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GTPL5846

Cat. No. M9245
GTPL5846 Structure
Synonym:

6-OAU

Size Price Availability Quantity
5mg USD 270  USD270 In stock
10mg USD 400  USD400 In stock
50mg USD 1200  USD1200 In stock
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Quality Control & Documentation
Biological Activity

GTPL5846 (6-OAU) increased [35S]GTPγS incorporated in Sf9 cell membranes expressing human GPR84-Gαi fusion protein with an EC50 of 512 nM. Stimulation with 6.25 μm 6-OAU began to induce GPR84-EGFP internalization, and the extensive internalization was observed at 200 μm 6-OAU stimulation. In a Transwell assay, 3-OH-C12 and the surrogate agonist, GTPL5846 (6-OAU), provoked chemotaxis of PMNs prepared from human peripheral blood in a concentration-dependent manner with an EC50 of 24.2 μm and 318 nm, respectively.

In vivo, injection of GTPL5846 (6-OAU) suspension in 1% rat serum into the rat jugular vein (10 mg/kg) leads to the elevation of a chemokine, CXCL1 concentration in the serum peaking at 3 h after the injection. In the rat air pouch model, GTPL5846 (6-OAU) at 1 mg/ml dissolved in 0.3% BSA attracted both PMNs and macrophages into the air pouch, peaking at 4 h after GTPL5846 inoculation.

Chemical Information
Molecular Weight 239.31
Formula C12H21N3O2
CAS Number 83797-69-7
Solubility (25°C) DMSO > 1 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Suzuki M, et al. J Biol Chem. Medium-chain fatty acid-sensing receptor, GPR84, is a proinflammatory receptor.

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Keywords: GTPL5846, 6-OAU supplier, GPR/FFAR, inhibitors, activators


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