AR 231453

Name: AR 231453
Brand: MedChemExpress
SKU: HY-15564
Rating: 4.5 (1 reviews)

Cat. No.: HY-15564 Purity: 99.70%: FAQs
Data Sheet SDS COA Handling Instructions Technical Support

AR 231453 is a potent, specific and orally available GPR119 agonist. AR 231453 can stimulate β-cell replication and improve islet graft function s.

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

AR 231453 Chemical Structure

CAS No. : 733750-99-7

Size	Stock	Quantity

Free Sample (0.1 - 0.5 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE AR 231453

•Nat Commun. 2022 Nov 17;13(1):7033. [Abstract]

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Description

AR 231453 is a potent, specific and orally available GPR119 agonist. AR 231453 can stimulate β-cell replication and improve islet graft function s^[1]^[2].

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	0.003 mM Compound: 1, AR231453	Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay	[PMID: 24751443]
HEK293	EC₅₀	0.7 μM Compound: 2; AR231453	Agonist activity at CREB-LBD and GAL4-DBD fused human GPR119 expressed in HEK293 cells by luciferase reporter gene assay Agonist activity at CREB-LBD and GAL4-DBD fused human GPR119 expressed in HEK293 cells by luciferase reporter gene assay	[PMID: 27560285]
HEK293	EC₅₀	4.78 nM Compound: AR231543	Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay	[PMID: 31630858]

In Vitro

AR 231453 is inactive at all other GPCRs tested (more than 230, including all known pancreatic islet receptors), indicating that it is highly selective for GPR119^[1].
AR 231453 potently stimulats cAMP accumulation (EC₅₀ = 4.7 nM) with a maximal efficacy similar to that seen with forskolin. AR 231453 significantly enhancesinsulin release in HIT-T15 cells, with an EC₅₀ of 3.5 nM^[1].
AR 231453 also stimulates insulin release in isolated mouse islets at glucose concentrations ranging from 8-17 mM^[1].

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

In Vivo

AR231453 (20 mg/kg, orally) markedly improves oral glucose tolerance in a dose-dependent fashion, with efficacy similar to maximally effective doses of the sulfonylurea glyburide^[1].

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

Animal Model:	Mice^[1].
Dosage:	20 mg/kg.
Administration:	Orally, once.
Result:	Improved glucose tolerance in mice.

Molecular Weight

505.52

Formula

C₂₁H₂₄FN₇O₅S

CAS No.

733750-99-7

Appearance

Solid

Color

Light yellow to yellow

SMILES

CC(C)C1=NOC(C2CCN(C3=NC=NC(NC4=CC=C(S(=O)(C)=O)C=C4F)=C3[N+]([O-])=O)CC2)=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (49.45 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9782 mL	9.8908 mL	19.7816 mL
5 mM	0.3956 mL	1.9782 mL	3.9563 mL
10 mM	0.1978 mL	0.9891 mL	1.9782 mL

View the 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.70%

Select Batch:

Data Sheet (272 KB) SDS (251 KB)

COA (248 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. Chu ZL, et al. A role for beta-cell-expressed G protein-coupled receptor 119 in glycemic control by enhancing glucose-dependent insulin release. Endocrinology. 2007 Jun;148(6):2601-9. [Content Brief]

[2]. J Gao, et al. Stimulating β-cell replication and improving islet graft function by AR231453, A GPR119 agonist. Transplant Proc. 2011 Nov;43(9):3217-20. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.9782 mL	9.8908 mL	19.7816 mL	49.4540 mL
	5 mM	0.3956 mL	1.9782 mL	3.9563 mL	9.8908 mL
	10 mM	0.1978 mL	0.9891 mL	1.9782 mL	4.9454 mL
	15 mM	0.1319 mL	0.6594 mL	1.3188 mL	3.2969 mL
	20 mM	0.0989 mL	0.4945 mL	0.9891 mL	2.4727 mL
	25 mM	0.0791 mL	0.3956 mL	0.7913 mL	1.9782 mL
	30 mM	0.0659 mL	0.3297 mL	0.6594 mL	1.6485 mL
	40 mM	0.0495 mL	0.2473 mL	0.4945 mL	1.2364 mL

AR 231453 Related Classifications

Metabolic Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AR 231453733750-99-7AR231453AR-231453GPR119G Protein-Coupled Receptor 119GPCRHIT-T15insulinglucosediabetesInhibitorinhibitorinhibit

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AR 231453

Customer Review

AR 231453 Related Antibodies

1 Publications Citing Use of MCE AR 231453

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AR 231453 Related Antibodies

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Complete Stock Solution Preparation Table

AR 231453 Related Classifications

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