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Etrasimod (APD334)

Cat. No. M10226
Etrasimod (APD334) Structure
Synonym:

APD-334

Size Price Availability Quantity
5mg USD 355  USD355 In stock
10mg USD 550  USD550 In stock
25mg USD 1065  USD1065 In stock
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Quality Control
Biological Activity

Etrasimod (APD334) is a specific and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor, with IC50 of 1.88 nM in CHO cells. Etrasimod (APD334) induced effects on blood lymphopenia are determined in male Sprague-Dawley rats and male BALB/c mice.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 457.48
Formula C26H26F3NO3
CAS Number 1206123-37-6
Purity 98.94%
Solubility DMSO 25 mg/mL
Storage at -20°C
References

[1] Daniel J Buzard, et al. ACS Med Chem Lett. Discovery of APD334: Design of a Clinical Stage Functional Antagonist of the Sphingosine-1-phosphate-1 Receptor

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Keywords: Etrasimod (APD334), APD-334 supplier, S1P Receptor, inhibitors

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