BAY u3405|116649-85-5|(雷马曲班; BAY u3405)-陌孚医药/Medlife

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BAY u3405 (Synonyms: 雷马曲班; BAY u3405)

目录号: PC11447 纯度: ≥98%

CAS No. :116649-85-5

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中文名称

BAY u3405

中文别名

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;2,4-已二烯-1-醇;3R-[[(4-氟苯基)磺酰]氨基]-1,2,3,4-四氢-9H-咔唑-9-丙酸

英文名称

BAY u3405

英文别名

(R)-3-(3-(4-Fluorophenylsulfonamido)-3,4-dihydro-1H-carbazol-9(2H)-yl)propanoic acid;Ramatroban;BAY u3405;BAY-u 3405;3-[(3R)-3-[(4-fluorophenyl)sulfonylamino]-1,2,3,4-tetrahydrocarbazol-9-yl]propanoic acid;(+)-(3R)-3-[[(4-Fluorophenyl)sulfonyl]amino]-1,2,3,4-tetrahydro-9H-carbazole-9-propanoic acid;3R-[[(4-Fluorophenyl)sulfonyl]amino]-1,2,3,4-tetrahydro-9H-. carbazole-9-propanoic acid;Baynas;RaMantroban;RaMatroban(BAY-u3405);Ramatroban for research;RAFFINOSE UNDECAACETATE, D-(+)-(RG);3R-[[(4-Fluorophenyl)sulfonyl]amino]-1,2,3,4-tetrahydro-9H-carbazole-9-;3R-[[(4-FLUOROPHENYL)SULFONYL]AMINO]-1,2,3,4-TETRAHYDRO-9H-CARBAZOLE-9-PROPANOIC ACID;Rema Quban;Bay u 3405;Bay u 3406;C21H21FN2O4S;P1ALI72U6C;3-(4-Fluorophenylsulfonamido)-1,2,3,4-tetrahydro-9-carbazole propanoic acid;(+)-(3R)-3-(p-Fluorobenzenesulfonamido)-1,2,3,4-tetrahydrocarbazole-9-propionic acid;DSSTox_RID_81819;9H-Carbazole-9-propanoic acid, 3-(((4-fluorophenyl)sulfonyl

Cas No.

116649-85-5

分子式

C₂₁H₂₁FN₂O₄S

分子量

416.47

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

Ramatroban is a selective thromboxane A₂ (TxA₂, IC₅₀=14 nM) antagonist, which also antagonizes CRTH2 (IC₅₀=113 nM) by inhibiting PGD₂ binding.

性状

Solid

IC50 & Target[1][2]

hTP

14 nM (IC₅₀)

hDP2

113 nM (IC₅₀)

hDP2

33.4 μM (IC₅₀)

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. 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. H-labeled PGD₂ binds to a single site on CRTH2 transfectants with high affinity (K_D=6.3 nM, B_max=450 pM). Nonlabeled PGD₂ inhibits the binding of H-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 H-labeled PGD₂ to CRTH2, albeit with much lower potency (IC₅₀=100 nM). Ramatroban also inhibits PGD₂-induced Ca 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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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<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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

参考文献

[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. [Information]

[2]. Sugimoto H, et al. An orally bioavailable small molecule antagonist of CRTH2, ramatroban (BAY u3405), inhibits prostaglandin D₂-induced eosinophil migration 体外研究. J Pharmacol Exp Ther. 2003 Apr;305(1):347-52. [Information]

[3]. Haba R, et al. Central CRTH2, a second prostaglandin D₂ receptor, mediates emotional impairment in the lipopolysaccharide and tumor-induced sickness behavior model. J Neurosci. 2014 Feb 12;34(7):2514-23. [Information]

溶解度数据

体外研究:

DMSO : 125 mg/mL (300.14 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4011 mL	12.0057 mL	24.0113 mL
5 mM	0.4802 mL	2.4011 mL	4.8023 mL
10 mM	0.2401 mL	1.2006 mL	2.4011 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (4.99 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.99 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (4.99 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.99 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.99 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.99 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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