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S18-000003

Cat. No. M10170
S18-000003 Structure
Synonym:

S18000003

Size Price Availability Quantity
5mg USD 260  USD260 In stock
10mg USD 420  USD420 In stock
25mg USD 820  USD820 In stock
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Quality Control & Documentation
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.

Chemical Information
Molecular Weight 518.55
Formula C26H25F3N2O4S
CAS Number 2068119-11-7
Solubility (25°C) DMSO 100 mg/mL
Storage -20°C, sealed
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] Chihiro Imura, et al. J Dermatol Sci. A novel RORγt inhibitor is a potential therapeutic agent for the topical treatment of psoriasis with low risk of thymic aberrations

[2] Yoshikazu Sasaki, et al. Bioorg Med Chem Lett. Discovery of a potent orally bioavailable retinoic acid receptor-related orphan receptor-gamma-t (RORγt) inhibitor, S18-000003

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RORγ antagonist 1

RORγ antagonist 1, a potent betulinic acid derivative, is an antagonist of RORγ (KD=0.18 μM).

RORγt inverse agonist 31

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  Catalog
Abmole Inhibitor Catalog




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


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