Cat. No.: HY-P1124

AS2034178 free base

AS2034178 free base is an orally active GPR40/FFAR1 agonist. AS2034178 free base elevates intracellular calcium through the Gq/PLC/PKC pathway, stimulates glucose-dependent insulin secretion, and activates GLP-2 production in intestinal L cells. AS2034178 free base inhibits transient, late, and persistent sodium currents, and blocks the delayed rectifier potassium current. AS2034178 free base activates c-Src, AKT, NF-κB, and cyclooxygenase signaling pathways, inhibits EGFR/ERK and STAT signaling pathways, modulates EMT markers, promotes tumor cell proliferation and growth, and inhibits migration and invasion. AS2034178 free base can be used for research on type 2 diabetes, DSS-induced colitis, and papillary renal cell carcinoma.

For research use only. We do not sell to patients.

CAS No.: 1030846-42-4
Formula: C₂₇H₂₉FN₂O₃
Molecular Weight:448.53

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (286 KB)

AS2034178 free base Chemical Structure

CAS No.: 1030846-42-4

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Use of MCE Products

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]^[2]^[3]^[4]

Akt

NF-κB

COX-2

PI3K

C-src

erk1

ERK2

EGFR

STAT3

All Free Fatty Acid Receptor Isoforms :

All PKC Isoforms :

All Src Isoforms :

All Akt Isoforms :

All NF-κB Isoforms :

All PI3K Isoforms :

All COX Isoforms :

All EGFR Isoforms :

All STAT Isoforms :

All Sodium Channel Isoforms :

In Vitro

Anti-cancerCarbohydrate MetabolismOthers

Anti-cancer

AS2034178 (10 µM; once every 24 h for 6 days) free base promotes ACHN pRCC cell proliferation, and this effect is reversed by FFA1 antagonism^[3].
AS2034178 (10 µM) free base-driven ACHN proliferation depends on the AKT, NF-κB, and COX-2 signaling pathways, and MK2206 (HY-108232) and BAY 11-7082 (HY-13453) reduce this effect by approximately 70% and 80%, respectively^[3].
AS2034178 (10 µM; 24 h) free base inhibits ACHN scratch wound healing/migration, and GW1100 (HY-50691) reverses this effect^[3].
AS2034178 (10 µM; 24 h) free base reduces ACHN Matrigel invasion and partially blocks EGF-stimulated invasion^[3].
AS2034178 (0-24 h) free base activates the c-Src/PI3K/AKT/NF-κB/COX-2 signaling pathway in ACHN pRCC cells^[3].
AS2034178 (10 μM; 0-24 h) free base inhibits EGFR Tyr1068 and ERK1/2 phosphorylation in ACHN pRCC cells and partially blocks EGF-induced EGFR/ERK signaling^[3].
AS2034178 (10 μM; 0-24 h) free base inhibits STAT3 Tyr705 phosphorylation in ACHN pRCC cells in an EGFR- and β-arrestin-independent manner^[3].
AS2034178 (0-24 h) free base reduces E-cadherin, vimentin, and fibronectin-1 levels in ACHN pRCC cells without affecting N-cadherin, and the regulation of fibronectin-1 involves β-arrestin signaling^[3].

Carbohydrate Metabolism

AS2034178 (0.1-3 µM; 20 min) free base enhances glucose-dependent insulin secretion in MIN6 cells only under high-glucose (22.4 mM) conditions^[1].

Others

AS2034178 (0.001-100 µM; 2 h) free base is a potent human GPR40 agonist in the CHO Ca²⁺ flux assay^[1].
AS2034178 (1-100 μM) free base inhibits transient and delayed voltage-gated Na⁺ currents in GH3 pituitary prolactin cells, with IC₅₀ values of 29.8 μM and 5.3 μM for I_{Na (T)} and I_{Na (L)}, respectively^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[3]

Cell Line:

ACHN human papillary RCC cells
Concentration:

10 µM
Incubation Time:

every 24 h for 6 days; cell counts every 24 h
Result:

Increased ACHN cell proliferation on days 5 and 6 compared with vehicle-treated cells.
GW1100 blocked the increase on days 5 and 6.

Cell Migration Assay ^[3]

Cell Line:

ACHN human papillary RCC cells
Concentration:

10 µM
Incubation Time:

24 h
Result:

Wider wounds than control cells were observed after 24 h, indicating inhibition of migration.
GW1100 blocked the negative effect on wound closure and increased wound healing.

Cell Invasion Assay^[3]

Cell Line:

ACHN human papillary RCC cells
Concentration:

10 µM
Incubation Time:

24 h
Result:

Reduced ACHN invasion through Matrigel.
Partially inhibited EGF-induced invasion in EGF-stimulated cells.

Western Blot Analysis^[3]

Cell Line:

ACHN human papillary RCC cells
Concentration:

10 µM
Incubation Time:

24 h
Result:

Inhibited EGFR Tyr1068 and ERK1/2 phosphorylation in ACHN pRCC cells.
Partially blocked EGF-induced EGFR/ERK signaling.
Inhibited STAT3 Tyr705 phosphorylation in ACHN pRCC cells in an EGFR- and β-arrestin-independent manner.

In Vivo

Anti-cancerCarbohydrate MetabolismLipid MetabolismInnate ImmunityCytokines & Chemokines

Anti-cancer

AS2034178 (10 mg/kg; i.p.; once daily; 28 days) free base promotes pRCC xenograft tumor growth in homozygous athymic nude mice, increases tumor volume from day 16 of dosing, and increases final tumor weight compared with vehicle^[3].

