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| 10mg |
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| 25mg |
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Rosiptor (AQX-1125; AQX1125; AQX 1125) is an orally bioavailable and selective activator of the phosphatase SHIP1 (SH2 domain-containing inositol-5′-phosphatase 1) with potential anti-inflammatory activities. It inhibits Akt phosphorylation, inflammatory mediator production and leukocyte chemotaxis in vitro.
| ln Vitro |
In MOLT-4 cells, but not in Jurkat cells, rosiptor (0.1–10 μM; 30 minutes) suppresses Akt activation [1].
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|---|---|
| ln Vivo |
In mice exposed with NSC-125066, rosiptor (3–30 mg/kg; oral; given daily for 3 days) significantly decreased MPO activity and total BAL leukocytes [2]. The Cmax and t1/2 values of rosiptor (10 mg/kg; po) are 0.830 μM and 5.2 hours, respectively. Additionally, AQX-1125 has an oral bioavailability of >80% [1].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: MOLT-4 cells and SHIP1-deficient Jurkat cells (IGF-1 stimulation) Tested Concentrations: 0.1, 1, 10 μM Incubation Duration: 30 minutes Experimental Results: Induced Akt phosphorylation concentration-dependent reduction in MOLT- 4 cells, whereas it failed to affect Akt phosphorylation in Jurkat cells. |
| Animal Protocol |
Animal/Disease Models: 6-8 weeks old male CD-1 mice [1]
Doses: 3, 10, 30 mg/kg Route of Administration: po; one time/day for 3 days Experimental Results: NSC-125066 challenged BAL leukocytes of mice The total number was Dramatically diminished, at a dose of 30 mg/kg, by up to 60% on day 7, and by up to 63% on day 21; at a dose of 30 mg/kg, MPO activity was diminished by 54% on day 7, and on day 21 Days dropped by 74%. Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat[1] Doses: 10 mg/kg (pharmacokinetic/PK/PK study) Route of Administration: Oral Experimental Results:Cmax value is 0.830 μM, t1/2 value is 5.2 hrs (hrs (hours)). |
| References |
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| Additional Infomation |
AQX-1125 has been used in trials studying the treatment of COPD, Atopic Dermatitis, Interstitial Cystitis, and Bladder Pain Syndrome.
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| Molecular Formula |
C20H35NO2
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|---|---|
| Molecular Weight |
321.505
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| Exact Mass |
321.266
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| CAS # |
782487-28-9
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| Related CAS # |
Rosiptor acetate;782487-29-0
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| PubChem CID |
76965484
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
451.6±45.0 °C at 760 mmHg
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| Flash Point |
226.9±28.7 °C
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| Vapour Pressure |
0.0±2.5 mmHg at 25°C
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| Index of Refraction |
1.547
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| LogP |
3.34
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
465
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| Defined Atom Stereocenter Count |
7
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| SMILES |
C[C@@]1(CC[C@@H](C[C@@H]1CO)O)[C@H]2CC[C@]3([C@H]([C@@H]2CN)CCC3=C)C
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| InChi Key |
MDEJTPWQNNMAQF-BVMLLJBZSA-N
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| InChi Code |
InChI=1S/C20H35NO2/c1-13-4-5-17-16(11-21)18(7-9-19(13,17)2)20(3)8-6-15(23)10-14(20)12-22/h14-18,22-23H,1,4-12,21H2,2-3H3/t14-,15+,16+,17+,18+,19-,20+/m1/s1
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| Chemical Name |
(1S,3S,4R)-4-[(3aS,4R,5S,7aS)-4-(aminomethyl)-7a-methyl-1-methylidene-3,3a,4,5,6,7-hexahydro-2H-inden-5-yl]-3-(hydroxymethyl)-4-methylcyclohexan-1-ol
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| Synonyms |
AQX-1125AQX1125AQX 1125
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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 : ~150 mg/mL (~466.56 mM)
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1103 mL | 15.5516 mL | 31.1032 mL | |
| 5 mM | 0.6221 mL | 3.1103 mL | 6.2206 mL | |
| 10 mM | 0.3110 mL | 1.5552 mL | 3.1103 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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