雷马曲班
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- CAS号:
- 116649-85-5
- 英文名:
- Ramatroban
- 英文别名:
- Baynas;CS-1350;BAY-U3405;RAMATROBAN;RaMantroban;Ray ma music class;BAY U3405; BAY-U3405;RaMatroban(BAY-u3405);Ramatroban for research;RAFFINOSE UNDECAACETATE, D-(+)-(RG)
- 中文名:
- 雷马曲班
- 中文别名:
- 雷马曲斑;雷马曲班;3R-(4-氟苯磺酰氨基)-1,2,3,4-四氢化-9H-咔唑-9-丙酸;3R-[[(4-氟苯基)磺酰]氨基]-1,2,3,4-四氢-9H-咔唑-9-丙 酸;(R)-3-(3-(4-氟苯基磺酰胺基)-3,4-二氢-1H-咔唑-9(2H)-基)丙酸
- CBNumber:
- CB5735921
- 分子式:
- C21H21FN2O4S
- 分子量:
- 416.47
- MOL File:
- 116649-85-5.mol
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雷马曲班化学性质
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熔点:
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134-135°
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比旋光度:
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D +70.1° (c = 1.0 in methanol)
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沸点:
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654.7±65.0 °C(Predicted)
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密度:
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1.43±0.1 g/cm3(Predicted)
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储存条件:
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Sealed in dry,2-8°C
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溶解度:
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DMSO: ≥40mg/mL
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形态:
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solid
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酸度系数(pKa):
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4.60±0.10(Predicted)
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颜色:
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white
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CAS 数据库:
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116649-85-5(CAS DataBase Reference)
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雷马曲班性质、用途与生产工艺
雷马曲班由德国拜耳公司研制，是作为抗心血管疾病药物开发的TP抑制剂，与日本新药株式会社合作在日本推广上市。仅在日本被批准为治疗哮喘和过敏性鼻炎的药物。
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)。
| 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.
用途
雷马曲班为高效的选择性TxA2/PGH2受体拮抗剂，可与平滑肌和血小板的TxA2受体特异性结合。雷马曲班的抗过敏反应基于抑制血管通透性和鼻粘膜高敏性及防止其它炎性反应发生。用于过敏性鼻炎。
雷马曲班
上下游产品信息
上游原料
1,2,4,9-四氢螺[咔唑-3,2'-[1,3]二氧戊环]
1,2,4,9-四氢咔唑-3-酮
(R)-3-氨基-1,2,3,4-四氢咔唑
1,4-环己二酮单乙二醇缩酮
苯肼
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-B0745 | Ramatroban | | 5 mg | 425元 |
| 2024/01/25 | HY-B0745 | 雷马曲班
Ramatroban | 116649-85-5 | 10mg | 680元 |
雷马曲班
生产厂家
全球有 186家供应商
雷马曲班国内生产厂家
116649-85-5, 雷马曲班 相关搜索:
- Pharmaceuticals
- Intermediates & Fine Chemicals
- Inhibitors
- 药靶配体
- 化学试剂
- 生物试剂
- 日用化学品
- 原料药
- 医药化工类
- 医药原料
- 医药原料
- 医药 抗组胺药
- 医药原料药
- 小分子抑制剂，天然产物
- 小分子抑制剂
- 医药中间体
- C21H21FN2O4S
- (R)-3-(3-(4-氟苯基磺酰胺基)-3,4-二氢-1H-咔唑-9(2H)-基)丙酸
- 雷马曲斑
- 3R-[[(4-氟苯基)磺酰]氨基]-1,2,3,4-四氢-9H-咔唑-9-丙 酸
- 雷马曲班
- 3R-(4-氟苯磺酰氨基)-1,2,3,4-四氢化-9H-咔唑-9-丙酸
- 116649-85-5
- Ray ma music class
- (R)-3-[3-[(4-Fluorophenyl)sulfonamido]-1,2,3,4-tetrahydro-9H-carbazol-9-yl]propanoic Acid
- 9H-Carbazole-9-propanoic acid, 3-[[(4-fluorophenyl)sulfonyl]amino]-1,2,3,4-tetrahydro-, (3R)-
- 3-(1,2,3,4-tetrahydrocarbazol-9-yl)propanoic acid [(4-fluorophenyl)sulfonylamino] ester
- CS-1350
- BAY U3405; BAY-U3405
- RAMATROBAN
- RaMantroban
- Ramatroban for research
- 3R-[[(4-Fluorophenyl)sulfonyl]amino]-1,2,3,4-tetrahydro-9H-carbazole-9-
- Baynas
- 9H-Carbazole-9-propanoic acid, 3-[[(4-fluorophenyl)sulfonyl]amino]-1,2,3,4-tetrahydro-, (R)-
- 9H-Carbazole-9-propanoic acid, 3-[[(4-fluorophenyl)sulfonyl]amino]-1,2,3,4-tetrahydro-, (3R)- (9CI)
- RaMatroban(BAY-u3405)
- (3R)-3-[[(4-Fluorophenyl)sulfonyl]amino]-1,2,3,4-tetrahydro-9H-carbazole-9-propanoicacid
- RAFFINOSE UNDECAACETATE, D-(+)-(RG)
- (R)-3-(3-(4-fluorophenylsulfonamido)-3,4-dihydro-1H-carbazol-9(2H)-yl)propanoic acid
- 3-[(3R)-3-(4-Fluorophenylsulfonylamino)-1,2,3,4-tetrahydro-9H-carbazole-9-yl]propionic acid
- (3R)-3-[[(4-Fluorophenyl)sulfonyl]amino]-1,2,3,4-tetrahydro-9H-carbazole-9-propionic acid
- 3R-[[(4-FLUOROPHENYL)SULFONYL]AMINO]-1,2,3,4-TETRAHYDRO-9H-CARBAZOLE-9-PROPANOIC ACID
- BAY-U3405