| Identification | Back Directory | [Name]
semaglutide | [CAS]
782487-28-9 | [Synonyms]
AQX10
Rosiptor
semaglutide API
Rosiptor(AQX-1125)
AQX 1125
(AQX-1125
Semaglutide-fermented
semaglutide USP/EP/BP
AQX-1125;AQX1125;ROSIPTOR
Cyclohexanemethanol, 2-[(3aS,4R,5S,7aS)-4-(aminomethyl)octahydro-7a-methyl-1-methylene-1H-inden-5-yl]-5-hydroxy-2-methyl-, (1S,2R,5S)- | [EINECS(EC#)]
200-001-8 | [Molecular Formula]
C20H35NO2 | [MDL Number]
MFCD31619271 | [MOL File]
782487-28-9.mol | [Molecular Weight]
321.5 |
| Chemical Properties | Back Directory | [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) | [form ]
Solid | [pka]
15.05±0.10(Predicted) | [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 |
| Hazard Information | Back Directory | [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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