| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
ATC0175 targets the melanin-concentrating hormone 1 receptor (MCH1R). It is a potent and selective antagonist. It has an IC50 of 13.5 nM for MCH1R and greater than 10,000 nM for MCH2R, demonstrating high selectivity. It also shows good selectivity over Y5 and α2A receptors.
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|---|---|
| ln Vitro |
ATC0175 demonstrates affinity for 5-HT2B and 5-HT1A, with corresponding IC50 values of 9.66 and 16.9 nM[1].
In vitro, ATC0175 is a potent and selective MCH1R antagonist with an IC50 of 13.5 nM. It has an IC50 of 3.4 nM in some assays. It binds to MCH1R and inhibits MCH-induced signaling. It is used in research on depression, anxiety, and obesity. |
| ln Vivo |
The antidepressant-like effect of ATC0175 (1, 3, 10 mg/kg; po) is demonstrated by its considerable and dose-dependent reduction in immobility time[1].
In vivo, ATC0175 demonstrates antidepressant and anxiolytic effects in animal models. It is an orally active compound. It is used in research on depression, anxiety disorders, and obesity. It provides strong experimental relevance for depression and anxiety disorder research. |
| Enzyme Assay |
Cell-free MCH1R binding assays for ATC0175 use membrane preparations from cells expressing human MCH1R. Radioligand binding is performed with a labeled MCHR1 ligand (e.g., [125I]MCH). ATC0175 is tested at concentrations ranging from 0.01 nM to 10 µM. Non-specific binding is determined using an excess of unlabeled MCH. IC50 and Ki values are calculated from competition curves.
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| Cell Assay |
In vitro cellular assays for ATC0175 use cells expressing MCH1R (e.g., HEK293 cells transfected with MCH1R). Cells are treated with ATC0175 at concentrations of 0.1-1000 nM for 1-24 hours. Receptor antagonism is assessed by measuring the inhibition of MCH-stimulated intracellular calcium increase using fluorescent calcium indicators. Functional assays such as inhibition of MCH-induced cAMP accumulation are also performed.
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| Animal Protocol |
In vivo animal experiments for ATC0175 use rodent models of depression and anxiety (e.g., forced swim test, tail suspension test, elevated plus maze, light-dark box). ATC0175 is administered orally at doses of 0.1-10 mg/kg. Endpoints include depression- and anxiety-related behaviors, locomotor activity, and MCH1R occupancy in brain tissues measured by ex vivo binding assays.
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| References |
| Molecular Formula |
C23H25F2N5O
|
|---|---|
| Molecular Weight |
425.4838
|
| Exact Mass |
425.202
|
| CAS # |
509118-03-0
|
| PubChem CID |
9934033
|
| Appearance |
White to light yellow solid powder
|
| Density |
1.30±0.1 g/cm3(Predicted)
|
| LogP |
4.8
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
31
|
| Complexity |
601
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CN(C1=NC(N[C@H]2CC[C@H](CC2)NC(C3=CC(F)=C(C=C3)F)=O)=NC4=C1C=CC=C4)C
|
| InChi Key |
FAIMGWSOSCFGRU-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C23H25F2N5O/c1-30(2)21-17-5-3-4-6-20(17)28-23(29-21)27-16-10-8-15(9-11-16)26-22(31)14-7-12-18(24)19(25)13-14/h3-7,12-13,15-16H,8-11H2,1-2H3,(H,26,31)(H,27,28,29)
|
| Chemical Name |
N-[4-[[4-(dimethylamino)quinazolin-2-yl]amino]cyclohexyl]-3,4-difluorobenzamide
|
| 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) |
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 | 2.3503 mL | 11.7514 mL | 23.5029 mL | |
| 5 mM | 0.4701 mL | 2.3503 mL | 4.7006 mL | |
| 10 mM | 0.2350 mL | 1.1751 mL | 2.3503 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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