Catalog No.
Product Name
Application
Product Information
Citations
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Renin inhibitor
SR 42128 is a potent renin inhibitor that primarily targets the renin-angiotensin system. This compound demonstrates significant inhibition of primate renin activity, while exhibiting reduced efficacy against renins from other species. SR 42128 is valuable for research applications focused on hypertension, cardiovascular disease, and renal function studies. -
Renin Inhibitor
Ditekiren is a pseudohexapeptide renin inhibitor that targets the renin-angiotensin system. It effectively inhibits renin activity, leading to a reduction in the formation of angiotensin II, a key vasoconstrictor involved in blood pressure regulation. This compound is valuable for research applications focused on hypertension, cardiovascular physiology, and fluid balance studies. -
Renin Inhibitor
U-80125 is a competitive inhibitor of human renin, demonstrating an IC50 value of 2.3 μM. This dansylated peptide is characterized by excitation and emission maxima at 340 and 530 nm, respectively. U-80125 is valuable for research focused on hypertension and cardiovascular disease, facilitating the study of renin's role in the renin-angiotensin-aldosterone system. -
Renin Inhibitor
MK-8141 (ACT-077825) is a selective renin inhibitor that increases immunoreactive renin (ir-AR) levels by up to sevenfold. Its primary research applications are focused on evaluating antihypertensive efficacy in hypertensive models. Although MK-8141 demonstrates changes in ir-AR, it does not result in sustained reductions in plasma renin activity (PRA) and does not produce significant blood pressure-lowering effects. -
Renin Inhibitor
Renin-IN-3 is a potent renin inhibitor that selectively targets the renin-angiotensin system. It has demonstrated significant biological activity in modulating blood pressure, making it a valuable tool for hypertension research. This compound can be utilized to explore mechanisms of renal function and cardiovascular regulation in various experimental models. -
Renin Inhibitor/Microbiota Modulator
Theasinensin C is an orally active renin inhibitor with an IC50 of 40.21 μM, demonstrating significant modulation of gut microbiota. It selectively enhances the population of Akkermansia muciniphila, promoting beneficial hydrolysis of mucin and influencing the gut-kidney-liver metabolic signaling pathways that contribute to creatine biosynthesis. This compound is valuable for studying hypertension and neuroinflammation, especially in the context of high-fructose diets, as it has been shown to improve cognitive function, reduce pro-inflammatory cytokines, and restore intestinal barrier integrity. -
Renin Inhibitor
PD 132002 is a potent, orally active inhibitor of renin, a key enzyme in the renin-angiotensin system. By effectively reducing plasma renin activity, PD 132002 leads to significant decreases in blood pressure. This compound serves as a valuable tool for research into hypertension and related cardiovascular disorders. Additionally, it exhibits weak inhibition of pepsin, highlighting its specific targeting mechanism. -
Renin Inhibitor
CP 71362 is a potent renin inhibitor that acts as a substrate-analog transition state mimic, demonstrating significant antihypertensive activity. It effectively inhibits plasma renin across species, with IC50 values of 3 nM in rats, 0.0033 nM in dogs, and 20 nM in humans. CP 71362 significantly reduces mean arterial pressure in both anesthetized and conscious sodium-depleted models, showing a dose-dependent effect. This compound is valuable for research focused on hypertension and congestive heart failure. -
Renin Inhibitor
A-74273 is an orally active peptide renin inhibitor with an IC50 value of 3.1 nM. This compound competitively inhibits renin by binding to its active site, thereby obstructing the conversion of angiotensinogen to angiotensin I and subsequently reducing angiotensin II levels. A-74273 is utilized in research focused on hypertension and related cardiovascular diseases. -
Renin Inhibitor
Renin inhibitor-1 is a potent, orally active renin inhibitor with IC50 values of 0.9 nM for recombinant human renin and 1.8 nM for human plasma renin activity (hPRA). This compound demonstrates significant antihypertensive efficacy, making it a valuable tool for studying hypertension and related cardiovascular and renal diseases. Its ability to effectively inhibit renin positions it as a key agent in cardiovascular research. -
