Rosiptor
Rosiptor Basic information
- Product Name:
- Rosiptor
- Synonyms:
-
- AQX10
- Rosiptor
- AQX-1125;AQX1125;ROSIPTOR
- Rosiptor(AQX-1125)
- AQX 1125 (AQX-1125
- semaglutide API
- Cyclohexanemethanol, 2-[(3aS,4R,5S,7aS)-4-(aminomethyl)octahydro-7a-methyl-1-methylene-1H-inden-5-yl]-5-hydroxy-2-methyl-, (1S,2R,5S)-
- Semaglutide-fermented
- CAS:
- 782487-28-9
- MF:
- C20H35NO2
- MW:
- 321.5
- EINECS:
- 200-001-8
- Product Categories:
-
- APIs
- 782487-28-9
- Mol File:
- 782487-28-9.mol
Rosiptor Chemical Properties
- Boiling point:
- 451.6±45.0 °C(Predicted)
- Density
- 1.07±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 150 mg/mL (466.56 mM)
- pka
- 15.05±0.10(Predicted)
- form
- Solid
- color
- White to off-white
- InChI
- 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
- InChIKey
- MDEJTPWQNNMAQF-BVMLLJBZSA-N
- SMILES
- [C@H]1(CO)C[C@@H](O)CC[C@@]1([C@H]1CC[C@@]2(C)[C@]([H])([C@@H]1CN)CCC2=C)C
Rosiptor Usage And Synthesis
Description
Rosiptor (AQX-1125) is a selective and orally active phosphatase SHIP1 activator with anti-inflammatory effects. It inhibits Akt phosphorylation, inflammatory mediator production and leukocyte chemotaxis in vitro.
Uses
Rosiptor has been used in trials studying the treatment of COPD, Atopic Dermatitis, Interstitial Cystitis, and Bladder Pain Syndrome.
Biological Activity
Rosiptor is a small-molecule SHIP1 activator.The activating effect of Rosiptor on SHIP1 is 28% at 100 μM in the native enzyme but no effect of Rosiptor is observed when the SHIP1δC2 enzyme is used. Rosiptor induces a concentration-dependent decrease in Akt phosphorylation in MOLT-4 cells, while it fails to affect Akt phosphorylation in Jurkat cells. At 0.1 μM Rosiptor the inhibition amounts to an average of 34%, while at 10 μM the inhibition amounts to an average of 82% in two independent experiments. Rosiptor also induces a concentration-dependent decrease in the production of multiple pro-inflammatory mediators in this system, without affecting cell viability. Rosiptor dose dependently inhibits chemotaxis of most cell types at low micromolar concentrations independent of the chemotactic stimulus.
in vivo
Rosiptor (3-30 mg/kg; p.o.; daily for 3 days) significantly reduces the total number of BAL leukocytes in NSC-125066-challenged mice and reduces MPO activity[2].
Rosiptor (10 mg/kg; p.o.) has the Cmax value of 0.830 μM and the t1/2 value of 5.2 hours. AQX-1125 also exhibits >80% oral bioavailability[1].
| Animal Model: | 6-8 weeks old male CD-1 mice[1] |
| Dosage: | 3, 10, 30 mg/kg |
| Administration: | p.o.; daily for 3 days |
| Result: | Significantly reduced the total number of BAL leukocytes in NSC-125066-challenged mice, up to a maximum of 60% at 7 days and 63% at 21 days at 30 mg/kg; Reduced MPO activity by 54% at Day 7 and by 74% at Day 21 at 30 mg/kg. |
| Animal Model: | Male Sprague-Dawley rats[1] |
| Dosage: | 10 mg/kg (Pharmacokinetic Study) |
| Administration: | Oral administration |
| Result: | The Cmax value is 0.830 μM and the t1/2 value is 5.2 hours. |
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