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S1P5 receptor antagonist 1

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Catalog No. T218351 Copy Product Info
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S1P5 receptor antagonist 1 is a selective antagonist of the S1P5 receptor that is capable of crossing the blood-brain barrier. It has an EC50 of 0.1 nM and a Ki of 4.4 nM. This compound inhibits the migration of natural killer cells towards sphingosine 1-phosphate in vitro, while having no effect on T cell migration. S1P5 receptor antagonist 1 is applicable in central nervous system disease research.

S1P5 receptor antagonist 1

Cas No. 1621065-22-2
Pack SizePriceUSA StockGlobal StockQuantity
10 mgInquiry10-14 weeks10-14 weeks
50 mgInquiry10-14 weeks10-14 weeks
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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For research use only—not for human use. No sales to individuals. Use as intended only.
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Product Introduction

Bioactivity
Description
S1P5 receptor antagonist 1 is a selective antagonist of the S1P5 receptor that is capable of crossing the blood-brain barrier. It has an EC50 of 0.1 nM and a Ki of 4.4 nM. This compound inhibits the migration of natural killer cells towards sphingosine 1-phosphate in vitro, while having no effect on T cell migration. S1P5 receptor antagonist 1 is applicable in central nervous system disease research.
In vitro
S1P5 receptor antagonist 1 (Compound 15) inhibits the migration of mouse spleen NK cells towards S1P with an IC50 of 553 nM, tested at concentrations ranging from 1-25000 nM for 1 hour. This compound does not affect the migration of naive T cells from the mouse spleen, although it exhibits a biphasic response: migration is enhanced at 100 nM but is inhibited at higher doses. S1P5 receptor antagonist 1 shows good in vitro hepatocyte stability, demonstrating a Qh% of 30% in rat hepatocytes and 49% in human hepatocytes.
In vivo
Compound 15, an S1P5 receptor antagonist, administered to rats either orally or via intravenous injection at doses of 1-5 mg/kg, results in optimal systemic exposure, achieves 92% oral bioavailability, and consistently penetrates the blood-brain barrier.
Chemical Properties
Molecular Weight437.61
FormulaC28H39NO3
Cas No.1621065-22-2
SmilesC(C=1C2=C(C(C)=CC1O[C@@H]3CC[C@@H](C(C)(C)C)CC3)C=CC=C2)N4CCC(C(O)=O)CC4
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 µL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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g
µL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
Related Tags: S1P5 receptor antagonist 1 in vivo | S1P5 receptor antagonist 1 in vitro | S1P5 receptor antagonist 1 formula | S1P5 receptor antagonist 1 molecular weight