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| ln Vitro |
AQX-016A (5 μg/mL, 30 minutes) decreases intracellular PIP3 levels via activating 5' phosphatase and prevents the PI3K-mediated increase in PIP3 levels [1]. In a SHIP-dependent way, AQX-01 6A (0–5 μg/mL, 30 minutes) prevents PKB phosphorylation caused by LPS [1]. At 1 and 5 μg/mL doses, AQX-016A (0-5 μg/mL, 2 hours) effectively suppresses TNFa in J774 and peritoneal macrophages [1]. For BMDM, AQX-016A (0–6 μg/mL, 30 minutes) needs SHIP to maximally suppress TNFa production. It also specifically inhibits TNF production in SHIP1+/+ macrophages, but not in SHIP1–/– macrophages [1].. TNFa translation is inhibited by AQX-016A (0–5 μg/mL, 0-90 minutes) [1]. AQX-016A (0–15 μM, 30 minutes) suppresses mast cell and macrophage activation while increasing SHIP1 enzyme activity in intact cells and in vitro [2]. In a manner that is dependent on SHIP, AQX-016A (15 μM, 30 minutes) decreases mast cell and PI3K-dependent macrophage responses while also inhibiting immune cell activation [2].
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| ln Vivo |
In a mouse model of endotoxemia, AQX-016A (20 mg/kg, orally, once) significantly reduces plasma TNFa levels and reduces inflammation [1][2].
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| Cell Assay |
Western blot analysis
Cell Types: SHIP1+/+ and SHIP1-/- mast cells [2] Tested Concentrations: 0, 3, 6, 15, 30 μM Incubation Duration: 30 minutes Experimental Results: PIP3-regulated intracellular signaling in SHIP-expressing cells Induction events were inhibited in hematopoietic cells, but not in SHIP-deficient hematopoietic or non-hematopoietic cells. Preferentially inhibits LPS-stimulated PKB phosphorylation in SHIP1+/+ but not SHIP1-/- macrophages in a dose-dependent manner, and inhibits the phosphorylation of PKB, p38MAPK, and extracellular signal-regulated kinase (ERK) in SHIP1+/+ , but not in SHIP1-/- mast cells. |
| References |
[1]. Yau, Tien Yin. Novel strategies for antagonizing the phosphatidylinositol-3-kinase pathway in disease. University of British Columbia. 2010.
[2]. Ong CJ, et al. Small-molecule agonists of SHIP1 inhibit the phosphoinositide 3-kinase pathway in hematopoietic cells. Blood. 2007 Sep 15;110(6):1942-9. |
| Molecular Formula |
C22H32O2
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|---|---|
| Molecular Weight |
328.496
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| CAS # |
849669-54-1
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| SMILES |
OC1=C(C=C(C)C2=C1C[C@H]1[C@@]2(C)CCC2C(C)(C)CCC[C@]12C)O
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| Chemical Name |
(6aR,11aR,11bS)-4,4,6a,7,11b-pentamethyl-1,2,3,4a,5,6,11,11a-octahydrobenzo[a]fluorene-9,10-diol
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| Synonyms |
NSC 741764 NSC-741764 NSC741764AQX 016A AQX-016A AQX016A
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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 Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0441 mL | 15.2207 mL | 30.4414 mL | |
| 5 mM | 0.6088 mL | 3.0441 mL | 6.0883 mL | |
| 10 mM | 0.3044 mL | 1.5221 mL | 3.0441 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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