| CAS: | 116649-85-5 | |
| 分子式: | C21H21FN2O4S | |
| 分子量: | 416.47 | |
| 英文名称: |
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| 用途: | Ramatroban (BAY u 3405) is a thromboxane A2(TxA2) receptor antagonist with Ki value of 10 to 13 nM. It also antagonizes a newly identified PGD2 receptor, CRTh2 expressed on the inflammatory cells. |
| 货号 | 品牌 | 产品名称 | 规格 | 包装、参考价格 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
| B873294 | MACKLIN | Ramatroban | 99% | 71元/10mg; | 咨询 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||
储存：-20℃ 状态：白色到浅黄色到浅橙色粉末到晶体 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| R0144 | TCI | Ramatroban | >95.0%(T)(HPLC) | 990元/10MG; 2990元/50MG; | 咨询 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| R0531 | Sigma-Aldrich | Ramatroban | ≥98% (HPLC), solid | 1804.21元/5 MG; 6869.89元/25 MG; | 咨询 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||
产品说明 包装 5, 25 mg in glass bottle 生化/生理作用 Ramatroban is used for the treatment of allergic rhinitis as an antagonist of the thromboxane receptor. It is also an antagonist of the DP2 receptor with IC50 values of 100-170 nM. It is more potent at the DP2 receptor than the TP receptor by 4-5 fold. It is therefore a useful tool for the elucidation of PGD2/DP2 function in eosinophils, basophils, and other cells of the TH2 cell-type. 特点和优势 This compound was developed by Bayer. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here. 基本信息
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| HY-B0745 | MCE | Ramatroban,116649-85-5,雷马曲班_MCE(MedChemExpress) | 467元/10 mM * 1 mL in DMSO; 425元/5 mg; 680元/10 mg; 1300元/25 mg; 2100元/50 mg; 3200元/100 mg; | 咨询 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。 RamatrobanMCE 国际站：Ramatroban 品牌：MedChemExpress (MCE) 货号：HY-B0745 CAS 号：116649-85-5 生物活性：拉马曲班是一种选择性血栓素 A2 (TxA2, IC50=14 nM) 拮抗剂，它还能通过抑制 PGD2 结合来拮抗 CRTH2 (IC50=113 nM)。 体外研究(In Vitro)：Ramatroban is a potent human thromboxane receptor (hTP) antagonist with an IC50 of 18 nM in a human TP binding assay. Ramatroban inhibits prostaglandin D2 receptor DP2 (CRTH2) with an IC50 of 113 nM in a human DP2 binding assay. Ramatroban also inhibits human CYP isoform CYP2C9 with an IC50 of 15 μM[1]. Ramatroban is a selective thromboxane-type prostanoid (TP) receptor antagonist. PGD2-stimulated human eosinophil migration is shown to be mediated exclusively through activation of CRTH2, and surprisingly, these effects are completely inhibited by Ramatroban. Ramatroban is an antagonist for CRTH2, and inhibits PGD2-induced migration of eosinophils via CRTH2 blockade. 