AM4113 (Synonyms: AM4113) |
カタログ番号GC15093
One-Click Copy Product Info
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AM4113 は、特許 WO2016184310A1 から抽出されたカイマビノイド 1 (CB1) アンタゴニストであり、化合物 3 は、in vivo で CB1 を 25.5 nM の IC50 で阻害します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 614726-85-1
Sample solution is provided at 25 µL, 10mM.
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AM4113, a pyrazole analog structurally related to SR141716 and AM251, is a novel cannabinoid CB1 neutral antagonist. AM4113 suppressed food intake and food-reinforced behavior in rats.
In vitro: AM4113 was able to bind with high affinity to CB1 receptors, exhibiting 100-fold selectivity for CB1 against CB2 receptors. The Ki value for CB1 was 0.897 ± 0.44 nM, while the Ki value for hCB2 was 92 ± 6.9 nM [1].
In vivo: In rats, treatment with AM4113 (2.0 and 4.0 mg/kg) attenuated the AM411-induced locomotor suppression and analgesia. In addition, 4.0 mg/kg AM4113 alone significantly suppressed locomotor activity when compared with vehicle. AM4113 dose-dependently decreased lever pressing on an FR1 schedule. AM4113 produced conditioned taste avoidance and suppression of ingestive (hedonic) taste reactivity scores in a dose-dependent manner [1]. AM4113 didn’t induce signs of nausea [1].
Reference:
[1] Sink K S, McLaughlin P J, Wood J A T, et al. The novel cannabinoid CB1 receptor neutral antagonist AM4113 suppresses food intake and food-reinforced behavior but does not induce signs of nausea in rats[J]. Neuropsychopharmacology, 2008, 33(4): 946-955.
| Cas No. | 614726-85-1 | SDF | |
| 同義語 | AM4113 | ||
| Chemical Name | 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide | ||
| Canonical SMILES | ClC1=CC(Cl)=CC=C1N2C(C3=CC=C(Cl)C=C3)=C(C)C(C(N)=O)=N2 | ||
| Formula | C17H12Cl3N3O | M.Wt | 380.7 |
| 溶解度 | ≤0.5mg/ml in ethanol;3mg/ml in DMSO;10mg/ml in dimethyl formamide | Storage | Store at -20°C |
| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6267 mL | 13.1337 mL | 26.2674 mL |
| 5 mM | 525.3 μL | 2.6267 mL | 5.2535 mL |
| 10 mM | 262.7 μL | 1.3134 mL | 2.6267 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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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 saline, 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: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 27 reference(s) in Google Scholar.)