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SSR240612

产品编号 T5048 CAS 464930-42-5

SSR240612 是口服有活性的非肽类缓激肽 B1 (bradykinin B1) 受体特异性拮抗剂。

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SSR240612, CAS 464930-42-5

规格	价格/CNY	货期
1 mg	￥ 2,480	现货
5 mg	￥ 5,720	现货
10 mg	￥ 7,780	现货
25 mg	￥ 11,500	现货
50 mg	￥ 15,600	现货
100 mg	￥ 20,800	现货

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	SSR240612 is a potent, and orally active specific non-peptide bradykinin B1 receptor antagonist (Kis = 0.48-0.73 and 358-481 nM for B1 and B2 receptors, respectively).
靶点活性	Bradykinin B1 (human HEK-B1):0.73 nM (Ki), Bradykinin B2 (human CHO-B2):358 nM (Ki), Bradykinin B1 (human MRC5):0.48 nM (Ki)
体外活性	SSR240612 inhibited the binding of [(3)H]Lys(0)-des-Arg(9)-BK to the B(1) receptor in human fibroblast MRC5 and to recombinant human B(1) receptor expressed in human embryonic kidney cells with inhibition constants (K(i)) of 0.48 and 0.73 nM, respectively. SSR240612 inhibited Lys(0)-desAr(9)-BK (10 nM)-induced inositol monophosphate formation in human fibroblast MRC5, with an IC(50) of 1.9 nM [1]. M. tuberculosis was not susceptible to the concentrations of antagonists tested, which suggests that the minimum inhibitory concentration values are larger than 250 μM for SSR240612 [2].
体内活性	SSR240612 inhibited des-Arg(9)-BK-induced paw edema in mice (3 and 10 mg/kg p.o. and 0.3 and 1 mg/kg i.p.). Moreover, SSR240612 reduced capsaicin-induced ear edema in mice (0.3, 3 and 30 mg/kg p.o.) and tissue destruction and neutrophil accumulation in the rat intestine following splanchnic artery occlusion/reperfusion (0.3 mg/kg i.v.). The compound also inhibited thermal hyperalgesia induced by UV irradiation (1 and 3 mg/kg p.o.) and the late phase of nociceptive response to formalin in rats (10 and 30 mg/kg p.o.). SSR240612 (20 and 30 mg/kg p.o.) prevented neuropathic thermal pain induced by sciatic nerve constriction in the rat [1]. SSR240612 blocked tactile and cold allodynia at 3 h (ID(50)=5.5 and 7.1 mg/kg, respectively) in glucose-fed rats but had no effect in control rats. The antagonist (10 mg/kg) had no effect on plasma glucose and insulin, insulin resistance (HOMA index) and aortic superoxide anion production in glucose-fed rats [3].
激酶实验	MRC5 human fibroblasts and transfected HEK-293 cells expressing human B1 receptors were routinely grown in Dulbecco's modified Eagle's medium (DMEM) with Glutamax-I supplemented with 10% fetal calf serum and antibiotics. MRC5 were incubated for 4 h in DMEM containing 0.5 μg/ml interleukin-1β (IL-1β) to induce B1 receptor synthesis. Cells were scraped and homogenized for 1 min using a Polytron (setting 8) in 25 mM TES-HCl containing 1 mM 1-10 phenantrolin. Homogenates were centrifuged at 40,000g for 15 min at 4°C, and pellets were resuspended in the same buffer using the Polytron (setting 8) for 1 min. Membranes were pelleted at 40,000g for 10 min at 4°C, resuspended in the same buffer, and conserved at 80°C. [3H]Lys0-des-Arg9-BK binding to cell membranes was 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 were 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. The reaction was terminated by filtration using a Brandel Harvester onto GF/B Whatman filters previously soaked for 2 h in 0.1% polyethyleneimine. Filters were washed three times with 5 ml of binding buffer, and radioactivity was determined by liquid scintillation spectrometry. Nonspecific binding was determined by the addition of 1 μM of unlabeled Lys0 -des-Arg9 BK [1].
细胞实验	[3H]Inositol phosphate1 accumulation was measured in MRC5 fibroblasts labeled with [3H]myoinositol according to the method described by Oury-Donat et al. Cells cultured in 6-well plates were labeled for 48 h with 5 μCi/ml [3H]myoinositol added to the culture medium (DMEM). Cells were then incubated for 4 h in DMEM containing 0.5 μg/ml IL-1β to induce B1 receptor synthesis. Agonist stimulation of inositol phosphate 1 accumulation was performed in DMEM containing 50 mM LiCl and test compounds. Antagonists were added 15 min before 10 nM Lys0-desArg10BK. After 30 min of incubation at 37°C, the medium was discarded, and the reaction was stopped by rapid addition of 1 ml of cold methanol and 1 N HCl (v/v). The cells were scraped, and the suspension was transferred to a glass tube with 1 ml of chloroform and 20 μl of 12 N HCl. The aqueous phase was neutralized by 350 μl of 1 M NaHCO3 and applied to 1 ml of Dowex AG1 × eight columns. [3H]inositol phosphate 1 was eluted with 0.2 M ammonium formate and 0.1 M formic acid. Radioactivity was measured by liquid scintillation spectrometry [1].
动物实验	Groups of eight male albino mice under isoflurane anesthesia received 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 received, under anesthesia, 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] was 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 was 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 was 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 [1].

分子量	793.41
分子式	C42H53ClN4O7S
CAS No.	464930-42-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: Insoluble

DMSO: 100 mg/mL (126 mM)

溶液配制表

可选溶剂	浓度体积质量	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	0.126 mL	0.6302 mL	1.2604 mL	3.151 mL
	20 mM	0.063 mL	0.3151 mL	0.6302 mL	1.5755 mL
	50 mM	0.0252 mL	0.126 mL	0.2521 mL	0.6302 mL
	100 mM	0.0126 mL	0.063 mL	0.126 mL	0.3151 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Gougat J, et al. SSR240612 [(2R)-2-[((3R)-3-(1,3-benzodioxol-5-yl)-3-[[(6-methoxy-2-naphthyl)sulfonyl]amino]propanoyl)amino]-3-(4-[[2R,6S)-2,6-dimethylpiperidinyl]methyl]phenyl)-N-isopropyl-N-methylpropanamide hydrochloride], a new nonpeptide antagonist of the bradykinin B1 receptor: biochemical and pharmacological characterization. J Pharmacol Exp Ther. 2004 May;309(2):661-9. 2. Rodrigues-Junior VS, et al. Effect of the bradykinin 1 receptor antagonist SSR240612 after oral administration in Mycobacterium tuberculosis-infected mice. Tuberculosis (Edinb). 2018 Mar;109:1-7. 3. Dias JP, et al. The kinin B1 receptor antagonist SSR240612 reverses tactile and cold allodynia in an experimental rat model of insulin resistance. Br J Pharmacol. 2007 Sep;152(2):280-7.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

SSR240612 464930-42-5 GPCR/G Protein Bradykinin Receptor SSR 240612 Inhibitor inhibit SSR-240612 inhibitor

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SSR240612

存储

溶解度

溶液配制表

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参考文献

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剂量换算

体内实验配液计算器

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