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BC1618

Alias: BC1618BC 1618BC-1618
Cat No.:V2440 Purity: ≥98%
BC1618, an orally bioactive Fbxo48 inhibitor, stimulates Ampk signaling (preventing activated pAmpkα from being degraded by the Fbxo48-mediated proteasome).
BC1618
BC1618 Chemical Structure CAS No.: 2222094-18-8
Product category: AMPK
This product is for research use only, not for human use. We do not sell to patients.
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Product Description
BC1618, an orally bioactive Fbxo48 inhibitor, stimulates Ampk signaling (preventing activated pAmpkα from being degraded by the Fbxo48-mediated proteasome). BC1618 promotes mitochondrial fission, promotes autophagy, and improves liver insulin sensitivity.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
During CHX treatment, BC1618 improves the stability of the pAmpkα protein [1]. Compared to metformaldehyde, BC1618 stimulates pAmpkα activity in cells over a thousandfold [1]. A trend in pAmpkα and pACC protein levels is induced by BC1618 (0.1-2 μM, 16 hours), while BC1618 (1 μM) effectively breaks the link between Fbxo48 and pAmpkα while having no effect on Fbxo48, Ampkα1, or Ampkα2 messenger RNA. In human primary-like hepatocytes, dose-and time-dependent increases were also verified [1]. During intermittent depletion, BC1618 increases the abundance of several autophagy marker proteins. In line with the established mTOR inhibitory function played by activated Ampk, BC1618 decreases pS6 levels and phosphorylates the mTORC1-related protein Raptor [1].
ln Vivo
In high-fat diet-induced electrode nozzles, BC1618 fosters ischemic defects, enhances autophagy, and improves diabetic insulin [1]. BC1618 exhibits superior electrode tolerance and seems to be roughly 1,000 times more effective than the dimethyl bielectrode. With a peak value of 2 in 0.5 hours following 20 mg/kg in the blood vessel wall, BC1618 exhibits remarkable blood vessel wall bioavailability. 000ng/mL, with blood vessels reaching a peak value of 500ng/mL after 4 hours[1].
Cell Assay
Western Blot analysis [1]
Cell Types: BEAS-2B cells. 1].
Tested Concentrations: 0-2μM.
Incubation Duration: 16 hrs (hours).
Experimental Results: The induced pAmpkα and pACC protein levels were dose-dependent.
Animal Protocol
Animal/Disease Models: C57BL/6 mice[1].
Doses: 2 or 10 mg/kg (challenge with LPS (3 mg/kg) for an additional 18 hrs (hrs (hours))). Management: IP, once.
Experimental Results: Lung inflammation was diminished in endotoxin-treated mice.

Animal/Disease Models: C57BL/6 mice[1].
Doses: 15 and 30 mg/kg/day. How to take: Drink water for 3 months.
Experimental Results: No significant toxicity was demonstrated.
References

[1]. A Fbxo48 inhibitor prevents pAMPKα degradation and ameliorates insulin resistance. Nat Chem Biol. 2021 Mar;17(3):298-306.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C24H24F3NO2
Molecular Weight
415.4481
Exact Mass
415.18
Elemental Analysis
C, 69.38; H, 5.82; F, 13.72; N, 3.37; O, 7.70
CAS #
2222094-18-8
PubChem CID
134417552
Appearance
White to off-white solid powder
LogP
5.2
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
6
Rotatable Bond Count
9
Heavy Atom Count
30
Complexity
448
Defined Atom Stereocenter Count
0
InChi Key
LGTYABNNHILKHF-UHFFFAOYSA-N
InChi Code
InChI=1S/C24H24F3NO2/c25-24(26,27)21-11-13-23(14-12-21)30-18-22(29)17-28(15-19-7-3-1-4-8-19)16-20-9-5-2-6-10-20/h1-14,22,29H,15-18H2
Chemical Name
2-Propanol, 1-[bis(phenylmethyl)amino]-3-[4-(trifluoromethyl)phenoxy]-
Synonyms
BC1618BC 1618BC-1618
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

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 : ~100 mg/mL (~240.70 mM)
H2O : < 0.1 mg/mL
Solubility (In Vivo)
Solubility in Formulation 1: 2.5 mg/mL (6.02 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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.

Solubility in Formulation 2: ≥ 2.5 mg/mL (6.02 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.

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Solubility in Formulation 3: 5 mg/mL (12.04 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.4070 mL 12.0351 mL 24.0703 mL
5 mM 0.4814 mL 2.4070 mL 4.8141 mL
10 mM 0.2407 mL 1.2035 mL 2.4070 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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  • 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
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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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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