2. GPCR/G Protein Neuronal Signaling
  3. Neuropeptide Y Receptor
  4. BMS-193885

BMS-193885 is a selective neuropeptide Y1 receptor antagonist (Ki=3.3 nM) that competitively blocks the receptor to inhibit NPY-mediated appetite regulation signaling pathways, reduce food intake and inhibit weight gain. BMS-193885 has good blood-brain barrier penetration and is mainly used in the study of obesity and related metabolic diseases.

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BMS-193885 Chemical Structure

BMS-193885 Chemical Structure

CAS No. : 186185-03-5

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Other Forms of BMS-193885:

BMS-193885 Related Antibodies

Top Publications Citing Use of Products

View All Neuropeptide Y Receptor Isoform Specific Products:

View All Isoforms
NPY Y1 receptor NPY Y2 receptor NPY Y4 receptor NPY Y5 receptor

  • Biological Activity

  • Purity & Documentation

  • References

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Description

BMS-193885 is a selective neuropeptide Y1 receptor antagonist (Ki=3.3 nM) that competitively blocks the receptor to inhibit NPY-mediated appetite regulation signaling pathways, reduce food intake and inhibit weight gain. BMS-193885 has good blood-brain barrier penetration and is mainly used in the study of obesity and related metabolic diseases[1][2][3].

IC50 & Target[1]

NPY Y1 receptor

 

NPY Y1 receptor

3.3 nM (Ki)

Cellular Effect
Cell Line Type Value Description References
SK-N-MC IC50
4.2 nM
Compound: 2f (dihydropyridine analogs)
Binding affinity against Neuropeptide Y receptor type 1 using I-PYY as a radioligand in human neuroblastoma SK-N-MC cells
Binding affinity against Neuropeptide Y receptor type 1 using I-PYY as a radioligand in human neuroblastoma SK-N-MC cells
[PMID: 11814791]
In Vitro

Binding assay: BMS-193885 competitively inhibits the binding of [125I]Peptide YY to human Y1 receptor in SK-N-MC cell membranes with a Ki value of 3.3 nM for Y1 receptor[1].
Functional cAMP assay: BMS-193885 (30-3000 nM; 30 min) reverses NPY-induced inhibition of Forskolin (HY-15371)-stimulated cAMP production in CHO cells expressing human Y1 receptor as a competitive antagonist with an apparent Kb of 4.5 nM[1].
Selectivity analysis: BMS-193885 (10 nM; 1 h) has no significant affinity for other NPY receptors Y2, Y4, and Y5, and is 200-fold less selective for the α1-adrenergic receptor[1].

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

BMS-193885 Related Antibodies
In Vivo

Acute feeding suppression: BMS-193885 (30-50 μg/5 μL; i.c.v.; single dose) blocks NPY (5 μg, 10 μg)-induced feeding in satious Sprague-Dawley rats[1].
Peripheral feeding suppression: BMS-193885 (10 mg/kg; i.p.; single dose) reduces NPY-induced 1-hour food intake and spontaneous nocturnal food intake in male Sprague-Dawley rats[1][2].
Chronic weight loss: BMS-193885 (10 mg/kg; i.p.; once daily for 44 days) reduces cumulative food intake and weight gain in male Sprague-Dawley rats without tolerance[1].
Cardiovascular safety: BMS-193885 (30 mg/kg; i.v.; single dose) had no serious adverse effects on heart rate and blood pressure in conscious rats and anesthetized dogs[1].
BMS-193885 (5 mg/kg; i.p.; single dose) significantly blocked NPY Y1 receptors in Wistar rats and reduced the effects of NPY injection on cardiopulmonary function[3].

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

Animal Model: Male Sprague-Dawley rats (220-280 g), satiated, with i.c.v. cannula implantation[1]
Dosage: 30-50 μg (10% DMSO in sterile Ringer)
Administration: i.c.v. injection (5 μL), single dose
Result: Significantly reduced NPY-induced 1-h food intake by 57% (30 μg) and 63% (50 μg) compared to vehicle controls. No effect was observed on basal food intake1.
Animal Model: Male Sprague-Dawley rats (220-280 g), satiated[1]
Dosage: 10 mg/kg (40% PEG 400 + 60% saline)
Administration: i.p. injection, single dose 30 min before dark cycle
Result: Reduced NPY-induced 1-h food intake by 33-57% and spontaneous overnight food intake by 29-54% compared to vehicle.
Animal Model: Male Sprague-Dawley rats (220-280 g), naive[1]
Dosage: 10 mg/kg BMS-193885 (40% PEG 400 + 60% saline)
Administration: i.p. injection daily for 44 days, 2 h before dark cycle
Result: Reduced cumulative food intake by 12-15% and suppressed body weight gain by 8.5% compared to vehicle. No tolerance developed, but adhesive peritonitis occurred in some animals.
Animal Model: Conscious male Sprague-Dawley rats (220-280 g); anesthetized dogs[1]
Dosage: 30 mg/kg (rats), 10 mg/kg (dogs) (in sterile saline)
Administration: i.v. injection, single dose
Result: No significant changes in heart rate or blood pressure were observed in rats or dogs. Oral bioavailability was <0.1% due to poor absorption[1]1.
Molecular Weight

590.71

Formula

C33H42N4O6
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C(C1=C(C)NC(C)=C(C(OC)=O)C1C2=CC=CC(NC(NCCCN3CCC(C4=CC=CC(OC)=C4)CC3)=O)=C2)OC
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 (169.29 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 1.6929 mL 8.4644 mL 16.9288 mL
5 mM 0.3386 mL 1.6929 mL 3.3858 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
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Volume
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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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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.23 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (4.23 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(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

Purity: 99.08%

SDS (392 KB)

COA (246 KB) HNMR (243 KB) LCMS (238 KB)

Handling Instructions (2659 KB)
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 1.6929 mL 8.4644 mL 16.9288 mL 42.3219 mL
5 mM 0.3386 mL 1.6929 mL 3.3858 mL 8.4644 mL
10 mM 0.1693 mL 0.8464 mL 1.6929 mL 4.2322 mL
15 mM 0.1129 mL 0.5643 mL 1.1286 mL 2.8215 mL
20 mM 0.0846 mL 0.4232 mL 0.8464 mL 2.1161 mL
25 mM 0.0677 mL 0.3386 mL 0.6772 mL 1.6929 mL
30 mM 0.0564 mL 0.2821 mL 0.5643 mL 1.4107 mL
40 mM 0.0423 mL 0.2116 mL 0.4232 mL 1.0580 mL
50 mM 0.0339 mL 0.1693 mL 0.3386 mL 0.8464 mL
60 mM 0.0282 mL 0.1411 mL 0.2821 mL 0.7054 mL
80 mM 0.0212 mL 0.1058 mL 0.2116 mL 0.5290 mL
100 mM 0.0169 mL 0.0846 mL 0.1693 mL 0.4232 mL
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BMS-193885 Related Classifications

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  • 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-193885186185-03-5BMS193885BMS 193885Neuropeptide Y ReceptorNPY receptorInhibitorinhibitorinhibit

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