3H-labeled PGD2 binds to a single site on CRTH2 transfectants with high affinity (KD=6.3 nM, Bmax=450 pM). Nonlabeled PGD2 inhibits the binding of 3H-labeled PGD2 to CRTH2 transfectants in a concentration-dependent manner with an EC50 value of 2.7 nM. Ramatroban shows significant inhibitory effects on the binding of 3H-labeled PGD2 to CRTH2, albeit with much lower potency (IC50=100 nM). Ramatroban also inhibits PGD2-induced Ca2+ mobilization in CRTH2 transfectants to almost the same extent with an IC50 value of 30 nM. Ramatroban completely inhibits the PGD2-induced migration of eosinophils in a concentration-dependent manner with an IC50 value of 170 nM[2]. MCE尚未独立确认这些方法的准确性。 仅供参考。 体内研究(In Vivo)：Ramatroban is an orally bioavailable small molecule antagonist of CRTH2. Systemic administration of Ramatroban (30 mg/kg) in CRTH2+/+ mice produces the same effects as seen in CRTH2 deficiency. Ramatroban completely blocks LPS-induced decreases in social and object exploratory behavior (p+/+ mice are completely reversed by a single injection of Ramatroban, even when the tumor is enlarged[3]. MCE尚未独立确认这些方法的准确性。 仅供参考。 分子量：416.47 Formula：C21H21FN2O4S 性状：固体 颜色：White to off-white 中文名称：雷马曲班 运输条件：美国大陆地区的室温；其他地区可能有所不同。 储存方式：粉末 -20°C 3年 Kinase Assay [2]：将CRTH2转染细胞重悬于结合缓冲液（50 mM Tris-HCl，pH 7.4，40 mM MgCl₂，0.1% BSA，0.1% NaN₃）中。将细胞悬液（2×10⁵个细胞）、³H标记的PGD₂和不同浓度的拉马曲班（0.1 nM、1 nM、10 nM、100 nM、1 μM和10 μM）混合于96孔U型底聚丙烯板中，并在100 μL的最终体积下于室温孵育60分钟。孵育后，将细胞悬液转移至滤板，并用结合缓冲液洗涤三次。向滤板中加入闪烁液，用闪烁计数器测量滤膜上残留的放射性。非特异性结合通过在 1 μM 未标记 PGD2 存在的情况下孵育细胞悬浮液和 3H 标记的 PGD2 来确定[2]。 MCE 尚未独立确认这些方法的准确性。仅供参考。 Cell Assay [2]：纯化人嗜酸性粒细胞，并将其重悬于迁移缓冲液（20 mM HEPES，pH 7.6，0.1% BSA，Hanks 溶液）中，细胞密度为 6 × 10⁶ 个/mL。取 50 μL 细胞悬液（3 × 10⁵ 个细胞/孔）加入 96 孔趋化小室（孔径 5 μm）的上室，下室加入 30 μL 配体溶液。将细胞与不同浓度的拉马曲班（0.1 nM、1 nM、10 nM、100 nM、1 μM 和 10 μM）或 BWA868C 在 37°C 下预孵育 10 分钟。在 37°C、5% CO₂ 的加湿培养箱中进行迁移实验 2 小时。计数迁移到下室的细胞数量[2]。 MCE 尚未独立确认这些方法的准确性。仅供参考。 Animal Administration [3]：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. MCE尚未独立确认这些方法的准确性。 仅供参考。 提供质量检测报告：Data Sheet、SDS、COA、HNMR、CNMR、LCMS、产品使用指南 产品活性：Ramatroban 是一种选择性血栓素 A2 (TxA2，IC50=14 nM) 拮抗剂。Ramatroban 还通过抑制 PGD2 结合从而拮抗 CRTH2 (IC50=113 nM)。 相关产品：Pirfenidone | Phorbol 12-myristate 13-acetate | Pirfenidone (Standard) | Phorbol 12-myristate 13-acetate (Standard) | Y-27632 dihydrochloride | Y-27632 dihydrochloride | Y-27632 dihydrochloride (Standard) | RSL3 | Navitoclax | Navitoclax (Standard) | JTE-013 | Q-VD-OPh 热门产品线：抑制剂 | 稳定性同位素标记物 | 脂质 | 糖类 Trending products：Inhibitors | Isotope-Labeled Compounds | Lipids | Saccharides MCE 抑制剂: MedChemExpress 信号通路产品覆盖细胞凋亡、自噬、细胞周期与 DNA 损伤、表观遗传、GPCR/G 蛋白、免疫与炎症、JAK/STAT、MAPK/ERK、膜转运体与离子通道、代谢酶与蛋白酶、神经信号、NF-κB、PI3K/Akt/mTOR、PROTAC、蛋白酪氨酸激酶/受体酪氨酸激酶、干细胞/Wnt、TGF-β/Smad 及维生素 D/核受体等研究方向，为肿瘤、感染、炎症与免疫、神经系统疾病、代谢性疾病、心血管疾病和内分泌研究提供多维度的产品选择，助力客户发表文献超 80,000 篇。 相关产品可根据具体情况提供化学结构、作用靶点、生物活性、纯度、溶解度、体内外研究信息、参考文献及质量分析报告 (COA)等资料。 客户发表文献： 参考文献： 品牌介绍:
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