ACH-000143
Based on 1 Customer Validation
ACH-000143 is a potent and orally active melatonin receptor agonist, with EC50 values of 0.06 nM and 0.32 nM for MT1 and MT2, respectively.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.58%
- CAS 番号: 2225836-30-4
- 分子式: C13H16ClN3O3
- 分子量:297.74
-
保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
生物活性
|
MT1 0.06 nM (EC50) |
MT2 0.32 nM (EC50) |
ACH-000143 is devoid of hERG binding, genotoxicity, and behavioral alterations at doses up to 100 mg/kg p.o., supporting further investigation of this compound as a drug candidate[1].
ACH-000143 significantly reduces plasma glucose at 10 mg/kg (−16.4%, p < 0.05) and 30 mg/kg (−16.9%, p < 0.01)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:High-fat diet rats[1].
-
Dosage:10 and 30 mg/kg.
-
Administration:Orally, once daily for two months.
-
Result:Significantly reduced the weekly BW gain on weeks.
化学情報
-
CAS 番号 2225836-30-4
-
性状 Solid
-
分子量 297.74
-
分子式 C13H16ClN3O3
-
Color White to off-white
-
SMILES
CC(NCCN1C2=CC(OC)=C(Cl)C=C2N=C1OC)=O
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
DMSO : 50 mg/mL (167.93 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.40 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.40 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
-
データシート (275 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.3586 mL | 16.7932 mL | 33.5864 mL | 83.9659 mL |
| 5 mM | 0.6717 mL | 3.3586 mL | 6.7173 mL | 16.7932 mL | |
| 10 mM | 0.3359 mL | 1.6793 mL | 3.3586 mL | 8.3966 mL | |
| 15 mM | 0.2239 mL | 1.1195 mL | 2.2391 mL | 5.5977 mL | |
| 20 mM | 0.1679 mL | 0.8397 mL | 1.6793 mL | 4.1983 mL | |
| 25 mM | 0.1343 mL | 0.6717 mL | 1.3435 mL | 3.3586 mL | |
| 30 mM | 0.1120 mL | 0.5598 mL | 1.1195 mL | 2.7989 mL | |
| 40 mM | 0.0840 mL | 0.4198 mL | 0.8397 mL | 2.0991 mL | |
| 50 mM | 0.0672 mL | 0.3359 mL | 0.6717 mL | 1.6793 mL | |
| 60 mM | 0.0560 mL | 0.2799 mL | 0.5598 mL | 1.3994 mL | |
| 80 mM | 0.0420 mL | 0.2099 mL | 0.4198 mL | 1.0496 mL | |
| 100 mM | 0.0336 mL | 0.1679 mL | 0.3359 mL | 0.8397 mL |