Aaptamine |
Catalog No.GC41327
One-Click Copy Product Info
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해면 Aaptos aaptos에서 분리된 해면 알칼로이드인 Aaptamine은 α-adrenoceptor의 경쟁적 길항제로 p53과 독립적으로 p21 프로모터를 활성화합니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 85547-22-4
Sample solution is provided at 25 µL, 10mM.
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Aaptamine is a marine sponge alkaloid originally isolated from A. aaptos with diverse biological activities, including antiproliferative and antidepressant properties. It is an agonist of δ- and μ-opioid receptors (EC50s = 5.1 and 10.1 μM, respectively, in HEK293 cells expressing human recombinant receptors) and a competitive antagonist of α-adrenergic receptors (α-ARs; pA2s = 4.88 and 5.43, respectively, in isolated rabbit aorta and renal artery). Aaptamine inhibits growth of HeLa cervical cancer (IC50 = 15 μg/ml) and K562 leukemia (GI50 = 10 μM) cells and induces cell cycle arrest in the G2/M phase in K562 leukemia and MG63 osteosarcoma cells. It is a proteasome inhibitor that inhibits chymotrypsin-, caspase-, and trypsin-like activity in a partially purified rat liver proteasome preparation (IC50s = 1.6, 2.7, and 18 μg/ml, respectively) and dose-dependently activates p21 independent of p53 in MG63 cells when used at concentrations ranging from 20 to 50 μM. Aaptamine (40 mg/kg, i.p.) decreases immobility time in the forced swim test in mice, indicating antidepressant-like activity.
| Cas No. | 85547-22-4 | SDF | |
| Canonical SMILES | COC1=C(OC)C=C2C3=C1NC=CC3=NC=C2 | ||
| Formula | C13H12N2O2 | M.Wt | 228.3 |
| Solubility | DMSO : 100 mg/mL (438.12 mM; Need ultrasonic) | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.3802 mL | 21.901 mL | 43.802 mL |
| 5 mM | 876 μL | 4.3802 mL | 8.7604 mL |
| 10 mM | 438 μL | 2.1901 mL | 4.3802 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)