| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| Targets |
ATC0175 primarily targets the melanin-concentrating hormone receptor 1 (MCHR1). It acts as a potent antagonist with an IC50 of 13 nM for MCH1R. In addition to MCHR1, ATC0175 demonstrates affinity for both 5-HT2B and 5-HT1A receptors, with IC50 values of 9.66 and 16.9 nM, respectively. These additional affinities may contribute to its overall pharmacological profile and antidepressant-like effects. The compound is a quinazoline derivative and belongs to the class of synthetic, non-peptidic small molecules.
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| ln Vitro |
ATC0175 demonstrates affinity for both 5-HT2B and 5-HT1A, with IC50 values of 9.66 and 16.9 nM, respectively[1].
In vitro, ATC0175 exhibits potent antagonist activity at MCHR1, with an IC50 of 13 nM. Receptor binding and functional assays, such as measuring MCH-induced increases in intracellular calcium [Ca2+], confirm its high affinity and potent antagonism at MCH1R. The compound also shows affinity for 5-HT2B (IC50 = 9.66 nM) and 5-HT1A (IC50 = 16.9 nM) receptors. These in vitro activities demonstrate its potent and selective profile at MCHR1 with additional serotonergic receptor interactions. |
| ln Vivo |
ATC0175 (1, 3, 10 mg/kg; oral) decreases immobility time considerably and in a dose-dependent manner, indicating potential antidepressant properties [1].
In vivo, ATC0175 has demonstrated anxiolytic- and antidepressant-like effects in rodent models. In the forced swimming test, ATC0175 significantly and dose-dependently reduced immobility time, indicating antidepressant-like activity. It increased swimming performance without altering climbing behavior, as observed with selective serotonin reuptake inhibitors. Microinjections of MCH into the dorsal raphe induce prodepressive effects, which are reversed by ATC0175. These findings support the potential of ATC0175 for the treatment of depression and anxiety disorders. |
| Enzyme Assay |
The in vitro receptor binding assay for ATC0175 typically involves radioligand displacement studies using membrane preparations from cells expressing the human MCHR1, 5-HT2B, or 5-HT1A receptors. The compound's affinity (IC50 or Ki) is determined by measuring its ability to displace a specific radiolabeled ligand from the receptor. Functional antagonist activity at MCHR1 is assessed by measuring the inhibition of MCH-induced increases in intracellular calcium [Ca2+] in cells expressing the receptor. These cell-free assays provide a direct measure of receptor binding and functional antagonism.
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| Cell Assay |
In vitro cellular assays for ATC0175 typically measure its ability to antagonize MCHR1-mediated signaling. Cells expressing the human MCHR1 are loaded with a calcium-sensitive fluorescent dye and stimulated with MCH, which induces an increase in intracellular calcium. The compound's ability to inhibit this calcium flux is measured, providing a functional measure of antagonist activity. These assays quantify the compound's potency as an MCHR1 antagonist in a relevant cellular context, complementing the receptor binding data.
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| Animal Protocol |
In vivo animal studies for ATC0175 have been conducted in rodent models to assess its antidepressant- and anxiolytic-like effects. The forced swimming test is commonly used to assess antidepressant-like activity, where the compound's ability to reduce immobility time is measured. The elevated plus maze or other anxiety tests can be used to assess anxiolytic-like effects. Microinjection studies into the dorsal raphe are also conducted to assess the reversal of MCH-induced prodepressive effects. These studies demonstrate the in vivo efficacy of ATC0175 in relevant behavioral models.
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| ADME/Pharmacokinetics |
ATC0175 HCl is orally active, supporting its development as an oral therapeutic agent. However, detailed pharmacokinetic parameters such as half-life, Cmax, and bioavailability are not extensively detailed in the available literature. As a hydrochloride salt, it exhibits enhanced aqueous solubility for administration. Its oral bioavailability and ability to cross the blood-brain barrier are important for its central nervous system activity. The compound's pharmacokinetic profile supports its investigation for the treatment of psychiatric disorders.
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| Toxicity/Toxicokinetics |
Specific toxicity data for ATC0175 HCl are not extensively detailed in the available literature. As a MCHR1 antagonist with additional serotonergic receptor affinities, its toxicity profile is likely related to its pharmacological activity. Preclinical toxicology studies would typically be conducted to assess the compound's safety margin for the treatment of depression and anxiety. However, these specific data are not provided in the search results. The compound's safety would be evaluated in standard in vitro and in vivo models as part of drug development.
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| References | |
| Additional Infomation |
ATC0175 HCl is a research compound that has been investigated for the potential treatment of depression and anxiety disorders. It is a potent, selective, and orally active MCHR1 antagonist that has shown anxiolytic- and antidepressant-like effects in preclinical studies. The compound was developed as a non-peptidic small molecule belonging to the quinazoline derivative class. It is not approved for clinical use and is intended for research purposes only, serving as a valuable tool for studying the role of MCHR1 in stress, emotion, anxiety, and depression.
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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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| InChi Key |
HUUPKFUYSQNNLO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H25F2N5O.ClH/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);1H
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| Chemical Name |
N-[4-[[4-(dimethylamino)quinazolin-2-yl]amino]cyclohexyl]-3,4-difluorobenzamide;hydrochloride
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| Synonyms |
ATC0175 ATC-0175
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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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