116649-85-5
基本信息
雷马曲班
3R-[[(4-氟苯基)磺酰]氨基]-1,2,3,4-四氢-9H-咔唑-9-丙 酸
BAY-U3405
RAMATROBAN
9H-Carbazole-9-propanoic acid, 3-[[(4-fluorophenyl)sulfonyl]amino]-1,2,3,4-tetrahydro-, (3R)- (9CI)
9H-Carbazole-9-propanoic acid, 3-[[(4-fluorophenyl)sulfonyl]amino]-1,2,3,4-tetrahydro-, (R)-
Baynas
3R-[[(4-Fluorophenyl)sulfonyl]amino]-1,2,3,4-tetrahydro-9H-carbazole-9-
Ramatroban for research
(3R)-3-[[(4-Fluorophenyl)sulfonyl]amino]-1,2,3,4-tetrahydro-9H-carbazole-9-propionic acid
3-[(3R)-3-(4-Fluorophenylsulfonylamino)-1,2,3,4-tetrahydro-9H-carbazole-9-yl]propionic acid
物理化学性质
| 熔点 | 134-135° |
| 比旋光度 | D +70.1° (c = 1.0 in methanol) |
| 沸点 | 654.7±65.0 °C(Predicted) |
| 密度 | 1.43±0.1 g/cm3(Predicted) |
| 储存条件 | Sealed in dry,2-8°C |
| 溶解度 | 二甲基亚砜：≥40mg/mL |
| 酸度系数(pKa) | 4.60±0.10(Predicted) |
| 形态 | 固体 |
| 颜色 | 白色 |
| CAS 数据库 | 116649-85-5(CAS DataBase Reference) |
| 用法用量 | 成人一日2次，每次75mg，早餐和晚餐后（或临睡前）口服。 |
| 注意事项 | 有出血倾向者、妇女月经期间、肝损伤者和老年人慎用。3R-(4-氟苯磺酰氨基)-1,2,3,4-四氢化-9H-咔唑-9-丙酸可与抗血小板药如噻氯匹定，血栓溶解药如尿激酶，抗凝药如肝素、华法林，水杨酸类制剂如阿司匹林，以及茶碱发生相互作用。 |
| 适 应 证 | 过敏性鼻炎。 |
| 不良反应 | 本品的不良反应包括GOP、GTP和胆红素升高、紫斑、凝血酶原时间（PT）/活化部分凝血活酶原时间（APTT）延长、皮下出血、腹泻、腹痛、消化不良和头痛等。 |
安全数据
| 危险性符号(GHS) |  GHS07 |
| 警示词 | 警告 |
| 危险性描述 | H315-H319-H335 |
| 防范说明 | P261-P264-P271-P280-P302+P352-P305+P351+P338 |
| 危险品标志 | Xi |
| 危险类别码 | 36/37/38 |
| 安全说明 | 26-36/37/39-45 |
| WGK Germany | 1 |
应用领域
化学品安全说明书(MSDS)
3R-[[(4-Fluorophenyl)sulfonyl]amino]-1,2,3,4-tetrahydro-9H-. carbazole-9-propanoic acid(116649-85-5).msds常见问题列表
| Target | Value |
|
TxA2 receptor
() |
Ramatroban is a potent human thromboxane receptor (hTP) antagonist with an IC 50 of 18 nM in a human TP binding assay. Ramatroban inhibits prostaglandin D 2 receptor DP2 (CRTH2) with an IC 50 of 113 nM in a human DP2 binding assay. Ramatroban also inhibits human CYP isoform CYP2C9 with an IC 50 of 15 μM. Ramatroban is a selective thromboxane-type prostanoid (TP) receptor antagonist. PGD 2 -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 PGD 2 -induced migration of eosinophils via CRTH2 blockade. 3 H-labeled PGD 2 binds to a single site on CRTH2 transfectants with high affinity (K D =6.3 nM, B max =450 pM). Nonlabeled PGD 2 inhibits the binding of 3 H-labeled PGD 2 to CRTH2 transfectants in a concentration-dependent manner with an EC 50 value of 2.7 nM. Ramatroban shows significant inhibitory effects on the binding of 3 H-labeled PGD 2 to CRTH2, albeit with much lower potency (IC 50 =100 nM). Ramatroban also inhibits PGD 2 -induced Ca 2+ mobilization in CRTH2 transfectants to almost the same extent with an IC 50 value of 30 nM. Ramatroban completely inhibits the PGD 2 -induced migration of eosinophils in a concentration-dependent manner with an IC 50 value of 170 nM.
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<0.01). In addition, tumor-impaired social interaction and object exploratory behavior in CRTH2 +/+ mice are completely reversed by a single injection of Ramatroban, even when the tumor is enlarged.