Renin Antagonist
Handle region peptide, rat is a prorenin receptor antagonist that effectively inhibits the activation of prorenin, thereby mitigating the progression of diabetic nephropathy. This compound demonstrates significant anti-inflammatory properties, particularly within ocular tissues. Its applications extend to research on renal disease models and ocular inflammation, providing valuable insights into therapeutic interventions for these conditions. -
Oligopeptide Renin Inhibitor
PD 125967 is an oligopeptide renin inhibitor that specifically targets the renin-angiotensin system. It exhibits significant activity in lowering blood pressure, making it a valuable tool for cardiovascular research. This compound is useful for studying hypertension and related disorders, providing insights into the regulation of blood pressure through renin inhibition. -
Renin Inhibitor
Remikiren is a potent and selective inhibitor of renin, demonstrating high specificity with IC50 values of 0.7 nM for human renin and 0.8 nM for human plasma renin. This compound effectively lowers mean arterial blood pressure in sodium-depleted marmosets and squirrel monkeys, making it a valuable tool for research into hypertension. Remikiren serves as a key reagent for exploring the renin-angiotensin system and its implications in cardiovascular diseases. -
Renin Substrate
Suc-Arg-Pro-Phe-His-Leu-Leu-Val-Tyr-AMC is a specific renin substrate designed for studying renin activity. This peptide substrate facilitates the measurement of renin enzymatic activity in various biological assays, enabling researchers to investigate the renin-angiotensin system's role in cardiovascular and renal physiology. Its application includes the development of assays for screening renin inhibitors and elucidating mechanisms of blood pressure regulation. -
Renin Inhibitor
SR 43845 is a selective renin inhibitor that effectively reduces blood pressure by inhibiting plasma renin activity. This compound is primarily used in hypertension research, providing valuable insights into the regulation of blood pressure and the renin-angiotensin system. Its application in preclinical studies can aid in the development of therapeutic strategies for hypertension management. -
Renin Inhibitor
PD-134672 is a potent renin inhibitor featuring a 2-amino-4-thiazolyl substituent. It demonstrates significant in vitro inhibition of monkey renin, while exhibiting only minimal effects on the related protease bovine feline hepsin D. This compound has shown oral hypotensive activity in hyperreninemic normotensive monkeys and has been identified for further evaluation in renal hypertensive models due to its strong efficacy and prolonged effects. PD-134672 is a valuable tool for research exploring mechanisms of hypertension and the therapeutic potential of renin inhibition. -
Renin Inhibitor
EMD 52297 is a potent renin inhibitor that effectively modulates hemodynamic and hormonal responses. In addition to its primary action, EMD 52297 also exhibits activity as an angiotensin-converting enzyme (ACE) inhibitor. This compound is primarily utilized in cardiovascular research and hypertension studies, providing insights into the regulation of blood pressure and renal function. -
Renin Inhibitor
A-65317 is a primate-selective renin inhibitor that exhibits a potent inhibitory effect with an IC50 of 0.37 nM. This compound is known for its long-lasting hypotensive response, making it valuable in cardiovascular research. A-65317 can be utilized in studies focused on hypertension and renal function regulation. -
Renin Inhibitor
Cgp 38560 methanesulfonate is a selective renin inhibitor that modulates the renin-angiotensin system. This compound exhibits a dose-dependent decrease in angiotensin II levels and plasma renin activity, while simultaneously increasing active renin concentrations. Cgp 38560 methanesulfonate is utilized in research focused on hypertension and cardiovascular disease, providing valuable insight into renin regulation and therapeutic interventions. -
Renin Inhibitor
PD125754 is a potent oligopeptide inhibitor of renin, exhibiting an IC50 of 22 nM. This compound effectively reduces renin activity, making it valuable for studies related to hypertension and cardiovascular diseases. Its ability to modulate the renin-angiotensin system can aid in the exploration of mechanisms underlying renal and cardiovascular function. -
Renin
