1. Metabolic Enzyme/Protease
  2. Phosphatase
  3. Rosiptor

Rosiptor (Synonyms: AQX-1125)

Cat. No.: HY-109011 Purity: >98.0%
Handling Instructions

Rosiptor is an activator of SH2-containing inositol-5'-phosphatase 1 (SHIP1).

For research use only. We do not sell to patients.

Rosiptor Chemical Structure

Rosiptor Chemical Structure

CAS No. : 782487-28-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 770 In-stock
Estimated Time of Arrival: December 31
5 mg USD 700 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 3500 In-stock
Estimated Time of Arrival: December 31
100 mg USD 5500 In-stock
Estimated Time of Arrival: December 31
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500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

Rosiptor is an activator of SH2-containing inositol-5'-phosphatase 1 (SHIP1).

IC50 & Target

SHIP1[1]

In Vitro

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[1].

In Vivo

In female Sprague-Dawley rats, the single-dose pharmacokinetics of Rosiptor show that the increases in maximal plasma concentration (Cmax) and AUC0-∞ are dose-proportional at the lower end of the dosing regimen and greater than dose proportional at the higher doses. The oral bioavailability of Rosiptor in rats is 66 and 85% at 10 and 30 mg/kg respectively. Oral bioavailability of Rosiptor in dogs is 88 and 104% at 10 and 30 mg/kg respectively. High tissue concentrations of Rosiptor are detected, as compared to plasma concentrations, at each time point studied[1].

Clinical Trial
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 150 mg/mL (466.56 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1104 mL 15.5521 mL 31.1042 mL
5 mM 0.6221 mL 3.1104 mL 6.2208 mL
10 mM 0.3110 mL 1.5552 mL 3.1104 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

To study enzyme kinetics using either IP4 or diC8-PI(3,4,5)P3 (diC8-PIP3) as substrates, enzyme activity over time is measured in the absence or presence of Rosiptor and varying concentrations of IP4 or diC8-PIP3. Phosphate released at each substrate concentration is plotted against time, and initial velocities are determined and plotted against IP4 or diC8-PIP3 concentration[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

Bone marrow cells are obtained from 4- to 8-week-old SHIP1+/+ and SHIP1-/- mice and bone marrow-derived mast cells (BMMCs) are prepared. Mast cells are sensitized overnight with anti-DNP IgE (SPE-7). Cells are then washed and incubated in the presence of vehicle control (media only) or Rosiptor (60 μM) prior to stimulation with the indicated concentration of DNP-human serum albumin (DNP-HSA), followed by the measurement of β-hexosaminidase from the culture supernatant[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Female Sprague-Dawley rats and beagle dogs (male and female) are treated with Rosiptor in saline by bolus i.v. injection (at 1 mL/kg ) or by oral gavage (at 5 mL/kg). Blood is sampled 0 to 48 h post-dose and plasma isolated. Plasma concentrations of Rosiptor are quantified using a validated HPLC-MS/MS method. Pharmacokinetic parameters are determined by non-compartmental analysis[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

321.50

Formula

C₂₀H₃₅NO₂

CAS No.

782487-28-9

SMILES
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Rosiptor
Cat. No.:
HY-109011
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Rosiptor

Cat. No.: HY-109011