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ACH-000143

Alias: ACH 000143; ACH-000143; ACH000143
Cat No.:V2307 Purity: ≥98%
ACH-000143 is a potent, orally bioactive melatonin receptor agonist (activator) with EC50s of 0.06 nM and 0.32 nM for MT1 and MT2, respectively.
ACH-000143
ACH-000143 Chemical Structure CAS No.: 2225836-30-4
Product category: Melatonin Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
Other Sizes
Official Supplier of:
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Product Description
ACH-000143 is a potent, orally bioactive melatonin receptor agonist (activator) with EC50s of 0.06 nM and 0.32 nM for MT1 and MT2, respectively.
Biological Activity I Assay Protocols (From Reference)
Targets
MT1 ( EC50 = 0.06 nM ); MT2 ( EC50 = 0.32 nM )
ln Vivo
ACH-000143 reduces steatosis and liver triglycerides in diet-induced obese rats[1].
ACH-000143 is not hERG binding, genotoxic, or accompanied by behavioral changes at doses up to 100 mg/kg p.o., indicating that it is a compound that merits more research as a potential medication[1].
ACH-000143 significantly lowers plasma glucose at 10 mg/kg (−16.4%, p < 0.05) and 30 mg/kg (−16.9%, p < 0.01)[1].
Animal Protocol
High-fat diet rats
10 and 30 mg/kg
Orally, once daily for two months.
References

[1]. Discovery of ACH-000143: A Novel Potent and Peripherally Preferred Melatonin Receptor Agonist that Reduces Liver Triglycerides and Steatosis in Diet-Induced Obese Rats. J Med Chem. 2021 Feb 25;64(4):1904-1929.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C13H16CLN3O3
Molecular Weight
297.7374
Exact Mass
297.09
Elemental Analysis
C, 52.44; H, 5.42; Cl, 11.91; N, 14.11; O, 16.12
CAS #
2225836-30-4
Related CAS #
2225836-30-4
PubChem CID
139451790
Appearance
White to off-white solid powder
LogP
1.6
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
4
Rotatable Bond Count
5
Heavy Atom Count
20
Complexity
345
Defined Atom Stereocenter Count
0
InChi Key
BVSLRGAPRGQWNC-UHFFFAOYSA-N
InChi Code
InChI=1S/C13H16ClN3O3/c1-8(18)15-4-5-17-11-7-12(19-2)9(14)6-10(11)16-13(17)20-3/h6-7H,4-5H2,1-3H3,(H,15,18)
Chemical Name
N-[2-(5-chloro-2,6-dimethoxybenzimidazol-1-yl)ethyl]acetamide
Synonyms
ACH 000143; ACH-000143; ACH000143
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: This product requires protection from light (avoid light exposure) during transportation and storage.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~50 mg/mL (~167.9 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.40 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (8.40 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (8.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.3586 mL 16.7932 mL 33.5864 mL
5 mM 0.6717 mL 3.3586 mL 6.7173 mL
10 mM 0.3359 mL 1.6793 mL 3.3586 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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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