1. GPCR/G Protein
  2. Bradykinin Receptor
  3. SSR240612

SSR240612 是一种有效的,可口服的,特异性的非肽类缓激肽 B1 (bradykinin B1) 受体拮抗剂,对 bradykinin B1 受体(在人 MRC5 细胞和表达人 B1 受体的 HEK 细胞)的 Ki 值分别为 0.48 nM,0.73 nM;对 B2 受体 (在豚鼠回肠膜和表达人 B1 受体的 CHO 细胞) 的 Ki 较弱,分别为 481 nM 和 358 nM。

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SSR240612 Chemical Structure

SSR240612 Chemical Structure

CAS No. : 464930-42-5

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5 mg ¥6900
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查看 Bradykinin Receptor 亚型特异性产品:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

SSR240612 is a potent, and orally active specific non-peptide bradykinin B1 receptor antagonist, with Kis of 0.48 nM and 0.73 nM for B1 kinin receptors of human fibroblast MRC5 and HEK cells expressing human B1 receptors, 481 nM and 358 nM for B2 receptors of guinea pig ileum membranes and CHO cells expressing human B1 receptor, respectively.

IC50 & Target

Ki: 0.48 nM (bradykinin B1 receptor, Human MRC5), 0.73 nM (bradykinin B1 receptor, Human HEK-B1), 481 nM (bradykinin B2 receptor, guinea pig ileum membranes), 358 nM (bradykinin B2 receptor, Human CHO-B2)[1]

体外研究
(In Vitro)

SSR240612 is a potent bradykinin B1 receptor antagonist, with Kis of 0.48 nM and 0.73 nM for B2 kinin receptors of human fibroblast MRC5 and HEK cells expressing human B1 receptors, 481 nM and 358 nM for B1 receptors of guinea pig ileum membranes and CHO cells expressing human B1 receptor, respectively. SSR240612 inhibits inositol phosphate 1 formation with an IC50 of 1.9 nM, but shows no obvious effect on inositol phosphate-1 formation induced by BK (3 nM) activation of B2 receptor in human fibroblast MRC5[1].

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

体内研究
(In Vivo)

SSR240612 (10 mg/kg p.o. or 0.3, 1 mg/kg i.p.) obviously blocks the des-Arg9-BK-induced paw edema in the mice. SSR240612 (10 and 30 mg/kg) reduces the duration of the late phase of paw licking in a dose dependent manner in the formalin model of inflammation in mice. SSR240612 (0.3, 3, and 30 mg/kg, p.o.) treatment before capsaicin potently and non-concentration-dependently reduces the ear edema. SSR240612 (0.3 mg/kg, i.v.) also suppresses the tissue destruction and neutrophil accumulation in the rat intestine, after splanchnic artery occlusion/reperfusion. Moreover, SSR240612 (1 and 3 mg/kg p.o.) dramacally increases the withdrawal latencies in the thermal hyperalgesia induced by UV irradiation in rats[1]. SSR240612 inhibits tactile and cold allodynia at 3 h in glucose-fed rats but had no effect in control rats with ID50s of 5.5 and 7.1 mg/kg, respectively. SSR240612 shows no effect on plasma glucose and insulin, insulin resistance (HOMA index) and aortic superoxide anion production in glucose-fed rats at 10 mg/kg[2].

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

分子量

793.41

Formula

C42H53ClN4O7S

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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 50 mg/mL (63.02 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 1.2604 mL 6.3019 mL 12.6038 mL
5 mM 0.2521 mL 1.2604 mL 2.5208 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 (sealed storage, away from moisture)。-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

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

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (3.15 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    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;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (3.15 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    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。

    20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
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
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.51%

参考文献
Kinase Assay
[1]

[3H]Lys0-des-Arg9-BK binding to cell membranes is performed in binding buffer of the following composition: 137 mM NaCl, 5.4 mM KCl, 1.05 mM MgCl2, 1.8 mM CaCl2, 1.2 mM NaH2PO4, 15.5 mM NaHCO3, 10 mM HEPES, 1 g/L bovine serum albumin (BSA), 140 mg/L bacitracin, and 1 μM captopril, pH 7.4. Membranes are incubated for 30 min at 25°C in 500 μL of binding buffer containing 1 nM [3H]Lys0-des-Arg9-BK for competition curves or 0.1 to 10 nM for saturation isotherms. Filters are washed three times with 5 mL of binding buffer, and radioactivity is determined by liquid scintillation spectrometry. Nonspecific binding is determined by the addition of 1 μM of unlabeled Lys0-des-Arg9BK[1].

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

Animal Administration
[1]

Mice[1]
Groups of eight male albino mice under isoflurane anesthesia receive a 20-μL intraplantar injection into the right hind paw of 5 μg of IL-1β in phosphate-buffered saline/0.1% BSA. Forty minutes later (T = 0), mice under anesthesia receive a 20-μL intraplantar injection in the same paw of des-Arg9-BK (10 μg/paw) in water. SSR240612 or vehicle [5% (v/v) ethanol and 5% (v/v) Tween 80 in water] is administered by oral route at the doses of 1, 3, and 10 mg/kg 1 h before des-Arg9-BK injection and by intraperitoneal route at the doses of 0.1, 0.3, and 1 mg/kg 40 min before des-Arg9-BK injection. Paw volume is measured with a plethysmometer at T = -2 h (initial measurement) and at several times after edema induction (T = 20, 40, 60, and 120 min). Paw edema volume is expressed in milliliters as the difference between the paw volume at each time after edema induction and the initial paw volume. Results for each group are expressed as mean ± S.E.M. of individual paw edema volumes. Statistical analysis is performed after verification of normality and homogeneity of variances using repeated ANOVA, then Duncan's test, treated groups versus des-Arg9-BK control group[1].
Rats[1]
SSR240612 (suspended with 0.1% Tween 80 in saline) is administered by the oral route in a volume of 20 mL/kg, 2 h before the thermal hyperalgesia measurement. In the time course study, the compound is administered at 3 mg/kg p.o. 0.08, 0.25, 0.5, 1, 2, 4, 6, 8, and 24 h before measuring the withdrawal latencies in rats. Results are expressed in seconds as mean withdrawal latencies (s) ± S.E.M., and statistical analyses are performed using a two-way ANOVA followed by Dunnett's test[1].

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

参考文献

SSR240612 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 (sealed storage, away from moisture)。-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 1.2604 mL 6.3019 mL 12.6038 mL 31.5096 mL
5 mM 0.2521 mL 1.2604 mL 2.5208 mL 6.3019 mL
10 mM 0.1260 mL 0.6302 mL 1.2604 mL 3.1510 mL
15 mM 0.0840 mL 0.4201 mL 0.8403 mL 2.1006 mL
20 mM 0.0630 mL 0.3151 mL 0.6302 mL 1.5755 mL
25 mM 0.0504 mL 0.2521 mL 0.5042 mL 1.2604 mL
30 mM 0.0420 mL 0.2101 mL 0.4201 mL 1.0503 mL
40 mM 0.0315 mL 0.1575 mL 0.3151 mL 0.7877 mL
50 mM 0.0252 mL 0.1260 mL 0.2521 mL 0.6302 mL
60 mM 0.0210 mL 0.1050 mL 0.2101 mL 0.5252 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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SSR240612
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HY-15039
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