| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg | |||
| Other Sizes |
| Targets |
Rosiptor targets the phosphatase SHIP1. It is a selective activator of this enzyme, which plays a role in regulating inflammatory responses. By activating SHIP1, it inhibits Akt phosphorylation. This leads to a reduction in inflammatory mediator production and leukocyte chemotaxis. It shows no effect on other nuclear receptors like androgen, oestrogen, or glucocorticoid receptors at 30 μM.
|
|---|---|
| ln Vitro |
In MOLT-4 cells, but not in Jurkat cells, rosiptor (0.1–10 μM; 30 minutes) suppresses Akt activation [1].
In vitro, rosiptor inhibits Akt phosphorylation, inflammatory mediator production, and leukocyte chemotaxis. In MOLT-4 cells, rosiptor (0.1–10 μM; 30 minutes) suppresses Akt activation. It shows no effect on SHIP1-deficient Jurkat cells, confirming its target specificity. Its anti-inflammatory activity is confirmed in various cell-based assays. |
| 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].
In vivo, rosiptor has demonstrated significant anti-inflammatory effects. In mice exposed to NSC-125066, rosiptor (3–30 mg/kg; oral; given daily for 3 days) significantly decreased MPO activity and total BAL leukocytes. At a dose of 30 mg/kg, it reduced total BAL leukocytes by up to 60% on day 7 and up to 63% on day 21. Its oral bioavailability is >80%. It has been used in trials for COPD and atopic dermatitis. |
| Enzyme Assay |
Cell-free assays for rosiptor measure its ability to activate SHIP1 phosphatase activity. Its binding to SHIP1 can be assessed using surface plasmon resonance. Its molecular weight (321.505) and formula (C20H35NO2) are confirmed by mass spectrometry. Its purity (>98%) is confirmed by HPLC. Its density (1.1±0.1 g/cm3) is also determined.
|
| 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. Cellular assays for rosiptor measure its effect on Akt phosphorylation. In MOLT-4 cells, its ability to suppress Akt activation is assessed by Western blot analysis. Its effect on inflammatory mediator production and leukocyte chemotaxis is also measured. These assays confirm its functional activity as a SHIP1 activator. |
| 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)). In vivo animal experiments for rosiptor are conducted in mouse models. In mice exposed to NSC-125066, rosiptor (3–30 mg/kg; oral; daily for 3 days) significantly decreases MPO activity and total BAL leukocytes. Its pharmacokinetics are studied in male SD rats, where the Cmax is 0.830 μM and t1/2 is 5.2 hours. These studies confirm its in vivo efficacy and favorable pharmacokinetic profile. |
| ADME/Pharmacokinetics |
Rosiptor has a molecular weight of 321.505 and a molecular formula of C20H35NO2. It is an orally bioavailable compound with a bioavailability of >80%. In rats, the Cmax after oral administration (10 mg/kg) is 0.830 μM and the half-life is 5.2 hours. It has a density of 1.1±0.1 g/cm3. It is a white to off-white solid powder. It is soluble in organic solvents.
|
| Toxicity/Toxicokinetics |
The toxicological profile of rosiptor appears favorable based on clinical trials. Commonly reported side effects were mild and included headache and gastrointestinal disturbances. No significant safety concerns have been reported. Its safety has been evaluated in trials for interstitial cystitis and COPD.
|
| References |
|
| Additional Infomation |
AQX-1125 has been used in trials investigating the treatment of COPD, atopic dermatitis, interstitial cystitis, and bladder pain syndrome.
Rosiptor is an orally bioavailable and selective activator of the phosphatase SHIP1. It has potential anti-inflammatory activities and has been investigated for the treatment of interstitial cystitis, bladder pain syndrome, COPD, and atopic dermatitis. It is also known as AQX-1125. It is a research compound with promising anti-inflammatory properties. |
| Molecular Formula |
C20H35NO2
|
|---|---|
| Molecular Weight |
321.505
|
| Exact Mass |
321.266
|
| CAS # |
782487-28-9
|
| Related CAS # |
Rosiptor acetate;782487-29-0
|
| PubChem CID |
76965484
|
| Appearance |
White to off-white solid powder
|
| Density |
1.1±0.1 g/cm3
|
| Boiling Point |
451.6±45.0 °C at 760 mmHg
|
| Flash Point |
226.9±28.7 °C
|
| Vapour Pressure |
0.0±2.5 mmHg at 25°C
|
| Index of Refraction |
1.547
|
| LogP |
3.34
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
23
|
| Complexity |
465
|
| Defined Atom Stereocenter Count |
7
|
| 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
|
| InChi Key |
MDEJTPWQNNMAQF-BVMLLJBZSA-N
|
| 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
|
| 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
|
| Synonyms |
AQX-1125AQX1125AQX 1125
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~150 mg/mL (~466.56 mM)
|
|---|---|
| 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
