2. GPCR/G Protein Neuronal Signaling Metabolic Enzyme/Protease
  3. MCHR1 (GPR24) Cytochrome P450
  4. BMS-819881

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

For research use only. We do not sell to patients.

BMS-819881 Chemical Structure

BMS-819881 Chemical Structure

CAS No. : 1197420-05-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

BMS-819881 Related Antibodies

Top Publications Citing Use of Products

View All Cytochrome P450 Isoform Specific Products:

View All Isoforms
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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

IC50 & Target[1]

rat MCHR1

7 nM (Ki)

CYP3A4

13 μM (EC50)

In Vitro

BMS-819881 (Compound 27) is 99.8% binds to rat serum proteins and rat MCHR1 Ki is 7 nM. FLIPR-based assays establish that BMS-819881 is a potent and highly selective MCHR1 functional antagonist. BMS-819881 (Kb=32 nM) effectively blocks MCH stimulated Ca2+ mobilization in heterologous cells overexpressing MCHR1 but fails to inhibit MCH mediated Ca2+ mobilization of cells expressing MCHR2 at 10 μM. No activity is observed upon screening BMS-819881 at 10 μM versus a panel of 20 GPCRs associated with feeding homeostasis. The percent of BMS-819881 binds to serum proteins is species dependent ranging from 99.8%, 99.6%, and 99.3%, respectively, for rat, dog, and monkey. When BMS-819881 is screened for cytochrome P450 (CYP) activity, EC50 values for CYP1A2, CYP2C9, CYP2C19, CYP2D6 are >40 μM; however, the CYP3A4 EC50 is 13 μM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

BMS-819881 Related Antibodies
In Vivo

BMS-819881 has moderate terminal elimination half-life (t1/2=5.7 h, 32±8 h, and 14±3 h for rat (1 mg/kg, iv), dog (1 mg/kg, iv), and cynomologous monkey (1 mg/kg, iv))[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

468.95

Formula

C24H21ClN2O4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC=C(C2=CC(N=CN(C3=CC(OC)=C(OC[C@H](O)C4CC4)C=C3)C5=O)=C5S2)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (213.24 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1324 mL 10.6621 mL 21.3242 mL
5 mM 0.4265 mL 2.1324 mL 4.2648 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.33 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
Kinase Assay
[1]

Membranes from stably transfected HEK-293 cells expressing a mutated (E4Q, A5T) hMCHR1 receptor are prepared and differential centrifugation. Binding experiments are carried out with 0.5-1.0 μg of membrane protein incubated in a total of 0.2 mL in 25 mM HEPES (pH 7.4) with 10 mM MgCl2, 2 mM EGTA, and 0.1% BSA (binding buffer) for 90 min. For competition binding assays, reactions are carried out in the presence of 0.06–0.1 nM [Phe13, [125I]Tyr19]MCH and increasing concentrations of unlabeled test molecules. Reactions are terminated by rapid vacuum filtration over 96-well GFC Unifilter plates precoated with 0.075 mL of binding buffer containing 1% BSA and washed 3 times with 0.4 mL of PBS (pH 7.4) containing 0.01% TX-100. Filters are dried, 0.05 mL of MicroScint 20 is added to each well, and radioactivity is subsequently quantified by scintillation counting on a TopCount microplate scintillation counter. Inhibitory constants are determined by nonlinear least-squares analysis using a four-parameter logistic equation[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

Stable HEK-293 cells expressing human MCHR1 or MCHR2 receptor are plated at a density of 50 000 cells/well in 96-well polylysine coated plates and cultured overnight in DMEM (high glucose (4.5 g/mL), 25 mM HEPES, pH 7.4, 10% fetal bovine serum, 1 mM NaCl) at 37°C, 5% CO2 conditions. For assay, the medium is replaced with 90 mL per well dye solution consisting of 3.8 mM Fluo4 AM, 0.04% Pluronic F-127, and 2.5 mM Probencid in base buffer (Hank’s balanced salt solution, 25 mM HEPES, 0.1% BSA). Dye solution is allowed to “load” for 1 h at room temperature in subdued light. Dye is subsequently removed and replaced with 75 mL of base buffer and 75 mL of diluted test compound (e.g., BMS-819881; 10 μM) and incubated for an additional 15 min. Test compound dilution plates are prepared by serial diluting test and reference compounds from 100% DMSO stocks first 1:50 in base buffer and then serially (1:3.26) in base buffer containing 2% DMSO to generate 12 half log test concentrations[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Rats, Dogs, and Cynomologous monkeys [1]
PK studies using three species (rat, dog, and cynomologous monkey) are conducted with BMS-819881 administered iv at 1 mg/kg[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1324 mL 10.6621 mL 21.3242 mL 53.3106 mL
5 mM 0.4265 mL 2.1324 mL 4.2648 mL 10.6621 mL
10 mM 0.2132 mL 1.0662 mL 2.1324 mL 5.3311 mL
15 mM 0.1422 mL 0.7108 mL 1.4216 mL 3.5540 mL
20 mM 0.1066 mL 0.5331 mL 1.0662 mL 2.6655 mL
25 mM 0.0853 mL 0.4265 mL 0.8530 mL 2.1324 mL
30 mM 0.0711 mL 0.3554 mL 0.7108 mL 1.7770 mL
40 mM 0.0533 mL 0.2666 mL 0.5331 mL 1.3328 mL
50 mM 0.0426 mL 0.2132 mL 0.4265 mL 1.0662 mL
60 mM 0.0355 mL 0.1777 mL 0.3554 mL 0.8885 mL
80 mM 0.0267 mL 0.1333 mL 0.2666 mL 0.6664 mL
100 mM 0.0213 mL 0.1066 mL 0.2132 mL 0.5331 mL
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BMS-819881 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BMS-8198811197420-05-5BMS819881BMS 819881MCHR1 (GPR24)Cytochrome P450Melanin concentrating hormone receptor 1CYPsInhibitorinhibitorinhibit

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