1. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  2. ROR
  3. Vimirogant

Vimirogant (VTP-43742) is a potent, selective, and orally active RORγt inhibitor (Ki=3.5 nM; IC50=17 nM). Vimirogant exhibits >1000-fold selectivity versus the RORα and RORβ isotypes. Vimirogant inhibits Th17 differentiation and IL-17A secretion from mouse splenocytes (IC50=57 nM) without affecting Th1, Th2, or Treg cell differentiation. Vimirogant has the potential for autoimmune disorders research.

The free form of the compound is prone to instability, it is advisable to consider the stable salt form (Vimirogant hydrochloride) that retains the same biological activity.

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Vimirogant

Vimirogant Estructura química

No. CAS : 1802706-04-2

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Descripciòn

Vimirogant (VTP-43742) is a potent, selective, and orally active RORγt inhibitor (Ki=3.5 nM; IC50=17 nM). Vimirogant exhibits >1000-fold selectivity versus the RORα and RORβ isotypes. Vimirogant inhibits Th17 differentiation and IL-17A secretion from mouse splenocytes (IC50=57 nM) without affecting Th1, Th2, or Treg cell differentiation. Vimirogant has the potential for autoimmune disorders research[1][2].

IC50 & Target[1]

RORγt

3.5 nM (Ki)

RORγt

17 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
PBMC IC50
21 1
Compound: 22; VTP-43742, AGN 242428
Inhibition of IL-17A secretion in human PBMC cells
Inhibition of IL-17A secretion in human PBMC cells
[PMID: 30010338]
PBMC IC50
21 1
Compound: 22; VTP-43742, AGN 242428
Inhibition of IL-17A secretion in human PBMC cells
Inhibition of IL-17A secretion in human PBMC cells
[PMID: 30010338]
In Vitro

Vimirogant inhibits the secretion of IL-17A from activated hPBMCs (IC50=18 nM) and human whole blood (IC50=192 nM)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In the MOG35-55/CFA immunized mouse EAE model, Vimirogant (p.o.) significantly suppresses clinical symptoms, demyelination and mRNA expression of multiple inflammatory markers in the spinal cord[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Ensayo clínico
Peso molecular

552.65

Fòrmula

C27H35F3N4O3S

No. CAS
SMILES

O=C(C1=CN=C([C@H](C(C)C)N(C[C@H]2CC[C@H](C(F)(F)F)CC2)C3)C3=C1)NCC4=NC=C(S(=O)(CC)=O)C=C4

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureza y Documentación
Referencias
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

Nombre del producto:
Vimirogant
Cat. No.:
HY-103637
Cantidad:
MCE Japan Authorized Agent: