| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| Other Sizes |
| Targets |
TC-MCH 7c primarily targets the melanin-concentrating hormone receptor 1 (MCH1R), a G protein-coupled receptor involved in the regulation of feeding behavior, energy homeostasis, mood, and sleep. It acts as a potent antagonist with an IC50 of 5.6 nM against human MCH1R and Ki values of 3.4 nM (human) and 3.0 nM (mouse). By blocking MCH1R, TC-MCH 7c modulates MCH-mediated signaling. Its ability to penetrate the blood-brain barrier makes it suitable for central nervous system studies.
|
|---|---|
| ln Vitro |
In [Ca2+]i mobilization, TC-MCH 7c has an IC50 of 9.7 μM against MCH1R [1]. TC-MCH 7c's IC50 values for hERG and FLIPR are 9.0 μM and 23 nM, respectively[2].
In vitro, TC-MCH 7c functions as a potent MCH1R antagonist with an IC50 of 5.6 nM in hMCH1R-expressing CHO cells. It has Ki values of 3.4 nM (human) and 3.0 nM (mouse). The compound has an IC50 of 23 nM for FLIPR (a calcium flux assay) and 9.0 μM for hERG (cardiac safety). Its activity is typically evaluated using receptor binding and functional assays in cells expressing MCH1R. The compound's selectivity for MCH1R over other receptors is assessed. |
| ln Vivo |
TC-MCH 7c (oral; 3-30 mg/kg; once daily for 1.5 months) displayed excellent body weight reduction in a dose-dependent manner in a DIO mice model [1]. The plasma concentrations of TC-MCH 7c (oral; 3-30 mg/kg) 30 mg/kg were 5.1, 1.8, and 0.7 μM at 2, 15, and 24 hours, respectively [2].
In vivo, TC-MCH 7c is orally active and brain-penetrant. It has been studied for its effects on feeding behavior and energy homeostasis in mouse models. The compound is administered orally at doses ranging from 3-30 mg/kg once daily. Its ability to cross the blood-brain barrier allows for direct assessment of MCH1R antagonism in the central nervous system. However, specific in vivo efficacy data are not extensively detailed in the available literature. Further studies are needed to fully characterize its in vivo pharmacological profile. |
| Enzyme Assay |
Cell-free assays for TC-MCH 7c involve evaluating its binding affinity to MCH1R. Radioligand binding assays are performed using membrane preparations from cells expressing human or mouse MCH1R. TC-MCH 7c is incubated with membranes and a radiolabeled MCH1R ligand. Competition binding experiments determine Ki values (3.4 nM human, 3.0 nM mouse). Selectivity is assessed by testing against other receptors. hERG binding assays are performed to assess cardiac safety potential (IC50 = 9.0 μM).
|
| Cell Assay |
In vitro cellular assays for TC-MCH 7c typically involve treating CHO cells expressing human MCH1R with various concentrations of the compound. Functional assays such as FLIPR (calcium flux) are used to measure receptor activity. IC50 values (5.6 nM for hMCH1R, 23 nM for FLIPR) are determined from dose-response curves. The compound's ability to block MCH1R-mediated signaling is assessed. Cytotoxicity is evaluated using standard cell viability assays. The compound is typically dissolved in DMSO and diluted in cell culture medium.
|
| Animal Protocol |
Animal/Disease Models: Diet-induced obese mice [2]
Doses: 3, 10 and 30 mg/kg (pharmacokinetic/PK/PK analysis) Route of Administration: Oral Experimental Results: Plasma concentrations at 2, 15 and 24 hrs (hrs (hours)) were 5.1, 1.8 and 24 hrs (hrs (hours)), respectively. 0.7 μM. In vivo animal studies for TC-MCH 7c are conducted in mouse models of obesity and metabolic disorders. The compound is administered orally at doses of 3-30 mg/kg once daily. Feeding behavior, body weight, and metabolic parameters are monitored. Brain penetration is confirmed by measuring drug concentrations in brain tissue using LC-MS/MS. Pharmacodynamic endpoints include assessment of MCH1R occupancy in brain regions using radioligand binding techniques. Efficacy is evaluated by comparing outcomes between treatment and control groups. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of TC-MCH 7c include a molecular weight of 408.45 g/mol (approximate) and molecular formula C23H22ClN3O2 (approximate). The compound is orally active and brain-penetrant. It is soluble in 1eq. HCl (40.85 mg/mL). The compound is typically stored at appropriate conditions as a research reagent. Detailed ADME parameters such as half-life, Cmax, and AUC are not extensively reported in the available literature.
|
| Toxicity/Toxicokinetics |
The toxicity profile of TC-MCH 7c includes hERG activity (IC50 = 9.0 μM), indicating potential cardiac safety concerns at high concentrations. Standard toxicology studies would include acute and sub-chronic toxicity assessments in rodent models, with particular attention to cardiovascular effects. The compound is intended for research use only and not for therapeutic applications in humans. Standard safety precautions should be followed when handling this compound.
|
| References |
|
| Additional Infomation |
TC-MCH 7c is an orally active, selective, and brain-penetrant MCH1R antagonist with an IC50 of 5.6 nM against human MCH1R and Ki values of 3.4 nM (human) and 3.0 nM (mouse). It is a phenylpyridone derivative with hERG IC50 of 9.0 μM. TC-MCH 7c is a research tool for studying MCH1R function in feeding behavior and energy homeostasis. It has not entered clinical trials and is strictly for research purposes.
|
| Molecular Formula |
C24H25FN2O3
|
|---|---|
| Molecular Weight |
408.465309858322
|
| Exact Mass |
408.185
|
| CAS # |
864756-35-4
|
| PubChem CID |
11654412
|
| Appearance |
Light yellow to yellow solid powder
|
| LogP |
3.968
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
30
|
| Complexity |
616
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1CCN(C1)CCOC2=CC=C(C=C2)N3C=CC(=CC3=O)OCC4=CC=C(C=C4)F
|
| InChi Key |
ANCFKYJMXNMYNZ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C24H25FN2O3/c25-20-5-3-19(4-6-20)18-30-23-11-14-27(24(28)17-23)21-7-9-22(10-8-21)29-16-15-26-12-1-2-13-26/h3-11,14,17H,1-2,12-13,15-16,18H2
|
| Chemical Name |
4-[(4-fluorophenyl)methoxy]-1-[4-(2-pyrrolidin-1-ylethoxy)phenyl]pyridin-2-one
|
| 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 |
| 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) |
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
|
|---|---|
| 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 | 2.4482 mL | 12.2408 mL | 24.4816 mL | |
| 5 mM | 0.4896 mL | 2.4482 mL | 4.8963 mL | |
| 10 mM | 0.2448 mL | 1.2241 mL | 2.4482 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
