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| Targets |
ATC-0175 targets the melanin-concentrating hormone receptor 1 (MCH1 or MCHR1). It also displays affinity for serotonin receptors 5-HT2B and 5-HT1A. The compound is a potent antagonist at MCH1 with an IC50 of 13.5 nM and shows no significant activity at MCH2 (IC50 > 10,000 nM). It also exhibits affinity for 5-HT2B and 5-HT1A receptors.
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| ln Vitro |
ATC0175 exhibits affinity for 5-HT2B and 5-HT1A, with an IC50 of 9.66 and 16.9 nM, respectively[1].
In vitro, ATC-0175 is a potent antagonist at the MCH1 receptor. Receptor binding and functional assays indicate that ATC-0175 is a noncompetitive antagonist at MCH1 receptors. It displays an IC50 of 13.5 nM for MCH1 and >10,000 nM for MCH2. The compound also has IC50 values of 9.66 nM and 16.9 nM for 5-HT2B and 5-HT1A receptors, respectively. |
| ln Vivo |
The antidepressant-like potential of ATC0175 (1, 3, 10 mg/kg; oral) is suggested by its considerable and dose-dependent reduction in immobility time [1].
In vivo, ATC-0175 exhibits anxiolytic and antidepressant activity in rodents. It is an orally active compound. Studies have shown it to have a prodepressive effect when microinjected into the dorsal raphe, and this effect can be reversed by nortriptyline. The compound's oral activity makes it a valuable tool for in vivo studies of the MCH system. |
| Enzyme Assay |
In vitro receptor binding assays for ATC-0175 typically involve competitive binding studies using membranes from cells expressing MCH1, 5-HT2B, or 5-HT1A receptors. Radiolabeled ligands specific to each receptor are used, and the compound is tested at various concentrations to determine its affinity (IC50 or Ki values). Functional assays, such as measuring MCH-induced increase in intracellular calcium [Ca2+]i, are used to confirm antagonist activity.
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| Cell Assay |
In vitro cellular assays for ATC-0175 are used to confirm its antagonist activity at MCH1 receptors. Cells expressing the MCH1 receptor are loaded with a calcium-sensitive dye (e.g., Fluo-4). The cells are pre-incubated with the compound and then stimulated with MCH. The inhibition of the MCH-induced calcium flux is measured using a fluorescence plate reader to determine the compound's potency.
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| Animal Protocol |
In vivo animal studies with ATC-0175 are typically conducted in rodent models to assess its anxiolytic and antidepressant-like effects. The compound is administered orally, and behavioral tests such as the elevated plus maze, forced swim test, or tail suspension test are used to evaluate its activity. Microinjection studies into specific brain regions like the dorsal raphe are also performed to investigate its mechanism of action.
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| ADME/Pharmacokinetics |
ATC-0175 is orally active, indicating good oral bioavailability. It has a molecular weight of 461.94. The compound is typically stored at +4°C. Specific pharmacokinetic parameters such as half-life, volume of distribution, and clearance are not detailed in the available literature.
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| Toxicity/Toxicokinetics |
The toxicity profile of ATC-0175 is not extensively reported in the available literature. As a research compound, it is for research use only and not for human therapeutic use. Standard toxicity studies would be required for its development as a therapeutic agent. No specific toxicity data are detailed in the provided sources.
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| References | |
| Additional Infomation |
ATC-0175 (hydrochloride) is a potent, selective, and orally active MCH1 antagonist with anxiolytic and antidepressant-like effects in rodents. It is a valuable pharmacological tool for studying the role of the MCH system in stress, emotion, anxiety, and depression. The compound is not approved for clinical use and is available for research purposes only.
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| Molecular Formula |
C23H26CLF2N5O
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|---|---|
| Molecular Weight |
461.93500
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| Exact Mass |
461.179
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| Elemental Analysis |
C, 59.80; H, 5.67; Cl, 7.67; F, 8.23; N, 15.16; O, 3.46
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| CAS # |
510733-97-8
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| Related CAS # |
509118-03-0;510733-97-8 (HCl);
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| PubChem CID |
9934032
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| Appearance |
White to light yellow solid powder
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| LogP |
5.393
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
32
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| Complexity |
601
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.FC1=CC=C(C(NC2CCC(NC3=NC4=CC=CC=C4C(N(C)C)=N3)CC2)=O)C=C1F
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| Synonyms |
ATC0175; ATC-0175; ATC 0175; ATC0175 HCl; ATC0175 hydrochloride;
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| HS Tariff Code |
2934.99.03.00
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| 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)
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| Solubility (In Vitro) |
DMSO : ~12.5 mg/mL (~27.06 mM)
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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 | 2.1648 mL | 10.8239 mL | 21.6478 mL | |
| 5 mM | 0.4330 mL | 2.1648 mL | 4.3296 mL | |
| 10 mM | 0.2165 mL | 1.0824 mL | 2.1648 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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