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  6. Aurantiamide

Aurantiamide is a non-covalent, orally active, blood-brain-permeable GRPR selective antagonist with anti-inflammatory and neuroprotective effects. Aurantiamide reduces inflammation and oxidative stress in renal tissue by inhibiting GRPR-mediated renal necrosis pathways (such as RIPK3/MLKL signaling) and NF-κB inflammatory pathways, exerting anti-acute kidney injury and endothelial function activities. Aurantiamide also inhibits the M1 polarization of microglia and inhibits NLRP3 activation, thereby improving AD mouse models. Aurantiamide has in vivo inhibitory efficacy in acute kidney injury models such as ischemia/reperfusion, sepsis, and hypertension models.

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Aurantiamide Chemical Structure

Aurantiamide Chemical Structure

CAS No. : 58115-31-4

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Aurantiamide Related Antibodies

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Description

Aurantiamide is a non-covalent, orally active, blood-brain-permeable GRPR selective antagonist with anti-inflammatory and neuroprotective effects. Aurantiamide reduces inflammation and oxidative stress in renal tissue by inhibiting GRPR-mediated renal necrosis pathways (such as RIPK3/MLKL signaling) and NF-κB inflammatory pathways, exerting anti-acute kidney injury and endothelial function activities. Aurantiamide also inhibits the M1 polarization of microglia and inhibits NLRP3 activation, thereby improving AD mouse models. Aurantiamide has in vivo inhibitory efficacy in acute kidney injury models such as ischemia/reperfusion, sepsis, and hypertension models[1][2][3][4][5].

Cellular Effect
Cell Line Type Value Description References
N9 IC50
14.91 μM
Compound: 23
Antineuroinflammatory activity in mouse N9 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay
Antineuroinflammatory activity in mouse N9 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay
[PMID: 28073678]
In Vitro

Aurantiamide (25, 50, 100 μM; 12 h) significantly reduces the protein and mRNA expression of the renal injury marker KIM1 in the human renal proximal tubular epithelial cell (HK-2) hypoxia/reoxygenation and LPS (1 mg/mL) stimulation model, inhibits the phosphorylation of proteins related to the RIPK3/MLKL necrosis pathway and NF-κB inflammatory pathway, and alleviates cell damage and inflammatory response[1].
Aurantiamide (10, 20 μM; 24 h) inhibits LPS and IFN-γ-induced BV2 activation and M1 polarization in mouse BV2 cells, inhibited the activation of NLRP3, and thus exerted anti-CNS inflammatory activity[2].
Aurantiamide promotes M2 polarization of microglia and improves cognitive ability of Alzheimer's disease mice[3].
Aurantiamide (3 μM; 18 h) significantly upregulates the mRNA and protein expression of endothelial nitric oxide synthase (eNOS) in human umbilical vein endothelial cells (HUVECs), promotes the production of nitric oxide (NO), and has no significant toxic effect on cell viability[4].

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

Aurantiamide Related Antibodies

Western Blot Analysis[1]

Cell Line: Human proximal tubule epithelial cells (HK-2) [LPS-induced model]
Concentration: 25 μM, 50 μM, 100 μM
Incubation Time: 24 h
Result: WB (Western blot) : Reduced protein expression of renal injury marker KIM1, phosphorylated RIPK3 (p-RIPK3), phosphorylated MLKL (p-MLKL), and phosphorylated P65 (p-P65) in a dose-dependent manner, compared to H/R or LPS-stimulated controls.
qPCR : Downregulated mRNA levels of KIM1, MCP-1, and IL-6, with significant inhibition at 50 μM and 100 μM.
IF (Immunofluorescence) : Decreased immunofluorescent intensity of p-MLKL and KIM1 in cytoplasm, indicating reduced necroptosis and tubular injury.

Western Blot Analysis[4]

Cell Line: Human umbilical vein endothelial cells (HUVEC)
Concentration: 3 μM
Incubation Time: 18 h
Result: No significant cytotoxicity observed, with cell viability maintaining over 90% compared to control.
WB (Western blot) : Upregulated eNOS protein expression by 1.8-fold compared to control, with enhanced NO production detected by nitrite/nitrate assay.
\qPCR : Increased eNOS mRNA expression by 2.3-fold, confirming transcriptional activation of eNOS.
In Vivo

