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S18-000003

Cat. No. M10170
S18-000003 Structure
Synonym:

S18000003

Size Price Availability Quantity
5mg USD 333  USD370 In stock
10mg USD 558  USD620 In stock
25mg USD 1008  USD1120 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

S18-000003 is a potent, effective and orally active inhibitor of retinoic acid receptor-related orphan receptor-gamma-t (RORγt), with an IC50 of 29 nM. S18-000003 inhibits Th17 cells from naive CD4+T cells. S18-000003 inhibits IL-17 production in the skin of IL-23-treated mice in a dose-dependent manner.

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 518.55
Formula C26H25F3N2O4S
CAS Number 2068119-11-7
Purity >99%
Solubility DMSO 100 mg/mL
Storage -20°C, sealed
References

A novel RORγt inhibitor is a potential therapeutic agent for the topical treatment of psoriasis with low risk of thymic aberrations
Chihiro Imura, et al. J Dermatol Sci. 2019 Mar;93(3):176-185. PMID: 30905492.

Discovery of a potent orally bioavailable retinoic acid receptor-related orphan receptor-gamma-t (RORγt) inhibitor, S18-000003
Yoshikazu Sasaki, et al. Bioorg Med Chem Lett. 2018 Dec 1;28(22):3549-3553. PMID: 30301676.

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GSK805

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SR2211

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: S18-000003, S18000003 supplier, ROR, inhibitors

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