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Cat. No.: HY-103637

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Vimirogant

(Synonyms: VTP-43742)

1 Cited Publications

Customer Review

Based on 1 publication(s) in Google Scholar

Vimirogant (VTP-43742) is a potent, selective, and orally active RORγt inhibitor (K_i=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.

For research use only. We do not sell to patients.

CAS No.: 1802706-04-2
Formula: C₂₇H₃₅F₃N₄O₃S
Molecular Weight:552.65

Storage:

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

Data Sheet (268 KB)

Vimirogant Chemical Structure

CAS No.: 1802706-04-2

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

RORγt

3.5 nM (Ki)

RORγt

17 nM (IC₅₀)

All ROR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
PBMC	IC₅₀	21 nM 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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1802706-04-2
Molecular Weight 552.65
Formula C₂₇H₃₅F₃N₄O₃S
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
Synonyms

VTP-43742
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Publications (1)

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Journal Impact Factor

J Ethnopharmacol

Shaoyao decoction alleviates DSS-induced colitis by inhibiting IL-17a-mediated polarization of M1 macrophages. [Abstract]

2024 Oct 18:118941. PMID: 39427735

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (268 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Gege C. RORγt inhibitors as potential back-ups for the phase II candidate VTP-43742 from Vitae Pharmaceuticals: patent evaluation of WO2016061160 and US20160122345. Expert Opin Ther Pat. 2017;27(1):1-8. [Content Brief]

[2]. Gerard McGeehan, et al. VTP-43742 is a potent and selective RORγt blocker that demonstrates oral efficacy in a mouse model of autoimmunity through suppression of IL-17A production (THER7P.945). J Immunol May 1, 2015, 194 (1 Supplement) 208.5-208.5.

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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