ATC 0065 |
| Katalog-Nr.GC10994 |
MCH1 antagonist,potent and selective
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 510732-84-0
Sample solution is provided at 25 µL, 10mM.
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ATC0065 is a selective and potent antagonist of the melanin-concentrating hormone receptor 1 (MCH1) with IC50 of 15.7 nM. This component also displays affinity for 5-HT1A and 5-HT2B receptors with IC50 of 62.9nM and 266 nM respectively.
Melanin-concentrating hormone receptor (MCH1), a member of the G protein-coupled receptor family 1, is an integral plasma membrane protein which binds melanin-concentrating hormone. The protein can inhibit cAMP accumulation and stimulate intracellular calcium flux, and is probably involved in the neuronal regulation of food consumption.
In vitro assay, ATC0065 bounds with high affinity to the MCH-R1 with IC50 value of 16 nMand showed good metabolic stability in liver microsomes isolated from human and rat 1.
In rodents, ATC0065 is potent and orally active MCHR1 antagonists with anxiolytic and antidepressant activity. ATC0065 treatmetn significantly reversed swim stress-induced anxiety in the stress-induced hyperthermia in mice and elevated plus-maze test in rats2. However, ATC0065 did not affect spontaneous locomotor activity or rotarod performance in rats 2.
References:
1. Kanuma K, Omodera K, Nishiguchi M, et al. Identification of 4-amino-2-cyclohexylaminoquinazolines as metabolically stable melanin-concentrating hormone receptor 1 antagonists. Bioorganic & medicinal chemistry. 2006;14(10):3307-3319.
2. Chaki S, Funakoshi T, Hirota-Okuno S, et al. Anxiolytic- and antidepressant-like profile of ATC0065 and ATC0175: nonpeptidic and orally active melanin-concentrating hormone receptor 1 antagonists. The Journal of pharmacology and experimental therapeutics. 2005;313(2):831-839.
| Cas No. | 510732-84-0 | SDF | |
| Chemical Name | N2-((1r,4r)-4-((4-bromo-2-(trifluoromethoxy)phenethyl)amino)cyclohexyl)-N4,N4-dimethylquinazoline-2,4-diamine dihydrochloride | ||
| Canonical SMILES | BrC1=CC=C(C(OC(F)(F)F)=C1)CCN[C@@H](CC2)CC[C@H]2NC3=NC4=CC=CC=C4C(N(C)C)=N3.Cl.Cl | ||
| Formula | C25H29BrF3N5O.2HCl | M.Wt | 625.35 |
| Löslichkeit | Soluble in DMSO | Storage | Desiccate at RT |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.5991 mL | 7.9955 mL | 15.991 mL |
| 5 mM | 0.3198 mL | 1.5991 mL | 3.1982 mL |
| 10 mM | 0.1599 mL | 0.7996 mL | 1.5991 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)
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