AQX 1125

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AQX 1125 (Rosiptor) 是一种特异性口服生物可利用的 SHIP1 激活剂。

AQX 1125 (Rosiptor) is a specific, orally bioavailable SHIP1 activator with no effect on functional androgen, oestrogen, oestrogen-related receptor α, glucocorticoid, mineralocorticoid and progesterone receptor at 30 uM; inhibits the pAkt (S473) in MOLT-4 cells, and inhibits cytokine release in mixed splenocytes; significantly decreases β-hexosaminidase release in mouse BMMCs; inhibits chemotaxis in human mononuclear cells (EC50=0.26 uM); suppresses leukocyte accumulation and inflammatory mediator release in rodent models of pulmonary inflammation and allergy.COPD Phase 2 Clinical(In Vitro):Rosiptor (0.1-10 μM; 30 minutes) inhibits Akt activation in MOLT-4, but not in Jurkat cells.(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.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.

Rosiptor (0.1-10 μM; 30 minutes) inhibits Akt activation in MOLT-4, but not in Jurkat cells.Western Blot Analysis Cell Line:MOLT-4 cells and SHIP1-deficient Jurkat cells (IGF-1 stimulation) Concentration:0.1, 1, 10 μM Incubation Time:30 minutes Result:Induced a concentration-dependent decrease in Akt phosphorylation in MOLT-4 cells, while it failed to affect Akt phosphorylation in Jurkat cells.

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.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. Animal Model:6-8 weeks old male CD-1 miceDosage: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 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.

AQX-1125 | AQX1125 | Rosiptor

Metabolic Enzyme/Protease

Protein Phosphatase/PTP

Protein Phosphatase/PTP

Inflammation/Immunology

COPD

782487-28-9

321.505

C20H35NO2

>98% (HPLC)

DMSO : 150 mg/mL 466.56 mM

CC1(CCC(CC1CO)O)C2CCC3(C(C2CN)CCC3=C)C

(1S,3S,4R)-4-((3aS,4R,5S,7aS)-4-(aminomethyl)-7a-methyl-1-methyleneoctahydro-1H-inden-5-yl)-3-(hydroxymethyl)-4-methylcyclohexan-1-ol

(-20℃)

With Ice Pack

≥ 2 years