ES-8891 is a selective renin inhibitor that effectively reduces plasma renin activity and immunoreactive renin concentrations. In a study involving normotensive sodium-depleted macaques, administration of ES-8891 led to a significant decrease in plasma angiotensin I levels and a notable reduction in mean blood pressure, without affecting heart rate. This compound serves as a valuable tool for research on blood pressure regulation and the renin-angiotensin system. -
Renin Inhibitor
SC-46944 is an orally active renin inhibitor that effectively targets the renin-angiotensin system. It demonstrates significant potential in the study of hypertension by reducing renin activity and subsequently lowering blood pressure. This compound serves as a valuable tool in cardiovascular research and the development of antihypertensive therapies. -
Human Renin Inhibitor
ES 6864 is a potent, orally active competitive inhibitor of human renin, demonstrating an IC50 of 6.9 nM and a Ki of 7.3 nM. It possesses high specificity for both species and enzyme, making it a valuable tool in cardiovascular research. Additionally, ES 6864 exhibits metabolic stability in rat tissue homogenates and effectively lowers blood pressure in rat models and sodium-depleted awake marmosets, supporting its potential applications in hypertension studies. -
Renin Inhibitor
ACT 178882 is a potent renin inhibitor with an IC50 of 1.4 nM. It effectively modulates the renin-angiotensin-aldosterone system, leading to potential applications in the treatment of hypertension and related cardiovascular disorders. This compound serves as a valuable tool for research into the role of renin in blood pressure regulation and the development of novel antihypertensive therapies. -
REV-ERB Agonist
STL1267 is a potent REV-ERB agonist, demonstrating a Ki value of 0.16 µM for REV-ERBα. This compound effectively crosses the blood-brain barrier and has been shown to inhibit the gene expression of BMAL1. STL1267 is an invaluable tool for research into circadian rhythms and metabolic processes. Its lack of cytotoxicity further enhances its suitability for in vitro studies. -
REV-ERBα/β Antagonist
BE2012 is a potent and selective antagonist of REV-ERBα and REV-ERBβ, exhibiting EC50 values of 0.285 μM and 0.346 μM, respectively. By binding to the ligand-binding domain of REV-ERB, BE2012 inhibits the recruitment of co-inhibitory factors, leading to the release of transcriptional repression on downstream target genes. This compound has been demonstrated to upregulate myogenic transcription factors, such as Myf5 and Myod, and is applicable in research focused on muscle regeneration and repair in models of acute muscle injury. -
REV-ERB-specific Synthetic Ligand
SR12418 is a synthetic ligand that specifically targets REV-ERBα and REV-ERBβ, exhibiting IC50 values of 68 nM and 119 nM, respectively. This compound is valuable for studying the role of REV-ERBs in various biological processes and is particularly applicable in research related to experimental autoimmune encephalomyelitis (EAE) and colitis. Researchers can leverage SR12418 to investigate its potential therapeutic effects and the underlying mechanisms involved in these inflammatory conditions. -
REV-ERB Inverse Agonist
GSK1362 is a selective inverse agonist of REV-ERB, targeting the disruption of its interaction with repressive co-modulators such as NCoR1, SMRT2, and RIP140. By promoting the transcriptional activity of BMAL1, GSK1362 alleviates the repression caused by endogenous REV-ERB ligands. This compound has been shown to reduce LPS-induced inflammatory cytokine expression and inhibit IL-1β-induced Cxcl5 transcription in various cell types, making it a valuable tool for research into inflammatory diseases. -
TH17 Cell Differentiation Inhibitor
3-Oxo-5β-cholanoic acid, also known as Dehydrolithocholic acid, functions as a potent inhibitor of TH17 cell differentiation. This compound achieves its biological activity by directly binding to the transcription factor RORγt, with a dissociation constant (Kd) of 1.13 μM. It is useful in research applications aimed at understanding inflammatory responses and immune modulation. -
RORγt Inhibitor
GSK805 is an orally active RORγt inhibitor that effectively modulates immune responses. Its mechanism involves inhibiting RORγ and the differentiation of Th17 cells, demonstrating pIC50 values of 8.4 and >8.2, respectively. GSK805 further suppresses Th17 cell functionality, making it a valuable tool for investigating immune-related disorders and therapeutic approaches targeting RORγt in inflammatory conditions. -
RORα Agoinst
Neoruscogenin is a high-affinity agonist of the nuclear receptor RORα (NR1F1), exhibiting an EC50 of 0.11 µM. This compound plays a crucial role in modulating gene expression and is involved in various physiological processes, including circadian rhythm and metabolism. Neoruscogenin is applicable in research areas focusing on nuclear receptor signaling and the development of therapeutics targeting metabolic disorders. -
ROR-γ Antagonist
XY018 is a selective antagonist of ROR-γ (retinoic acid receptor-related orphan receptor gamma), designed to inhibit its constitutive activity. With an EC50 value of 190 nM in 293T cells, XY018 effectively disrupts ROR-γ signaling by binding to its hydrophobic ligand binding domain. This compound is valuable for research applications focused on autoimmune diseases, metabolic disorders, and inflammation by modulating ROR-γ activity. -
RORγt Antagonist
Bevurogant is a selective antagonist of the retinoid-related orphan receptor gamma t (RORγt), which plays a critical role in immune response and inflammation. This compound is primarily utilized in research focused on chronic inflammatory diseases, offering insights into therapeutic strategies for conditions such as autoimmune disorders. Its ability to modulate RORγt activity makes it a valuable tool in the study of immune regulation and potential treatment pathways. -
RORγt Inverse Agonist
MRL-871 is a potent allosteric inverse agonist of the retinoic acid receptor-related orphan receptor γt (RORγt), exhibiting an IC50 of 12.7 nM. This compound is characterized by its unique isoxazole chemotype and demonstrates significant efficacy in reducing IL-17a mRNA production in EL4 cells. MRL-871 is useful for research applications focused on immune response modulation and studying the role of RORγt in autoimmune diseases. -
RORγt Inverse Agonist
JNJ-61803534 is a potent RORγt inverse agonist, exhibiting an IC50 of 9.6 nM. This compound demonstrates significant anti-inflammatory activity by inhibiting the production of IL-17A in human CD4+ T cells during Th17 differentiation. JNJ-61803534 is valuable for research in autoimmune disease and inflammation pathways, facilitating the study of RORγt as a therapeutic target. -
RORγ Inverse Agonist
RORγ inverse agonist 1 is an inverse agonist of the retinoic acid receptor-related orphan receptor gamma (RORγ). This compound modulates RORγ activity, negatively regulating its transcriptional activity. It is primarily utilized in research related to immune responses and inflammation, offering insights into potential therapeutic strategies targeting autoimmune diseases and related disorders. -
ROR1 Inhibitor
LDR102 is a potent inhibitor of receptor tyrosine kinase-like orphan receptor 1 (ROR1) with a Ki value of 0.10 μM. This compound effectively inhibits the proliferation of various cancer cell lines, including H1975, A549, and MDA-MB-231, exhibiting IC50 values of 0.36 μM, 1.37 μM, and 0.47 μM, respectively. Additionally, LDR102 demonstrates antitumor efficacy in murine models and displays favorable pharmacokinetic properties in rat studies, making it a valuable tool for cancer research and therapeutic development. -
RORγt Inverse Agonist
RORγt inverse agonist 13 is a selective inverse agonist targeting the RORγt receptor with an IC50 of 63.8 nM. This compound demonstrates potent biological activity, making it suitable for research applications focusing on autoimmune diseases and T cell differentiation. Its improved agent-like properties enhance its utility in preclinical studies investigating the modulation of RORγt signaling pathways. -
RORγ Inverse Agonist
SR1555 is a specific inverse agonist of the retinoic acid receptor-related orphan nuclear receptor γ (RORγ), exhibiting an IC50 value of 1 μM. This compound is known to effectively inhibit TH17 cell development and function while promoting an increase in T regulatory cell frequency and downregulating IL-17 expression. SR1555 is valuable for investigating mechanisms in autoimmune disease research. -
RORγ Antagonist
(±)-ML 209 is a selective RORγ antagonist that effectively inhibits RORγt transcriptional activity, demonstrating an IC50 of 300 nM in HEK293t cells. This diphenylpropanamide compound specifically suppresses murine Th17 cell differentiation while leaving the differentiation of naïve CD4+ T cells into Th1 and regulatory T cell lineages unaffected. Its unique mechanism makes (±)-ML 209 a valuable tool for researchers investigating the role of RORγ in immune responses and related diseases. -
RORγt Activator
7ß,27-Dihydroxycholesterol (7β, 27-OHC) is a selective activator of RORγt, exhibiting a Ki of 120 nM. This compound plays a crucial role in promoting the differentiation of CD4+ Th17 cells in both mouse and human models. Additionally, 7ß,27-Dihydroxycholesterol enhances IL-17 production through a CYP27A1-dependent pathway, making it valuable for studies focused on immune response and related signaling pathways. -
RORγt Inverse Agonist
Cedirogant is an orally active inverse agonist of the retinoic acid receptor-related orphan receptor gamma-t (RORγt). It demonstrates significant potential in modulating immune responses, particularly in the context of psoriasis research. This compound serves as a valuable tool for investigating therapeutic strategies targeting autoimmune and inflammatory conditions. -
RORγt Antagonist
TMP920 is a potent and selective antagonist of RORγt, a retinoic acid receptor-related orphan receptor involved in immune signaling. It effectively inhibits the binding of RORγt to the SRC1 peptide, demonstrating an IC50 value of 0.03 μM. TMP920 is valuable for research applications focusing on autoimmune diseases, as well as the modulation of Th17 cell differentiation and function. -
ROR Antagonist
GNE-3500 is a selective, orally active antagonist of Retinoic Acid Receptor-Related Orphan Receptor C (RORc, also known as RORγ or NR1F3), exhibiting an EC50 of 12 nM. This compound demonstrates favorable pharmacokinetic properties in rat models, making it a valuable tool for research applications focused on modulating RORc-related pathways. GNE-3500 is particularly relevant for studies investigating autoimmune diseases and inflammatory responses where RORc plays a critical regulatory role. -
ROR-γ Inhibitor
JTE-151 is a potent ROR-γ inhibitor that effectively modulates immune responses by inhibiting ROR-γ activity associated with the activation of Th17 cells. This mechanism allows JTE-151 to serve as a valuable tool in the study of autoimmune diseases and related immunological disorders. By suppressing the overactive immune response, it holds promise for advancing research in therapeutic strategies targeting autoimmune conditions. -
RORγt Inverse Agonist
RORγt Inverse Agonist 10 is a potent inverse agonist targeting the retinoic acid receptor-related orphan nuclear receptor gamma t (RORγt), with an IC50 of 51 nM. This compound effectively suppresses the expression of key genes involved in the pathogenesis of psoriasis, including IL-17A, IL-22, and IL-23R. It is suitable for research applications exploring the mechanisms of autoimmune diseases and the development of novel therapeutics for psoriasis. -
ROR Agonist
RORγt inverse agonist 23 is a potent and selective inverse agonist targeting the retinoic acid receptor-related orphan receptor gamma t (RORγt). This compound demonstrates significant biological activity as an immunomodulator, making it valuable in the investigation of autoimmune diseases and inflammatory disorders. Its oral bioavailability enhances its utility in preclinical studies and therapeutic research applications. -
RORγt Agonist
RORγt Agonist 3 is a potent activator of RORγt, crucial for the differentiation of Th17 cells. This compound enhances the production of pro-inflammatory cytokines, thereby boosting lymphocyte cytotoxicity. Additionally, RORγt Agonist 3 suppresses the generation of regulatory T cells, which may lead to an augmented immune response, making it valuable for research into immune modulation and inflammatory diseases. -
RORγ(t) Agonist
Hexyl 4-hydroxybenzoate, also known as Hexylparaben, is a selective agonist for the retinoic acid-related orphan receptor RORγ(t), exhibiting an EC50 value of 144 nM. This compound is valuable in the investigation of autoimmune diseases and immune-related processes, providing insights into the modulation of immune responses and potential therapeutic interventions. Its role in RORγ(t) signaling makes it a crucial tool for researchers studying T-cell differentiation and related pathways. -
ROR1 Ligand
Antitumor agent-127 is a macrocyclic peptide that targets the ROR1 receptor. It exhibits nanomolar affinity for ROR1, demonstrating effective binding and substantial internalization in 786-O and MDA-MB-231 tumor cell lines. This compound is valuable for research in cancer biology, particularly in studies focused on ROR1-mediated signaling pathways and potential therapeutic applications in tumors expressing ROR1.
