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IL-17A inhibitor 1

Cat. No. M22522
IL-17A inhibitor 1 Structure
Synonym:

LY3509754

Size Price Availability Quantity
1mg USD 630  USD630 In stock
2mg USD 1090  USD1090 In stock
5mg USD 1520  USD1520 In stock
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Quality Control & Documentation
Biological Activity

IL-17A inhibitor 1 is a IL-17A inhibitor, with IC50 values of <9.45 nM and 9.3 nM in alphalisa assay and HT-29 cells.

Chemical Information
Molecular Weight 586.51
Formula C24H27F5N8O4
CAS Number 2452464-73-0
Solubility (25°C) DMSO ≥ 150 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] Zara Ali, et al. Expert Rev Clin Immunol. Bimekizumab: a dual IL-17A and IL-17F inhibitor for the treatment of psoriasis and psoriatic arthritis

[2] Chao Liu, et al. J Immunother Cancer. Blocking IL-17A enhances tumor response to anti-PD-1 immunotherapy in microsatellite stable colorectal cancer

[3] Sergiy Sukhanov, et al. Cell Signal. The SGLT2 inhibitor Empagliflozin attenuates interleukin-17A-induced human aortic smooth muscle cell proliferation and migration by targeting TRAF3IP2/ROS/NLRP3/Caspase-1-dependent IL-1β and IL-18 secretion

[4] James G Krueger, et al. J Allergy Clin Immunol. IL-17A inhibition by secukinumab induces early clinical, histopathologic, and molecular resolution of psoriasis

[5] Pierre Miossec, et al. Nat Rev Drug Discov. Targeting IL-17 and TH17 cells in chronic inflammation

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Keywords: IL-17A inhibitor 1, LY3509754 supplier, IL Receptor/Related, inhibitors, activators


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