| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 1g | |||
| Other Sizes |
| Targets |
BMS-193885 targets the neuropeptide Y1 receptor. It is a potent and selective antagonist with a Ki of 3.3 nM. It competitively inhibits neuropeptide Y binding. It displays > 47, > 100, > 160, > 160 and > 160-fold selectivity over σ1, α1, Y2, Y4 and Y5 receptors respectively. By blocking Y1 receptors, it modulates neuropeptide Y signaling.
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| ln Vitro |
In vitro, BMS-193885 is a potent and selective neuropeptide Y1 receptor antagonist with a Ki of 3.3 nM. It competitively acts on the neuropeptide Y binding site. Its activity is typically assessed in receptor binding studies and functional assays measuring the inhibition of neuropeptide Y-induced signaling. It displays high selectivity for Y1 over other receptors.
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| ln Vivo |
In vivo, BMS-193885 is a brain-penetrant compound. It can reduce food intake and body weight through central Y1 inhibition. As a neuropeptide Y1 receptor antagonist, it modulates neuropeptide Y-mediated effects on feeding behavior and energy homeostasis. However, comprehensive in vivo efficacy data from published literature are limited.
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| Enzyme Assay |
For non-cell-based receptor binding assays, BMS-193885 can be evaluated using membrane preparations from cells expressing human neuropeptide Y1 receptors. Radioligand binding displacement experiments are performed using a suitable radiolabeled ligand such as [125I]-Peptide YY. Membrane homogenates are incubated with increasing concentrations of the test compound and a fixed concentration of the radioligand. Bound radioligand is separated from free by rapid filtration through glass fiber filters. Non-specific binding is determined in the presence of excess unlabeled Peptide YY. Ki values are calculated from displacement curves using nonlinear regression analysis.
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| Cell Assay |
For in vitro cellular assays, cells expressing human neuropeptide Y1 receptors are cultured in appropriate media. For functional assays, the inhibition of forskolin-stimulated cAMP accumulation is measured. Cells are treated with various concentrations of BMS-193885 in the presence of a Y1 receptor agonist such as neuropeptide Y. cAMP levels are measured using ELISA or HTRF-based detection. The compound's ability to reverse the agonist-induced inhibition of cAMP accumulation is assessed, and IC50 values are calculated from dose-response curves.
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| Animal Protocol |
For in vivo animal studies, BMS-193885 can be administered to rodents via oral gavage or intraperitoneal injection. In models of feeding behavior, food intake and body weight are monitored following compound administration. In models of obesity, its effects on energy homeostasis are assessed. Dosing regimens vary depending on the specific model and desired exposure levels.
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| ADME/Pharmacokinetics |
BMS-193885 L-Lactic acid has a molecular formula of C30H35F7N4O2 and a molecular weight of 616.61. It is a brain-penetrant compound. It should be stored according to the manufacturer's recommendations. It is for research use only and is not intended for human consumption.
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| Toxicity/Toxicokinetics |
The toxicity profile of BMS-193885 has not been extensively reported. As a neuropeptide Y1 receptor antagonist, potential adverse effects may include modulation of feeding behavior and energy homeostasis. The compound is for research use only and is not intended for human consumption. Standard safety precautions should be observed when handling the compound.
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| References | |
| Additional Infomation |
BMS-193885 L-Lactic acid (CAS 679839-66-8) is a potent, selective, and brain-penetrant neuropeptide Y1 receptor antagonist. It has a Ki of 3.3 nM for the neuropeptide Y1 receptor and displays high selectivity over other receptors. It can reduce food intake and body weight through central Y1 inhibition. It is available for research purposes only.
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| Molecular Formula |
C36H48N4O9
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|---|---|
| Molecular Weight |
680.79
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| Exact Mass |
680.342
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| CAS # |
679839-66-8
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| Related CAS # |
BMS-193885;186185-03-5
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| PubChem CID |
56972234
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
49
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| Complexity |
1070
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| Defined Atom Stereocenter Count |
1
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| SMILES |
O(C)C1=CC=CC(=C1)C1CCN(CCCNC(NC2=CC=CC(=C2)C2C(C(=O)OC)=C(C)NC(C)=C2C(=O)OC)=O)CC1.O[C@H](C(=O)O)C
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| InChi Key |
BYHJIPSVXAFCDI-WNQIDUERSA-N
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| InChi Code |
InChI=1S/C33H42N4O6.C3H6O3/c1-21-28(31(38)42-4)30(29(22(2)35-21)32(39)43-5)25-10-6-11-26(19-25)36-33(40)34-15-8-16-37-17-13-23(14-18-37)24-9-7-12-27(20-24)41-3;1-2(4)3(5)6/h6-7,9-12,19-20,23,30,35H,8,13-18H2,1-5H3,(H2,34,36,40);2,4H,1H3,(H,5,6)/t;2-/m.0/s1
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| Chemical Name |
dimethyl 4-[3-[3-[4-(3-methoxyphenyl)piperidin-1-yl]propylcarbamoylamino]phenyl]-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate;(2S)-2-hydroxypropanoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4689 mL | 7.3444 mL | 14.6888 mL | |
| 5 mM | 0.2938 mL | 1.4689 mL | 2.9378 mL | |
| 10 mM | 0.1469 mL | 0.7344 mL | 1.4689 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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