TRBV1 Inhibitors
TRPV1 inhibitors represent a class of chemical compounds that specifically target the transient receptor potential vanilloid 1 (TRPV1) ion channel. TRPV1 is a non-selective cation channel that is primarily activated by various physical and chemical stimuli such as heat, capsaicin (the active component of chili peppers), and acidic environments. Structurally, the TRPV1 channel consists of six transmembrane domains with a pore-forming region between the fifth and sixth domains, typical of the TRP channel family. Inhibitors of TRPV1 interact with specific binding sites on the channel to modulate its activity, often blocking its ability to allow the influx of calcium and sodium ions. These inhibitors are highly sought after for their role in understanding the ion channel's functions, including its role in signal transduction pathways related to sensory perception, particularly in response to thermal and chemical stimuli.
From a chemical perspective, TRPV1 inhibitors are structurally diverse and encompass a range of organic molecules. Some inhibitors are small-molecule compounds that can competitively bind to the capsaicin binding site, while others may bind allosterically, thereby preventing channel activation without directly competing with endogenous ligands. The development of TRPV1 inhibitors requires a detailed understanding of the channel's conformational states, as these compounds may stabilize inactive states of the channel. The study of these inhibitors extends to the investigation of how changes in the molecular structure of the inhibitors impact their specificity and efficacy, and how these compounds affect the biophysical properties of TRPV1, including gating mechanisms, ion selectivity, and channel kinetics. Furthermore, research into TRPV1 inhibitors contributes to broader inquiries into TRP channel pharmacology and electrophysiology, as TRPV1 is part of a larger family of receptors that play pivotal roles in cellular signal transduction.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Cyclosporin A | 59865-13-3 | sc-3503 sc-3503-CW sc-3503A sc-3503B sc-3503C sc-3503D | 100 mg 100 mg 500 mg 10 g 25 g 100 g | $62.00 $90.00 $299.00 $475.00 $1015.00 $2099.00 | 69 | |
Cyclosporine inhibits TRBV1 expression by modulating T cell activation and the production of cytokines, ultimately leading to the downregulation of the protein. | ||||||
Dasatinib | 302962-49-8 | sc-358114 sc-358114A | 25 mg 1 g | $47.00 $145.00 | 51 | |
Dasatinib inhibits TRBV1 expression by targeting Src family kinases, which are involved in T cell receptor signaling pathways, thus reducing the activation and subsequent expression of TRBV1. | ||||||
Ibrutinib | 936563-96-1 | sc-483194 | 10 mg | $153.00 | 5 | |
Ibrutinib inhibits TRBV1 expression by irreversibly inhibiting Bruton's tyrosine kinase (BTK), a key enzyme involved in B-cell receptor signaling, thereby affecting downstream T cell activation and the expression of TRBV1. | ||||||
Mycophenolic acid | 24280-93-1 | sc-200110 sc-200110A | 100 mg 500 mg | $68.00 $261.00 | 8 | |
Mycophenolate inhibits TRBV1 expression by blocking the de novo synthesis of guanosine nucleotides, leading to the inhibition of T cell proliferation and the subsequent downregulation of TRBV1 expression. | ||||||
Rapamycin | 53123-88-9 | sc-3504 sc-3504A sc-3504B | 1 mg 5 mg 25 mg | $62.00 $155.00 $320.00 | 233 | |
Rapamycin inhibits TRBV1 expression by forming a complex with FKBP12, leading to the inhibition of mTOR complex 1 (mTORC1) and subsequently suppressing T cell activation and the expression of TRBV1. | ||||||
Vismodegib | 879085-55-9 | sc-396759 sc-396759A | 10 mg 25 mg | $80.00 $96.00 | 1 | |
Vismodegib inhibits TRBV1 expression by targeting the Hedgehog signaling pathway, which has been associated with T cell development and function, leading to the downregulation of TRBV1 expression. | ||||||
Sotrastaurin | 425637-18-9 | sc-474229 sc-474229A | 5 mg 10 mg | $300.00 $540.00 | ||
Sotrastaurin inhibits TRBV1 expression by selectively inhibiting protein kinase C (PKC), which plays a crucial role in T cell activation and the expression of TRBV1, ultimately leading to its downregulation. | ||||||
Pimecrolimus | 137071-32-0 | sc-208172 | 1 mg | $140.00 | 2 | |
Pimecrolimus inhibits TRBV1 expression by inhibiting calcineurin, a phosphatase that plays a role in T cell activation and the subsequent expression of TRBV1, ultimately leading to its downregulation. | ||||||
Apremilast | 608141-41-9 | sc-480062 | 5 mg | $444.00 | ||
Apremilast inhibits TRBV1 expression by inhibiting phosphodiesterase 4 (PDE4), which regulates the levels of cyclic adenosine monophosphate (cAMP) in immune cells, ultimately affecting T cell activation and the expression of TRBV1. | ||||||
Ruxolitinib | 941678-49-5 | sc-364729 sc-364729A sc-364729A-CW | 5 mg 25 mg 25 mg | $246.00 $490.00 $536.00 | 16 | |
Ruxolitinib inhibits TRBV1 expression by selectively inhibiting Janus kinases (JAKs), which are involved in cytokine receptor signaling, ultimately affecting T cell activation and the expression of TRBV1. | ||||||