| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Targets |
BMS-193885 targets the neuropeptide Y1 (NPY Y1) receptor, a G protein-coupled receptor that mediates the effects of neuropeptide Y (NPY). It acts as a potent, selective, competitive, and brain-penetrant antagonist. It has a Ki of 3.3 nM and an IC50 of 5.9 nM for hY1. It shows high selectivity over other NPY receptor subtypes and α1 receptors.
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| ln Vitro |
In vitro, BMS-193885 is a potent and selective NPY Y1 receptor antagonist. It has a Ki of 3.3 nM and an IC50 of 5.9 nM for hY1. It displays >100-fold selectivity over α1 receptors and >160-fold selectivity over hY2, hY4, and hY5 receptors. These activities confirm its profile as a highly selective NPY Y1 antagonist.
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| ln Vivo |
In vivo, BMS-193885 is a brain-penetrant compound. Its ability to cross the blood-brain barrier makes it useful for studying the role of NPY Y1 receptors in the central nervous system. However, specific details of in vivo efficacy studies are not extensively detailed in the available literature. It is a research compound and is not approved for clinical use.
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| Enzyme Assay |
The in vitro receptor binding assay for BMS-193885 typically involves radioligand displacement studies using membrane preparations from cells expressing the human NPY Y1 receptor. The compound's affinity (Ki) is determined by measuring its ability to displace a specific radiolabeled ligand. Its selectivity is assessed by testing against other NPY receptor subtypes and related receptors.
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| Cell Assay |
In vitro cellular assays for BMS-193885 assess its functional antagonism at the NPY Y1 receptor. Cells expressing the Y1 receptor are treated with BMS-193885, and its ability to inhibit NPY-induced signaling (e.g., calcium mobilization or cAMP inhibition) is measured. These assays demonstrate the compound's functional activity as a Y1 antagonist.
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| Animal Protocol |
In vivo animal studies for BMS-193885 are conducted to study the role of NPY Y1 receptors in various physiological and pathological processes, particularly in the brain. However, specific details of these studies are not extensively detailed in the available literature. It is a research compound and is not approved for clinical use.
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| ADME/Pharmacokinetics |
BMS-193885 is a brain-penetrant compound. Its ability to cross the blood-brain barrier is a key feature for studying central NPY Y1 receptors. However, detailed pharmacokinetic parameters such as half-life and bioavailability are not extensively detailed in the available literature. It is intended for research use only.
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| Toxicity/Toxicokinetics |
Specific toxicity data for BMS-193885 are not extensively detailed in the available literature. As a selective NPY Y1 receptor antagonist, its toxicity profile is likely related to its mechanism of action. However, its high selectivity may contribute to a favorable safety profile. It is intended for research purposes only.
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| References |
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| Additional Infomation |
BMS-193885 is a potent, selective, competitive, and brain-penetrant NPY Y1 receptor antagonist. It is a valuable research tool for studying the role of NPY Y1 receptors in appetite regulation, anxiety, and other neurological processes. It is not approved for clinical use and is intended for research purposes only.
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| Molecular Formula |
C33H42N4O6.C3H6O3
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|---|---|
| Molecular Weight |
680.78772
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| Exact Mass |
590.31
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| Elemental Analysis |
C, 67.10; H, 7.17; N, 9.48; O, 16.25
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| CAS # |
186185-03-5
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| Related CAS # |
BMS-193885 L-Lactic acid;679839-66-8
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| PubChem CID |
9960164
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| Appearance |
White to yellow solid powder
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| LogP |
5.211
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
43
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| Complexity |
1010
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C[C@H](C(=O)O)O.COC1=CC=CC(C2CCN(CCCNC(NC3=CC=CC(C4C(C(OC)=O)=C(C)NC(C)=C4C(OC)=O)=C3)=O)CC2)=C1
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| InChi Key |
WMYSXJSJXZFODY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C33H42N4O6/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/h6-7,9-12,19-20,23,30,35H,8,13-18H2,1-5H3,(H2,34,36,40)
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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
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| Synonyms |
BMS-193885; BMS 193885; BMS193885;
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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) |
DMSO : ~100 mg/mL (~169.29 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.23 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (4.23 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (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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