AH-7614

Alias: AH-7614 AH7614 AH 7614

Cat No.:V7948 Purity: ≥98%

COA Product Data Instructions for use SDS

AH-7614 is a potent and specific FFA4 (GPR120) antagonist (inhibitor) with pIC50s of 7.1, 8.1 and 8.1 for human, mouse and rat FFA4, respectively.

AH-7614 Chemical Structure CAS No.: 6326-06-3
Product category: New1

This product is for research use only, not for human use. We do not sell to patients.

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Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Biological Data

Product Description

AH-7614 is a potent and specific FFA4 (GPR120) antagonist (inhibitor) with pIC50s of 7.1, 8.1 and 8.1 for human, mouse and rat FFA4, respectively. AH-7614 is more selective for FFA4 than FFA1 (pIC50<4.6). AH-7614 blocks the effects of the polyunsaturated omega-6 fatty acid linoleic acid and FFA4 agonists.

Biological Activity I Assay Protocols (From Reference)

ln Vitro	In U2OS cells expressing FFA4, AH-7614 (Compound 39) (0.063-1 μM) inhibits the intracellular Ca2+ response brought on by linoleic acid and FFAR4 agonist [1]. In NCI-H716 cells, the increasing impact of GSK137647A on glucose-stimulated insulin production was eliminated by AH-7614 (100 μM) [1]. TUG-891-mediated internalization of FFA4 from the cell surface is blocked by AH-7614 (0.001-10 μM; 15 minutes) (pIC50=7.70) [2]. AH-7614 (10 μM; 30 minutes) inhibits intracellular myo-inositol monophosphate and FFA4 phosphorylation increases brought on by agonists [2].
ln Vivo	In mice, AH7614 (50 μg administered intraperitoneally every 4 μd for 20 days) can inhibit the formation of tumors [3]. ? When paired with epirubicin, AH7614 (50 μg; intratumoral injection given one day prior to the latter) can increase the susceptibility of cancer cells to chemotherapy by blocking GPR120 signaling and preventing tumor growth [3].
References	[1]. Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). Bioorg Med Chem Lett. 2014 Jul 15;24(14):3100-3. [2]. Probe-Dependent Negative Allosteric Modulators of the Long-Chain Free Fatty Acid Receptor FFA4. Mol Pharmacol. 2017 Jun;91(6):630-641. [3]. Fatty acid receptor GPR120 promotes breast cancer chemoresistance by upregulating ABC transporters expression and fatty acid synthesis. EBioMedicine. 2019 Feb;40:251-262.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula	C20H17NO3S
Molecular Weight	351.42
Exact Mass	351.093
Elemental Analysis	C, 68.36; H, 4.88; N, 3.99; O, 13.66; S, 9.12
CAS #	6326-06-3
PubChem CID	233085
Appearance	White to off-white solid powder
Density	1.37g/cm3
Boiling Point	505.9ºC at 760mmHg
Flash Point	259.8ºC
Index of Refraction	1.685
LogP	5.64
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	3
Heavy Atom Count	25
Complexity	528
Defined Atom Stereocenter Count	0
InChi Key	OZCQEUZTOAAWDK-UHFFFAOYSA-N
InChi Code	InChI=1S/C20H17NO3S/c1-14-10-12-15(13-11-14)25(22,23)21-20-16-6-2-4-8-18(16)24-19-9-5-3-7-17(19)20/h2-13,20-21H,1H3
Chemical Name	4-methyl-N-(9H-xanthen-9-yl)benzenesulfonamide
Synonyms	AH-7614 AH7614 AH 7614
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 (~284.56 mM)
Solubility (In Vivo)	Solubility in Formulation 1: ≥ 2.5 mg/mL (7.11 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.)

Solubility (In Vitro)

DMSO : ~100 mg/mL (~284.56 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (7.11 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	2.8456 mL	14.2280 mL	28.4560 mL
	5 mM	0.5691 mL	2.8456 mL	5.6912 mL
	10 mM	0.2846 mL	1.4228 mL	2.8456 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

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See Example

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.

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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

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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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To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

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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The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

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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.

Note： (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.

Biological Data

AH-7614 is a potent and selective inhibitor of both human and murine FFA4 function. Flp-In T-REx 293 cells induced to express hFFA4-eYFP were pretreated with either vehicle [1% (v/v) DMSO] or increasing concentrations of AH-7614 for 15 minutes, after which time they were treated with either 50 µM aLA (A) or 500 nM TUG-891 (B). Both aLA and TUG-891 induced calcium release that was potently inhibited in the presence of AH-7614 (aLA, pIC50 = 7.51 ± 0.08, n = 3; TUG-891, pIC50 = 8.13 ± 0.08, n = 3). HEK293T cells transiently expressing hFFA4-eYFP and β-arrestin-2-Renilla luciferase were preincubated with either vehicle [1% (v/v) DMSO] or increasing concentrations of AH-7614. The cells were then treated with either 50 µM aLA (C) or 500 nM TUG-891 (D), and β-arrestin-2 recruitment was subsequently determined using a BRET-based assay. Both aLA and TUG-891 promoted β-arrestin-2 recruitment that was potently inhibited (aLA, pIC50 = 7.66 ± 0.05, n = 5; TUG-891, pIC50 = 7.55 ± 0.07, n = 5) in the presence of increasing concentrations of AH-7614. mFFA4-dependent β-arrestin-2 recruitment in the presence of either 50 µM aLA (E) or 500 nM TUG-891.[2]. Watterson KR, et, al. Probe-Dependent Negative Allosteric Modulators of the Long-Chain Free Fatty Acid Receptor FFA4. Mol Pharmacol. 2017 Jun;91(6):630-641.

AH-7614 blocks agonist-induced receptor internalization of the human FFA4 receptor. Flp-In T-REx 293 cells induced to express hFFA4-mVenus were pretreated with 10 µM AH-7614 for 15 minutes, after which time cells were further treated with either vehicle [0.1% (v/v) DMSO] or TUG-891 (3 µM) for 30 minutes (A) and subsequently fixed. AH-7614 prevented TUG-891 induced receptor internalization (pIC50 = 7.70 ± 0.10). Cells were pretreated with varying concentrations of AH-7614 and exposed to increasing concentrations of TUG-891 (B) for 30 minutes, after which they were fixed. Cells were imaged using a Cellomics ArrayScan II, and the extent of internalization of the receptor construct was quantified.[2]. Watterson KR, et, al. Probe-Dependent Negative Allosteric Modulators of the Long-Chain Free Fatty Acid Receptor FFA4. Mol Pharmacol. 2017 Jun;91(6):630-641.

TUG-1387 and TUG-1506 are chemical derivatives of AH-7614 with varying activity at FFA4. (A) Chemical structures of AH-7614, TUG-1387, and TUG-1506. HEK293T cells transiently coexpressing hFFA4-eYFP and β-arrestin-2–Renilla luciferase were preincubated with vehicle (0.1% DMSO) or increasing concentrations of AH-7614, TUG-1387, or TUG-1506. β-Arrestin-2 recruitment to the receptor was then determined in the presence 500 nM TUG-891 (B). All data represent experiments carried out in triplicate at least three times.[2]. Watterson KR, et, al. Probe-Dependent Negative Allosteric Modulators of the Long-Chain Free Fatty Acid Receptor FFA4. Mol Pharmacol. 2017 Jun;91(6):630-641.