Aurantiamide (2.5, 5, 10 mg/kg; oral gavage; 3 times, 24 hours apart) improves cognitive impairment in C57BL/6 mice after ischemia/reperfusion (I/R) and cecal ligation and puncture (CLP) in a dose-dependent manner, and inhibits microglial polarization and NLRP3 activation[2].
Aurantiamide (0.5 mg/kg; intraperitoneal injection; once a day, 5 days a week; 4 weeks) significantly reduces mean arterial blood pressure, improves endothelium-dependent vasodilation, upregulates aortic endothelial nitric oxide synthase (eNOS) protein expression and promotes nitric oxide (NO) production in the two-kidney-one-clip (2K-1C) renovascular hypertension model in Sprague-Dawley rats[4].
The metabolic characteristics of Aurantiamide (0.1 mg/kg; oral gavage; single dose) and Aurantiamide acetate (HY-N2905) (0.2 mg/kg; oral gavage; single dose) in rats shows that they have the characteristics of rapid diffusion, wide distribution, and can pass through the blood-brain barrier, with a peak time of 0.5 h. In addition, the decline rate of aurantiamide acetate is faster than that of aurantiamide[5].

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

Animal Model: Male C57BL/6 mice (6-8 weeks old, 20-22 g) + cisplatin-induced, I/R, or CLP-induced acute kidney injury model[1]
Dosage: 2.5, 5, 10 mg/kg (dissolved in 0.5% carboxymethylcellulose + 0.1% Tween 80)
Administration: Oral gavage, three times before the surgery, with a 24 h interval between each administration
Result: Renal function : Reduced serum creatinine and BUN levels by 30-45% compared to model controls, with the 10 mg/kg dose showing the most pronounced effect.
Histopathology : PAS staining revealed decreased tubular dilation, glycogen deposition, and interstitial fibrosis; immunofluorescence showed reduced KIM1 (renal injury marker) and F4/80+ macrophage infiltration in renal tissues.
Protein expression : Western blot demonstrated dose-dependent inhibition of p-RIPK3, p-MLKL, and p-P65 (NF-κB) in renal lysates, with corresponding reduction in pro-inflammatory cytokines (IL-6, TNF-α) by qPCR.
Animal Model: Male Sprague-Dawley rats (8 weeks old, 230-250 g) + two-kidney one-clip (2K-1C) renovascular hypertension model[4]
Dosage: 0.5 mg/kg (dissolved in DMSO, final concentration 0.1%)
Administration: Intraperitoneal injection, once daily for 5 days/week, total 4 weeks
Result: Blood pressure : Reduced mean arterial pressure (MAP) by 20-25% compared to hypertensive controls, with significant improvement in endothelium-dependent relaxation to acetylcholine (ACh) and reduced constriction to phenylephrine (Phe).
Vascular function : Organ bath assays showed enhanced ACh-induced vasodilation and attenuated Phe-induced vasoconstriction in aortic rings, correlated with increased eNOS protein expression (1.5-fold by Western blot) and NO production (measured as nitrite/nitrate levels).
Red blood cell deformability : Ektacytometry revealed increased erythrocyte deformability (Elmax) in treated rats, indicating improved blood fluidity and microvascular flow.
Molecular Weight

402.49

Formula

C25H26N2O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N[C@H](CO)CC1=CC=CC=C1)[C@@H](NC(C2=CC=CC=C2)=O)CC3=CC=CC=C3
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (124.23 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 2.4845 mL 12.4227 mL 24.8453 mL
5 mM 0.4969 mL 2.4845 mL 4.9691 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.25 mg/mL (3.11 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 1.25 mg/mL (3.11 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4845 mL 12.4227 mL 24.8453 mL 62.1133 mL
5 mM 0.4969 mL 2.4845 mL 4.9691 mL 12.4227 mL
10 mM 0.2485 mL 1.2423 mL 2.4845 mL 6.2113 mL
15 mM 0.1656 mL 0.8282 mL 1.6564 mL 4.1409 mL
20 mM 0.1242 mL 0.6211 mL 1.2423 mL 3.1057 mL
25 mM 0.0994 mL 0.4969 mL 0.9938 mL 2.4845 mL
30 mM 0.0828 mL 0.4141 mL 0.8282 mL 2.0704 mL
40 mM 0.0621 mL 0.3106 mL 0.6211 mL 1.5528 mL
50 mM 0.0497 mL 0.2485 mL 0.4969 mL 1.2423 mL
60 mM 0.0414 mL 0.2070 mL 0.4141 mL 1.0352 mL
80 mM 0.0311 mL 0.1553 mL 0.3106 mL 0.7764 mL
100 mM 0.0248 mL 0.1242 mL 0.2485 mL 0.6211 mL
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Aurantiamide Related Classifications

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:

Aurantiamide58115-31-4Othersantioxidantantiplateletanti-inflammatoryantitumorInhibitorinhibitorinhibit

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