| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
SNT-207707 targets the melanocortin-4 receptor (MC4R), a G protein-coupled receptor (GPCR) that plays a central role in the central regulation of energy homeostasis, food intake, and body weight. It acts as an antagonist, blocking MC-4R signaling and reducing central energy-expenditure regulation. It has an IC50 of 8 nM for binding and 5 nM for function on the MC-4 receptor.
|
|---|---|
| ln Vitro |
SNT-207707 is more than 200 times more selective than MC-3 and MC-5, and it binds to the MC-4 receptor with an affinity of 8 nM. Compared to MC-3 and MC-5, SNT207858 is a 22 nM MC-4 antagonist that exhibits 170 times more selectivity [1].
In vitro, SNT-207707 demonstrates high potency as an MC4R antagonist, with an IC50 of 8 nM in binding assays and 5 nM in functional assays. It is used in pharmacological studies to characterize the MC4R pathway and to evaluate potential therapeutic agents for metabolic disorders. The compound is soluble in DMSO at ≥250 mg/mL. |
| ln Vivo |
Mice's food intake was markedly increased by a single subcutaneous injection of SNT-207707 (20 mg/kg). The day following tumor implantation, compounds SNT207858 and SNT-207707 were given orally once a day, which significantly reduced tumor-induced weight loss [1].
In vivo, SNT-207707 is orally active and has been shown to increase food intake in mice when administered at a dose of 20 mg/kg. This effect is consistent with its mechanism as an MC4R antagonist, as blocking this receptor is known to stimulate appetite. It is used in research on metabolism and cachexia, a condition characterized by weight loss and muscle wasting. |
| Enzyme Assay |
In vitro receptor binding assays for SNT-207707 are performed to measure its affinity for the melanocortin-4 receptor (MC4R). These assays typically involve competitive displacement of a radiolabeled or fluorescently labeled ligand from the receptor, using membranes from cells expressing human MC4R. The compound's binding affinity is expressed as an IC50 value, which for SNT-207707 is 8 nM.
|
| Cell Assay |
In vitro cellular functional assays for SNT-207707 are used to measure its antagonist activity at MC4R. These assays typically use cell lines that express the receptor and a reporter system, such as cAMP accumulation, which is inhibited upon receptor activation. The compound's ability to block agonist-induced signaling is measured, yielding a functional IC50 of 5 nM.
|
| Animal Protocol |
In vivo animal experiments with SNT-207707 are conducted in mice to study its effects on food intake and metabolism. In a typical protocol, mice are administered the compound orally at a dose of 20 mg/kg, and their food consumption is monitored. These studies are crucial for understanding the role of MC4R in appetite regulation and for evaluating the compound's potential in treating cachexia.
|
| ADME/Pharmacokinetics |
The pharmacokinetic properties of SNT-207707 are consistent with an orally active, small-molecule drug. It has a molecular weight of 550.18 g/mol and a molecular formula of C32H44ClN5O. The compound is typically stored at 4degC, sealed, and away from moisture. It is soluble in DMSO, and protocols for its formulation for in vivo administration are available.
|
| Toxicity/Toxicokinetics |
The toxicological profile of SNT-207707 is not fully detailed in the provided literature. As a research compound, its safety and toxicity are primarily evaluated in preclinical studies. The compound is for research use only and is not for therapeutic or human use. Its effects on food intake and metabolism are the primary focus of its study.
|
| References | |
| Additional Infomation |
SNT-207707 is a potent and selective MC4R antagonist, a tool compound for studying the melanocortin pathway. Its primary application is in metabolic research, particularly for investigating appetite regulation and cachexia. It is available as a hydrochloride salt and is not an FDA-approved drug, being intended for research purposes only.
|
| Molecular Formula |
C32H43N5O.HCL
|
|---|---|
| Molecular Weight |
550.17766
|
| Exact Mass |
549.323
|
| CAS # |
1064662-40-3
|
| PubChem CID |
131843715
|
| Appearance |
White to off-white solid powder
|
| LogP |
7.175
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
12
|
| Heavy Atom Count |
39
|
| Complexity |
764
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC(C)CCN(CCC(C)C)C(=O)C1=CN2C(=NC(=C2CCCN3CCCC3)C4=CC=C(C=C4)C#N)C=C1.Cl
|
| InChi Key |
FBNJDWPWZNPVSC-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C32H43N5O.ClH/c1-24(2)15-20-36(21-16-25(3)4)32(38)28-13-14-30-34-31(27-11-9-26(22-33)10-12-27)29(37(30)23-28)8-7-19-35-17-5-6-18-35;/h9-14,23-25H,5-8,15-21H2,1-4H3;1H
|
| Chemical Name |
2-(4-cyanophenyl)-N,N-bis(3-methylbutyl)-3-(3-pyrrolidin-1-ylpropyl)imidazo[1,2-a]pyridine-6-carboxamide;hydrochloride
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ≥ 250 mg/mL (~454.40 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.78 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 20.8 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: ≥ 2.08 mg/mL (3.78 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 20.8 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.78 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8176 mL | 9.0879 mL | 18.1759 mL | |
| 5 mM | 0.3635 mL | 1.8176 mL | 3.6352 mL | |
| 10 mM | 0.1818 mL | 0.9088 mL | 1.8176 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
