BAY u3405
(Synonyms: 雷马曲班; BAY u3405) 目录号 : GC15640
A dual TP and DP2/CRTH2 receptor antagonist
Cas No.:116649-85-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Kinase experiment: | CRTH2 transfectants are resuspended in binding buffer (50 mM Tris-HCl, pH 7.4, 40 mM MgCl2, 0.1% BSA, 0.1% NaN3). Cell suspension (2×105 cells), 3H-labeled PGD2, and various concentrations of Ramatroban (0.1 nM, 1 nM, 10 nM, 100 nM, 1 μM and 10 μM) are then mixed in a 96-well U-bottomed polypropylene plate and incubated in a final volume of 100 μL for 60 min at room temperature. After incubation, the cell suspension is transferred to a filtration plate and washed three times with binding buffer. Scintillant is added to the filtration plate, and radioactivity remaining on the filter is measured by a scintillation counter. Nonspecific binding is determined by incubating the cell suspension and 3H-labeled PGD2 in the presence of 1 μM unlabeled PGD2[2]. |
Cell experiment: | Human eosinophils are purified and resuspended in migration buffer (20 mM HEPES, pH 7.6, 0.1% BSA, Hanks' solution) at a density of 6 ×106 cells/mL. Fifty microliters of the cell suspension (3×105 cells/well) is then dispensed into the upper chamber of a 96-well type chemotaxis chamber (pore diameter=5 μm), and 30 μL of ligand solution is added to the lower chamber. Cells are preincubated with various concentrations of Ramatroban (0.1 nM, 1 nM, 10 nM, 100 nM, 1 μM and 10 μM) or BWA868C at 37°C for 10 min. The migration assays are performed in a humidified incubator at 37°C, 5% CO2 for 2 h. The number of cells migrating into the lower chamber is counted[2]. |
Animal experiment: | Mice[3]Five micrograms of LPS (closed columns) or saline (open columns) are intraperitoneally injected into CRTH2+/+ mice. CRTH2+/+ mice are pretreated intraperitoneally for 1 h with 30 mg/kg Ramatroban. |
References: [1]. Stearns BA, et al. Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine modelof allergic rhinitis. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4647-51. | |
IC50: 100-170 nM
BAY u3405 is a DP2 receptor antagonist.
The biological effects of prostaglandin D2 (PGD2) are transduced by at least two 7-transmembrane G protein-coupled receptors, designated DP1 and DP2/CRTH2.
In vitro: BAY u3405 showed significant inhibitory effects on the binding of 3H-labeled PGD2 to CRTH2, albeit with much lower potency. BAY u3405 and indomethacin also inhibited PGD2-induced Ca2+ mobilization in CRTH2 transfectants to almost the same extent. However, indomethacin but not BAY u3405 was confirmed as an agonist of Ca2+ mobilization at concentrations greater than 10 nM [1].
In vivo: For rat with splanchnic artery occlusion shock, administration of BAY u3405 at 30 mg/kg i.v. could significantly increase the survival time and survival rate, improve mean arterial blood pressure, reduce the plasma levels of myocardial depressant factor, partially restore macrophage phagocytosis and lower MPO activity in both the ileum and the lung [2].
Clinical trial: Twelve adult asthmatics were studied in a randomized, double-blind, placebo-controlled study. Three subjects were withdrawn from the evaluation. The Dmin value of 0.533 U after the BAY u3405 treatment was significantly greater than that of 0.135 U after the placebo treatment. There were no safety concerns in either treatment group [3].
References:
[1] Sugimoto, H. ,Shichijo, M.,Iino, T., et al. An orally bioavailable small molecule antagonist of CRTH2, Ramatroban (BAY u3405), inhibits prostaglandin D2-induced eosinophil migration in vitro. Journal of Pharmacology and Experimental Therapeutics 305, 347-352 (2003).
[2] Canale P, Squadrito F, Altavilla D, Ioculano M, Campo GM, Squadrito G, Urna G, Sardella A, Caputi AP. Beneficial effects of BAY u3405, a novel thromboxane A2 receptor antagonist, in splanchnic artery occlusion shock. Pharmacology. 1994 Dec;49(6):376-85.
[3] Aizawa H, Shigyo M, Nogami H, Hirose T, Hara N. BAY u3405, a thromboxane A2 antagonist, reduces bronchial hyperresponsiveness in asthmatics. Chest. 1996 Feb;109(2):338-42.
| Cas No. | 116649-85-5 | SDF | |
| 别名 | 雷马曲班; BAY u3405 | ||
| 化学名 | 3R-[[(4-fluorophenyl)sulfonyl]amino]-1,2,3,4-tetrahydro-9H-carbazole-9-propanoic acid | ||
| Canonical SMILES | O=S(N[C@H](CC1)CC2=C1N(CCC(O)=O)C3=CC=CC=C23)(C4=CC=C(F)C=C4)=O | ||
| 分子式 | C21H21FN2O4S | 分子量 | 416.5 |
| 溶解度 | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.401 mL | 12.0048 mL | 24.0096 mL |
| 5 mM | 0.4802 mL | 2.401 mL | 4.8019 mL |
| 10 mM | 0.2401 mL | 1.2005 mL | 2.401 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
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