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

SB-657510 是选择性的 urotensin II (UII) receptor (UT) 拮抗剂。 对于人,猴,猫,大鼠和小鼠的受体的 Ki 值分别为 61、17、30、65 和 56 nM。SB-657510 通过抑制 UII 诱导的人类血管内皮细胞中炎性介质,如粘附分子,细胞因子和组织因子上调发挥抗炎作用。

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SB-657510 Chemical Structure

SB-657510 Chemical Structure

CAS No. : 474960-44-6

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     可免费申领三个不同产品的试用装。

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2615
In-stock
5 mg ¥2350
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10 mg ¥3750
In-stock
25 mg ¥7500
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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].

体外研究
(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.
体内研究
(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 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (197.70 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 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
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.84%

参考文献

SB-657510 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 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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产品名称:
SB-657510
目录号:
HY-10656
需求量: