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Cat. No.: HY-103637B

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Vimirogant hydrobromide

Name: Vimirogant hydrobromide
Brand: MedChemExpress
SKU: HY-103637B
Availability: PreOrder

(Synonyms: VTP-43742 hydrobromide)

Vimirogant hydrobromide (VTP-43742 hydrobromide) is a potent, selective, and orally active RORγt inhibitor with a K_i of 3.5 nM for binding to RORγt. VTP-43742 blocks Th17 cell differentiation and reduces IL-17A production by inhibiting RORγt-mediated transcriptional activity, thereby suppressing the RORγt/Th17/IL-17 inflammatory axis. VTP-43742 can be used for research on autoimmune diseases and inflammation-related diseases.

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

CAS No.: 2115761-82-3
Formula: C₂₇H₃₇Br₂F₃N₄O₃S
Molecular Weight:714.48

Storage:

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

Vimirogant hydrobromide Chemical Structure

CAS No.: 2115761-82-3

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Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
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Bioz

Biological Activity

Description

IC₅₀ & Target

^[3]

RORγt

3.5 nM (Ki)

All ROR Isoforms :

All Interleukin Related Isoforms :

In Vitro

OthersAdaptive ImmunityCytokines and Chemokines

Others

Vimirogant hydrobromide (VTP-43742 hydrobromide) binds with high affinity to RORγt, with a K_i of 3.5 nM, and exhibits >1000-fold selectivity over RORα and RORβ^[3].

Adaptive Immunity

Cytokines and Chemokines

Vimirogant hydrobromide inhibits Th17 differentiation and IL-17A secretion in mouse splenocytes with an IC₅₀ of 57 nM, without affecting Th1, Th2, or Treg cell differentiation^[3].

Cytokines and Chemokines

Vimirogant hydrobromide inhibits IL-17A secretion in activated hPBMCs with an IC₅₀ of 18 nM^[3].
Vimirogant hydrobromide inhibits IL-17A secretion in whole blood from healthy and psoriasis donors with an IC₅₀ of 192 nM^[3].

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

In Vivo

OthersAdaptive ImmunityCytokines and ChemokinesInnate Immunity

Others

Vimirogant (p.o.) hydrobromide (VTP-43742 hydrobromide) significantly inhibits clinical symptoms, demyelination, and mRNA expression of multiple inflammatory markers in the spinal cord of MOG35-55/CFA-immunized EAE mice^[3].

Adaptive Immunity

Cytokines and Chemokines

Vimirogant (prophylactic administration; 11 days) hydrobromide dose-dependently inhibits CD4⁺IL-17⁺IFNγ⁻ and CD4⁺IL-17⁺IFNγ⁺ T cells in the spleen and draining lymph nodes of MOG35-55/CFA-immunized EAE mice; following ex vivo restimulation of splenocytes obtained from treated mice with MOG35-55, Th17-derived cytokines are specifically suppressed^[4].
Vimirogant (high dose; prophylactic administration) hydrobromide completely suppresses EAE clinical scores in chronic EAE studies, with a greater degree of suppression than MM17F3; it also inhibits Th17-related markers in the spinal cord and reduces demyelination and inflammatory cell infiltration^[4].

Innate Immunity

Vimirogant (30 μg/kg; p.o.; 7 days) hydrobromide reduces M1 macrophage polarization in the colonic mucosa of DSS-induced colitis mice and alleviates colitis-associated inflammatory injury; the main text states that IL-17a expression does not change under this condition^[5].
Vimirogant (30 μg/kg; intragastric administration; 7 days; combined with SYD 2.50 g/kg) hydrobromide inhibits colonic mucosal inflammatory injury in DSS-induced colitis mice more strongly than SYD alone^[5].

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

Animal Model:

C57BL/6N mice (male, 6-8 weeks old, 20 g, SPF grade)^[5]
Dosage:

30 μg/kg
Administration:

i.g.; daily; 7 days
Result:

Considerably decreased M1 macrophage polarization in the colonic mucosa.
Produced milder colonic inflammatory lesions and lower sensitivity to DSS-induced colitis.
Did not alter IL-17a expression according to the article text.

Related Protocols :

Chemical Information

CAS No. 2115761-82-3
Molecular Weight 714.48
Formula C₂₇H₃₇Br₂F₃N₄O₃S
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.Br.Br
Synonyms

VTP-43742 hydrobromide
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Gege C, et al. Retinoid-related orphan receptor gamma t (RORγt) inhibitors from Vitae Pharmaceuticals (WO2015116904) and structure proposal for their Phase I candidate VTP-43742. Expert opinion on therapeutic patents. 2016 Jun;26(6):737-44.

[2]. Gege C, et al. RORγt inhibitors as potential back-ups for the phase II candidate VTP-43742 from Vitae Pharmaceuticals: patent evaluation of WO2016061160 and US20160122345. Expert opinion on therapeutic patents. 2017 Jan;27(1):1-8. [Content Brief]

[3]. McGeehan G, 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. 2015;194(1 Suppl):208.5.

[4]. Zhao Y, et al. The potent, selective RORγt blocker, VTP-43742, suppresses Th17 production in vivo and provides greater benefit than IL-17 blockade in the EAE model of autoimmunity (THER3P.968). J Immunol. 2015;194(1 Suppl):68.1.

[5]. Wang S, et al. Shaoyao decoction alleviates DSS-induced colitis by inhibiting IL-17a-mediated polarization of M1 macrophages. Journal of ethnopharmacology. 2025 Jan 30;337(Pt 3):118941. [Content Brief]

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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.

Bioz

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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Vimirogant hydrobromide

All ROR Isoforms

All Interleukin Related Isoforms