937 and EA.hy926 cell. SB-657510 (1 μM; 0.5-8 hours) blocks the expression of tissue factor induced by UII in endothelial cells[1].
SB-706375 (1-10000 nM) inhibits [Ca2+]i mobilization elicited by 10?nM hU-II with an IC50 of 180?nM[2].

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

Western Blot Analysis[1]

Cell Line: EA.hy926 cells (UII-induced)
Concentration: 1 μM
Incubation Time: 0.5, 1, 2, 4, 8 hours
Result: Remarkably decreased the UII-induced protein expression of tissue factor.
體內(nèi)研究
(In Vivo)

SB-657510 inhibits the progression of high-fat diet induced atherosclerosis and diabetes-associated atherosclerosis[1].
Levels of phosphorylated ERK are significantly attenuated in the aorta of SB-657510-treated (30 mg/kg/day) diabetic mice (Male Apoe KO mice)[3].

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

505.81

Formula

C19H22BrClN2O5S
CAS 號(hào)
性狀

固體

顏色

White to off-white

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 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 100 mg/mL (197.70 mM; 超聲助溶; 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)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 1.9770 mL 9.8851 mL 19.7703 mL
5 mM 0.3954 mL 1.9770 mL 3.9541 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, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(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

只
由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.84%

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, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(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 1.9770 mL 9.8851 mL 19.7703 mL 49.4257 mL
5 mM 0.3954 mL 1.9770 mL 3.9541 mL 9.8851 mL
10 mM 0.1977 mL 0.9885 mL 1.9770 mL 4.9426 mL
15 mM 0.1318 mL 0.6590 mL 1.3180 mL 3.2950 mL
20 mM 0.0989 mL 0.4943 mL 0.9885 mL 2.4713 mL
25 mM 0.0791 mL 0.3954 mL 0.7908 mL 1.9770 mL
30 mM 0.0659 mL 0.3295 mL 0.6590 mL 1.6475 mL
40 mM 0.0494 mL 0.2471 mL 0.4943 mL 1.2356 mL
50 mM 0.0395 mL 0.1977 mL 0.3954 mL 0.9885 mL
60 mM 0.0330 mL 0.1648 mL 0.3295 mL 0.8238 mL
80 mM 0.0247 mL 0.1236 mL 0.2471 mL 0.6178 mL
100 mM 0.0198 mL 0.0989 mL 0.1977 mL 0.4943 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.

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產(chǎn)品名稱：
SB-657510
目錄號(hào)：
HY-10656
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