Shopping Cart

Remove All

Your shopping cart is currently empty

Proceed to checkout Continue shopping

BMS-819881

Name: BMS-819881
Brand: TargetMol
SKU: T14678
Rating: 4.5 (1 reviews)

Copy Product Info

😃Good

Catalog No. T14678Cas No. 1197420-05-5

BMS-819881, a melanin-concentrating hormone receptor 1 (MCHR1) antagonist, binds rat MCHR1 with a Ki of 7 nM, and is selective and potent for CYP3A4 activity with an EC50 of 13 μM.

BMS-819881

Copy Product Info

😃Good

Catalog No. T14678Cas No. 1197420-05-5

BMS-819881, a melanin-concentrating hormone receptor 1 (MCHR1) antagonist, binds rat MCHR1 with a Ki of 7 nM, and is selective and potent for CYP3A4 activity with an EC50 of 13 μM.

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$1,520	6-8 weeks	6-8 weeks
50 mg	$1,980	6-8 weeks	6-8 weeks
100 mg	$2,500	6-8 weeks	6-8 weeks

Add to Cart

Add to Quotation

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.

Questions

Resource Download

Product Introduction

Bioactivity

Description	BMS-819881, a melanin-concentrating hormone receptor 1 (MCHR1) antagonist, binds rat MCHR1 with a Ki of 7 nM, and is selective and potent for CYP3A4 activity with an EC50 of 13 μM.
Targets&IC50	MCH1R (rat):7 nM （ki）, CYP3A4:13 μM （EC50）
In vitro	BMS-819881 (Compound 27) binds 99.8% to rat serum proteins with a rat MCHR1 Ki of 7 nM. In cytochrome P450 (CYP) assays, it shows EC50 values >40 μM for CYP1A2, CYP2C9, CYP2C19, and CYP2D6, but 13 μM for CYP3A4. Binding to serum proteins is species-dependent: 99.8% in rats, 99.6% in dogs, and 99.3% in monkeys. FLIPR-based assays indicate BMS-819881 is a potent and selective MCHR1 antagonist (Kb=32 nM) that blocks MCH-stimulated Ca2+ mobilization in MCHR1-overexpressing cells but not in MCHR2-expressing cells at 10 μM. No activity is observed at 10 μM against a panel of 20 GPCRs associated with feeding homeostasis [1].
In vivo	BMS-819881 exhibits a moderate terminal elimination half-life, with values recorded at 5.7 hours for rats, 32±8 hours for dogs, and 14±3 hours for cynomolgus monkeys, all administered at a dosage of 1 mg/kg intravenously[1].

Chemical Properties

Molecular Weight	468.95
Formula	C₂₄H₂₁ClN₂O₄S
Cas No.	1197420-05-5
Smiles	O=C1C2=C(C=C(S2)C3=CC=C(Cl)C=C3)N=CN1C4=CC(OC)=C(OC[C@H](O)C5CC5)C=C4
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.

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

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