BMS-248360

Name: BMS-248360
Brand: TargetMol
SKU: T14672
Rating: 4.5 (1 reviews)

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Catalog No. T14672Cas No. 254737-87-6

BMS-248360 is a potent, orally active dual antagonist of both angiotensin II receptor (AT1) and endothelin A (ETA) receptor, with Kis of 10 nM and 1.9 nM for hAT1 and hETA receptors, respectively. BMS-248360 demonstrates hypertensive effects[1].

BMS-248360

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Catalog No. T14672Cas No. 254737-87-6

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	Inquiry	3-6 months	3-6 months
50 mg	Inquiry	3-6 months	3-6 months
100 mg	Inquiry	3-6 months	3-6 months

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Product Introduction

Bioactivity

Description	BMS-248360 is a potent, orally active dual antagonist of both angiotensin II receptor (AT1) and endothelin A (ETA) receptor, with Kis of 10 nM and 1.9 nM for hAT1 and hETA receptors, respectively. BMS-248360 demonstrates hypertensive effects[1].
Targets&IC50	ETA receptor (rat):1.9 nM, AT1 (rat):6.0 nM(ki), AT1 (human):（ki）10 nM, ETA receptor (human):1.9 nM(ki)
In vitro	BMS-248360 shows no activity against AT2 and ETB receptor subtypes and it also shows activity against rat AT1 and rat ETA receptor, with Kis of 6.0 nM and 1.9 nM, respectively[1].
In vivo	BMS-248360 is orally bioavailable in rats (%F=38) with excellent oral exposure (Cmax=3.1 μM) and a reasonable elimination profile (T1/2=5.5 hours)[1]. At dosages of 30 and 100 μmol/kg (p.o.), it effectively blocks the hypertensive effects of intravenously administered AII[1].

Chemical Properties

Molecular Weight	659.84
Formula	C₃₆H₄₅N₅O₅S
Cas No.	254737-87-6
Smiles	O=C1C2(N=C(CCCC)N1CC3=CC(CN4C(=O)C(C)(C)CC4)=C(C=C3)C5=C(S(NC6=C(C)C(C)=NO6)(=O)=O)C=CC=C5)CCCC2
Relative Density.	no data available

Storage & Solubility Information

Storage

Powder: -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:

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 DMSO TargetMol | 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 DMSO TargetMol | reagent stock solution to 400 μL PEG300 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 ddH₂O TargetMol | 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.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

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