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BMS-986278

Name: BMS-986278
Brand: TargetMol
SKU: T39647
Price: 64 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T39647Cas No. 2170126-74-4

BMS-986278 is an orally active and potent hemophosphatidic acid receptor 1 (LPA1) antagonist with Kb values of 6.9 nM and 4.0 nM for human and mouse LPA1, respectively.BMS-986278 may be investigated for use in idiopathic pulmonary fibrosis.

BMS-986278

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Purity: 99.88%

Catalog No. T39647Cas No. 2170126-74-4

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$64	In Stock	In Stock
5 mg	$156	In Stock	In Stock
10 mg	$218	In Stock	In Stock
25 mg	$396	In Stock	In Stock
50 mg	$538	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$169	In Stock	In Stock

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

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.88%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	BMS-986278 is an orally active and potent hemophosphatidic acid receptor 1 (LPA1) antagonist with Kb values of 6.9 nM and 4.0 nM for human and mouse LPA1, respectively.BMS-986278 may be investigated for use in idiopathic pulmonary fibrosis.
In vitro	With Kbs of 6.9 nM and 4.0 nM for human and mouse LPA1, respectively, BMS-986278 is a high-affinity LPA1 antagonist. These values were determined in CHO cells overexpressing LPA1[1]. BMS-986278 also antagonizes Lysophosphatidic acid (LPA)-stimulated calcium flux in normal human lung fibroblasts, exhibiting a Kb of 5.8 nM[1].
In vivo	In CD1 mice, a single oral administration of BMS-986278 (0.1-10 mg/kg) completely inhibits LPA-stimulated systemic histamine release in a concentration-dependent manner[1]. Furthermore, when administered orally twice daily for 14 days at doses ranging from 3 to 30 mg/kg, BMS-986278 reduces Bleomycin-induced collagen deposition and lung fibrosis in rats[1].

Chemical Properties

Molecular Weight	445.51
Formula	C₂₂H₃₁N₅O₅
Cas No.	2170126-74-4
Smiles	CCCN(C)C(=O)OCc1c(nnn1C)-c1ccc(O[C@H]2CCC[C@@H](C2)C(O)=O)c(C)n1

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.

Solubility Information

DMSO: 150 mg/mL (336.69 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (7.41 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2446 mL	11.2231 mL	22.4462 mL	112.2309 mL
5 mM	0.4489 mL	2.2446 mL	4.4892 mL	22.4462 mL
10 mM	0.2245 mL	1.1223 mL	2.2446 mL	11.2231 mL
20 mM	0.1122 mL	0.5612 mL	1.1223 mL	5.6115 mL
50 mM	0.0449 mL	0.2245 mL	0.4489 mL	2.2446 mL
100 mM	0.0224 mL	0.1122 mL	0.2245 mL	1.1223 mL

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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