Carbohydrate Metabolism

AS2034178 (0.3-10 mg/kg; p.o.; single administration; 30 minutes before oral glucose) free base improves glucose tolerance in normal ICR mice and exhibits glucose-dependent insulinotropic secretion^[1].
AS2034178 (1 mg/kg; p.o.; once daily for 10 consecutive days) free base repeated administration improves insulin sensitivity in ob/ob mice^[1].

Carbohydrate Metabolism

Lipid Metabolism

AS2034178 (0.03-1 mg/kg; p.o.; once daily; administration for 4 weeks) free base repeated dosing improves systemic glucose metabolism and disease-related biomarkers in ob/ob mice^[1].

Innate Immunity

Cytokines & Chemokines

AS2034178 (1-10 mg/kg; p.o.; once daily; days 0-6) free base attenuates DSS-induced colitis in mice and increases colonic GLP-2 without affecting plasma GLP-2^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

ICR (male; 5 weeks at purchase)^[1]
Dosage:

0.3, 1, 3, and 10 mg/kg
Administration:

p.o.; single dose 30 minutes before oral glucose
Result:

Dose-dependently suppressed the rise in plasma glucose after oral glucose; plasma glucose AUC was decreased at doses over 1 mg/kg.
Plasma insulin after oral glucose increased dose-dependently, with the 5-minute plasma insulin increase reported at doses over 3 mg/kg.

Animal Model:

ob/ob (male; 7 weeks)^[1]
Dosage:

0.03, 0.1, 0.3, and 1 mg/kg
Administration:

p.o.; once daily; repeated for 4 weeks
Result:

Plasma glucose decreased dose-dependently and reached maximum efficacy at dosages over 0.1 mg/kg; efficacy was observed from 0.03 mg/kg.
HbA1c decreased dose-dependently by approximately 1.5%.
Plasma insulin decreased dose-dependently.
Pancreatic insulin content increased dose-dependently and reached maximum efficacy at dosages over 0.1 mg/kg.
Plasma triglyceride levels were unchanged.
Body weight decreased at 1 mg/kg, with no body weight effect at the other doses.

Animal Model:

ob/ob (male; 7 weeks)^[1]
Dosage:

1 mg/kg
Administration:

p.o.; once daily for 10 days
Result:

At both insulin doses, plasma glucose decreased at 30 and 60 minutes after insulin administration compared with vehicle.

Animal Model:

C57BL/6 (male, 9-12 weeks, 22-26 g)^[2]
Dosage:

1 mg/kg; 3 mg/kg; 10 mg/kg
Administration:

p.o.; once daily; days 0-6
Result:

DSS increased the disease activity index from day 4, peaking on day 7.
Attenuated the increase in disease activity index in a dose-dependent manner, with reductions at 3 and 10 mg/kg relative to DSS alone.
Restored DSS-reduced colon length dose-dependently, with the 10 mg/kg group differing from DSS control.
Histological damage was mitigated at 3 and 10 mg/kg, with lower histological scores than DSS controls.
Blocked the DSS-induced increase in colonic MPO activity and reduced TNF-α mRNA expression.
IL-1β and IL-6 mRNA showed a decreasing tendency at 3 and 10 mg/kg.
Colonic tissue GLP-2 was decreased by DSS and was increased dose-dependently, with an increase at 10 mg/kg.
Plasma GLP-2 was not affected compared with DSS control.

Animal Model:

homozygous athymic nude (strain code 490; male; 3-4 weeks old)^[3]
Dosage:

10 mg/kg
Administration:

i.p.; daily; 28 days
Result:

Tumors were larger than vehicle-control tumors beginning at day 16 of administration and remained larger through the 28-day administration period.
Final average tumor weight was higher than in the vehicle-control group.

Related Protocols :

Chemical Information

CAS No. 1030846-42-4
Molecular Weight 448.53
Formula C₂₇H₂₉FN₂O₃
SMILES

O=C(O)CCC1=CC=C(NCC2=CC=CC3=C2CCCN3CCOC4=CC=CC=C4)C=C1F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Tanaka H, et al. Chronic treatment with novel GPR40 agonists improve whole-body glucose metabolism based on the glucose-dependent insulin secretion. The Journal of pharmacology and experimental therapeutics. 2013 Sep 1;346(3):443-52. [Content Brief]

[2]. Kato S, et al. G protein-coupled receptor 40 activation ameliorates dextran sulfate sodium-induced colitis in mice via the upregulation of glucagon-likepeptide-2. Journal of pharmacological sciences. 2019 Jun;140(2):144-152.

[3]. Karmokar PF, et al. Free-fatty acid receptor-1 (FFA1/GPR40) promotes papillary RCC proliferation and tumor growth via Src/PI3K/AKT/NF-κB but suppresses migration by inhibition of EGFR, ERK1/2, STAT3 and EMT. Cancer Cell International. 2023 Jun 24;23(1):126.

[4]. Chou CJ, et al. Evidence for effective suppression of INa and IK (DR) by AS2034178 (bis {2-[(4-{(4′-(2-hydroxyethoxy)-2′-methyl [1, 1′-biphenyl]-3-yl) methoxy} phenyl] methyl]-3, 5-dioxo-1, 2, 4-oxadiazolidin-4-ide} tetrahydrate), an agonist of free fatty acid receptor. Neuroscience Letters. 2025 Apr 23;855:138222.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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AS2034178 free base

All Free Fatty Acid Receptor Isoforms

All PKC Isoforms

All Src Isoforms

All Akt Isoforms

All NF-κB Isoforms

All PI3K Isoforms

All COX Isoforms

All EGFR Isoforms

All STAT Isoforms

All Sodium Channel Isoforms