Ramatroban

Synonyms: BAY u 3405

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.

Ramatroban Chemical Structure

Ramatroban Chemical Structure

CAS: 116649-85-5

Purity & Quality Control

Batch: Purity: 99.50%
99.50

Ramatroban Related Products

Choose Selective Prostaglandin Receptor Inhibitors

Biological Activity

Description 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.
Targets
TxA2 receptor [1]
In vitro
In vitro Ramatroban can block the PGD2 receptor, chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2). Ramatroban can suppress the expression of monocyte chemoattractant protein-1 (MCP-1) and adhesion molecules in endothelial cells and prevent exacerbation of inflammation by blocking these responses. It has inhibitory effects on platelet aggregation and vascular smooth muscle contraction. Ramatroban significantly inhibited binding of [3H]PGD2 to CRTh2 with an IC50 value of 100 nM. It also inhibited, in a concentration-dependent manner, PGD2-induced Ca2+ mobilization in CRTh2 transfectants with an IC50 = 30 nM and suppressed migration of human eosinophils induced by PGD2 with an IC50 = 170 nM[1].
In Vivo
In vivo In hypercholesterolemic rabbits, ramatroban prevents macrophage infiltration through MCP-1 downregulation and neointimal formation after balloon injury and attenuates vascular response to acetylcholine. The pharmacokinetic parameters after single oral administration of 75 mg ramatroban were studied in fasting healthy adult volunteers: relative bioavailability of ramatroban tablets (as compared with aqueous solution) was 80.3%. The pharmacokinetics of ramatroban at doses ranging from 25 to 150 mg was found to be linear. When a single dose of 50 mg of ramatroban was given orally to healthy volunteers postprandially, the AUC was 88.8% of that obtained in fasting state. A low total body clearance of ramatroban is shown in elderly subjects; After oral administration of [14C]ramatroban to male rats, maximum concentrations of radioactivity were higher in liver, kidneys and adipose tissues than in plasma. Other organs tissues had lower radioactivity levels than plasma. Radioactivity levels in most organs tissues declined in parallel with the decrease in the plasma radioactivity. In contrast, elimination of the radioactivity from the blood cells was relatively prolonged. Extremely low radioactivity levels were found only in the brain. The ratio of brain-to-plasma levels was as low as 8% at the maximum[1].

Chemical Information & Solubility

Molecular Weight 416.47 Formula

C21H21FN2O4S

CAS No. 116649-85-5 SDF --
Smiles C1CC2=C(CC1NS(=O)(=O)C3=CC=C(C=C3)F)C4=CC=CC=C4N2CCC(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 83 mg/mL ( (199.29 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 83 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Ramatroban | Ramatroban supplier | purchase Ramatroban | Ramatroban cost | Ramatroban manufacturer | order Ramatroban | Ramatroban distributor