Vimirogant hydrobromide
Vimirogant hydrobromide (VTP-43742 hydrobromide) is a potent, selective, and orally active RORγt inhibitor with a Ki 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.
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- CAS 番号: 2115761-82-3
- 分子式: C27H37Br2F3N4O3S
- 分子量:714.48
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
[3]|
RORγt 3.5 nM (Ki) |
体外実験
Vimirogant hydrobromide (VTP-43742 hydrobromide) binds with high affinity to RORγt, with a Ki of 3.5 nM, and exhibits >1000-fold selectivity over RORα and RORβ[3].
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].
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. Further protocols information, click here.
体内実験
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].
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.
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Animal Model:C57BL/6N mice (male, 6-8 weeks old, 20 g, SPF grade)[5]
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Dosage:30 μg/kg
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Administration:i.g.; daily; 7 days
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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.
化学情報
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CAS 番号 2115761-82-3
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分子量 714.48
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分子式 C27H37Br2F3N4O3S
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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
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別名
VTP-43742 hydrobromide
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Dual Luciferin reporter gene assay
Luciferin reporter gene assay is a reporting system to detect the activity of Firefly Luciferase using luciferin as a substrate, which is often used in the research of miRNA target gene verification and promoter transcriptive activity regulation. Dual luciferase usually refers to Firefly luciferase and Renilla luciferase.
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Naïve CD4+ T-cell subset differentiation/polarization
Naïve CD4+ T-cell subset differentiation/polarization is an in vitro assay in which purified naïve CD4+ T cells are activated through TCR and CD28 costimulation and cultured with defined cytokines and neutralizing antibodies to generate Th0, Th1, Th2, Th17, or induced Treg-like populations. Differentiation is detected by subset-associated cytokines and transcription factors: IFN-γ/T-bet for Th1, IL-4/GATA3 for Th2, IL-17A/RORγt for Th17, and Foxp3 for induced Treg cells. The assay readout is usually generated by intracellular cytokine staining after restimulation, transcription-factor staining by flow cytometry, ELISA of secreted cytokines, or gene-expression analysis. The result reflects cytokine-directed lineage commitment or polarization rather than antigen-specific immune protection by itself.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
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iPSC cell differentiation
Induced pluripotent stem cells (iPSCs) are a type of cell that has similar properties to embryonic stem cells through somatic cell reprogramming.
純度とドキュメンテーション
参考文献
[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]
[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]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Vimirogant hydrobromide 関連分類
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