| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Targets |
Binds to and inhibits the mitochondrial ADP/ATP carrier (ANT). Induces opening of the mitochondrial permeability transition pore (mPTP) . [1]
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| ln Vitro |
Atractyloside A (7.5, 10, 15 µM) treatment for 10 minutes induced dose-dependent swelling and damage (disorganized cristae, broken membranes) in the mitochondria of rat arteriolar smooth muscle cells (ASMCs) as observed by transmission electron microscopy.
Atractyloside A (10, 15 µM) treatment for 10 minutes significantly increased the percentage of ASMCs with low mitochondrial membrane potential (depolarization) to 59.77% and 66.56%, respectively, compared to control, as measured by JC-1 staining and flow cytometry. Atractyloside A (7.5, 10, 15 µM) treatment for 10 minutes significantly reduced relative ATP content in ASMCs to 48%, 63%, and 66% of control, respectively, as measured by a luciferase-based assay. Atractyloside A (10, 15 µM) treatment for 10 minutes significantly reduced plasma membrane potential (hyperpolarization) by 33.68% and 34.58% from baseline, respectively, as measured by DiBAC4(3) staining and confocal microscopy. Atractyloside A (10, 15 µM) treatment for 10 minutes significantly weakened the contractile responsiveness of ASMCs to norepinephrine (1 µM), reducing cell area change to 30.85% and 29.69%, respectively, compared to ~46% in controls. [1] |
| Cell Assay |
Mitochondrial Ultrastructure Analysis: Arteriolar smooth muscle cells (ASMCs) isolated from rat mesenteric arterioles are treated with Atractyloside A (0, 7.5, 10, 15 µM) for 10 or 30 minutes. Cells are then fixed in glutaraldehyde, post-fixed in osmium tetroxide, dehydrated, embedded in resin, sectioned, stained with uranyl acetate and lead citrate, and examined by transmission electron microscopy for mitochondrial morphology changes.
Mitochondrial Membrane Potential (ΔΨm) Assay: ASMCs treated with Atractyloside A are loaded with JC-1 fluorescent dye for 15 minutes. After washing, cells are analyzed by flow cytometry. The percentage of cells with green fluorescence (indicating low ΔΨm/depolarization) is quantified. Cellular ATP Level Assay: ASMCs treated with Atractyloside A are lysed, and ATP levels are determined using a luciferase-based luminescence assay in a microplate reader, with luminescence intensity proportional to ATP concentration. Plasma Membrane Potential Assay: ASMCs are pre-loaded with the potential-sensitive dye DiBAC4(3). After treatment with Atractyloside A, cells are imaged using a confocal laser scanning microscope. Fluorescence intensity is quantified, with a decrease indicating membrane hyperpolarization. Cell Contractile Reaction Assay: Phase-contrast images of ASMCs are captured before and after stimulation with norepinephrine (1 µM). The change in cell area (contraction) is quantified using image analysis software, and the percentage area change is calculated. [1] |
| Animal Protocol |
Wistar rats (180-220 g) are euthanized, and mesenteric arterioles (second A2 branch) are obtained from the small intestine mesentery. The arterioles are cut into segments. Arteriolar smooth muscle cells (ASMCs) are dissociated by incubating the segments with papain and collagenase solutions. The cell suspension is stored at 4°C and allowed to settle at room temperature before being used for in vitro experiments. [1]
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| Toxicity/Toxicokinetics |
This study showed that atractylodesin A has cytotoxic effects on small arterial smooth muscle cells, inducing mitochondrial damage, ATP depletion, and impaired contractile function, which is considered to be one of the mechanisms of hypotension observed in poisoning cases. However, the study did not provide specific toxicity parameters, such as LD₅₀, organ toxicity characteristics, or plasma protein binding rate. [1]
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| References | |
| Additional Infomation |
Atractylodes A is a terpenoid glycoside. It has been reported to exist in Atractylodes japonica, Atractylodes lancea, and Atractylodes macrocephala, with supporting data. Atractylodes A is a natural compound found in various plant genera and is a known cause of herbal and food poisoning (often fatal). Its primary mechanism of action is binding to the mitochondrial ADP/ATP carrier (ANT), inhibiting ATP/ADP exchange and inducing the opening of the mitochondrial permeability transition pore (mPTP). In ASMCs, this leads to mitochondrial damage, depolarization, swelling, ATP depletion, and plasma membrane hyperpolarization (possibly due to K-ATP channel activation caused by low ATP levels), ultimately resulting in reduced calcium ion influx and a weakened contractile response to vasoconstrictors such as norepinephrine.
In vitro experiments have shown that mitochondrial dysfunction in vascular smooth muscle may be a key mechanism of hypotension associated with atrazine A poisoning. [1] |
| Molecular Formula |
C21H36O10
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|---|---|
| Molecular Weight |
448.50454
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| Exact Mass |
448.23
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| CAS # |
126054-77-1
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| PubChem CID |
71307451
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| Appearance |
White to light yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
684.8±55.0 °C at 760 mmHg
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| Flash Point |
234.1±25.0 °C
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| Vapour Pressure |
0.0±4.8 mmHg at 25°C
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| Index of Refraction |
1.600
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| LogP |
-3.63
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
31
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| Complexity |
671
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| Defined Atom Stereocenter Count |
10
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| SMILES |
C[C@@]1([C@@H]2C[C@@H](CC[C@@]([C@H]2CC1=O)(CO)O)C(C)(C)O[C@H]3[C@@H]([C@H]([C@@H]([C@H](O3)CO)O)O)O)O
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| InChi Key |
QNBLVYVBWDIWDM-BSLJOXIBSA-N
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| InChi Code |
InChI=1S/C21H36O10/c1-19(2,31-18-17(27)16(26)15(25)13(8-22)30-18)10-4-5-21(29,9-23)12-7-14(24)20(3,28)11(12)6-10/h10-13,15-18,22-23,25-29H,4-9H2,1-3H3/t10-,11-,12+,13-,15-,16+,17-,18+,20+,21+/m1/s1
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| Chemical Name |
(3S,3aR,5R,8R,8aS)-3,8-dihydroxy-8-(hydroxymethyl)-3-methyl-5-[2-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxypropan-2-yl]-3a,4,5,6,7,8a-hexahydro-1H-azulen-2-one
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~111.48 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.64 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.64 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 20.8 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.64 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2297 mL | 11.1483 mL | 22.2965 mL | |
| 5 mM | 0.4459 mL | 2.2297 mL | 4.4593 mL | |
| 10 mM | 0.2230 mL | 1.1148 mL | 2.2297 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.
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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