Catalog No.
Product Name
Application
Product Information
Citations
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Stable Isotope
Budesonide-d6 is a deuterium-labeled derivative of Budesonide, primarily targeting the glucocorticoid receptor. Known for its anti-inflammatory properties, Budesonide-d6 is utilized in research to study mechanisms of action related to asthma and lung diseases. This stable isotope variant allows for enhanced tracking of Budesonide pharmacokinetics and dynamics in biological systems, making it valuable for studies focused on tumor reduction and gene expression modulation. -
Mineralocorticoid Receptor Antagonist
DSR-71167 is an orally active mineralocorticoid receptor antagonist exhibiting an IC50 of 0.26 μM. This compound displays weak carbonic anhydrase inhibitory activity with an IC50 of 19 μM. DSR-71167 has demonstrated the ability to dose-dependently enhance urinary sodium excretion and effectively lowers systolic blood pressure in hypertensive rat models, while presenting a low risk of hyperkalemia in potassium-loading scenarios. It is suitable for research focused on hypertension and heart failure. -
Drug-Linker Conjugate for ADC
Glucocorticoid receptor agonist-1 phosphate Gly-Glu-Br functions as a drug-linker conjugate for antibody-drug conjugate (ADC) applications. This compound facilitates the synthesis of various therapeutic agents, including ABBV-154, ABBV-927, and ABBV-368, by effectively targeting the glucocorticoid receptor. Its utility in ADC development makes it a valuable reagent for researchers focused on innovative treatment strategies in oncology and immunology. -
Glucocorticoid Receptor Agonist
Glucocorticoid receptor agonist-1 Ala-Ala-Mal is a potent agonist of the glucocorticoid receptor, playing a critical role in anti-inflammatory and immunosuppressive pathways. This compound can be strategically conjugated with Adalimumab to develop antibody-drug conjugates (ADCs) for targeted therapy applications. Its functionality makes it a valuable reagent for research in chronic inflammatory conditions and autoimmune diseases. -
ABBV-3373 Reference
Glucocorticoid receptor agonist-2 Ala-Ala-Mal acts as an active reference for ABBV-3373 and serves as a ligand for the glucocorticoid receptor. This compound is instrumental in the synthesis of antibody-drug conjugates (ADCs) with anti-inflammatory properties. Its ability to modulate glucocorticoid receptor activity makes it a valuable reagent in the development of therapeutics targeting inflammatory diseases. -
ADC/PROTAC Linkers
Glucocorticoid receptor agonist-1 phosphate(2,6-difluoro) Ala-Ala-Br serves as a versatile drug-linker conjugate for antibody-drug conjugate (ADC) applications. This reagent enables the synthesis of conjugates targeting the CD40 antigen, facilitating the development of targeted therapies. Its unique structure supports the design of PROTACs and other innovative bio-conjugates, contributing to advances in cancer research and immunotherapy. -
Glucocorticoid Receptor Agonist
Glucocorticoid receptor agonist-1 phosphate Ala-Ala-Mal is a selective agonist of the glucocorticoid receptor, facilitating the modulation of anti-inflammatory and immunomodulatory pathways. This compound is particularly useful in the development of antibody-drug conjugates (ADCs) targeting the CD40 receptor, offering insights into therapeutic strategies for conditions related to inflammation and immune regulation. It serves as a vital tool for researchers investigating glucocorticoid signaling in various biological contexts. -
Drug-Linker Conjugate
Glucocorticoid Receptor Drug-Linker 1 is a specialized drug-linker conjugate designed for the synthesis of Antibody-Drug Conjugates (ADCs) targeting BDCA2. This compound facilitates precise delivery of therapeutic agents to BDCA2-expressing cells, enhancing the efficacy of treatment while minimizing off-target effects. It is particularly relevant in research focused on immunology and targeted cancer therapies. -
RORγ Inverse Agonist
SR-1903 is an inverse agonist of RORγ and PPARγ, exhibiting IC50 values of approximately 100 nM and 209 nM for these targets, respectively. This compound demonstrates significant anti-inflammatory and anti-diabetic properties, making it valuable in models of collagen-induced arthritis and diet-induced obesity. SR-1903's unique mechanism of action positions it as a useful reagent in researching metabolic disorders and inflammatory diseases. -
PROTAC ERRα Degrader
PROTAC_ERRα is a targeted degrader of the estrogen-related receptor alpha (ERRα), employing a proteolysis-targeting chimera (PROTAC) mechanism for enhanced specificity. This compound induces over 80% proteasomal degradation of ERRα in MCF-7 cells, with a DC50 value of 100 nM. PROTAC_ERRα serves as a valuable tool for investigating the biological functions of ERRα in cancer research and for therapeutic development aimed at ERRα-related pathways. -
Androgen Receptor Antagonist
Atraric acid, known as Methyl atrarate, functions as a specific antagonist of androgen receptors (AR). This compound demonstrates significant anti-inflammatory and anticancer properties by downregulating the expression of the prostate-specific antigen gene in LNCaP and C4-2 cell lines. Additionally, atraric acid inhibits nitric oxide synthesis and cytokine production while suppressing the MAPK-NFκB signaling pathway. Its utility in research extends to investigations of prostate diseases and inflammatory conditions. -
GPR84 Agonist/AKR1C3 Inhibitor
Pyrone-211 is a potent agonist of the GPR84 receptor and an inhibitor of AKR1C3. This compound plays a significant role in modulating the expanded polyamine pathway, making it valuable for research in inflammation and metabolic diseases. Its dual functionality as both a receptor agonist and enzyme inhibitor positions Pyrone-211 as a useful tool for exploring cellular signaling and therapeutic interventions in related pathways. -
Stable Isotope
Fluocinolone acetonide-13C3 is a stable isotope-labeled form of Fluocinolone, a potent glucocorticoid receptor agonist. It exhibits anti-inflammatory properties and effectively inhibits lipid accumulation, making it valuable for investigating its effects on various biological processes. Fluocinolone acetonide-13C3 can be utilized in research involving the proliferation of dental pulp cells and the potential repair of injured pulp tissues, as well as in studies focused on mitigating chemotherapy-induced peripheral neuropathy, particularly in relation to drugs like Paclitaxel. -
ADC Linker
INX-P is an antibody-drug conjugate (ADC) linker designed for targeting glucocorticosteroids. It facilitates the delivery of cytotoxic agents specifically to cancer cells that express glucocorticoid receptors, enhancing therapeutic efficacy while minimizing systemic toxicity. This linker is particularly useful in research applications focusing on ADC development and targeted cancer therapies. -
ADC Linker
Glucocorticoid receptor agonist-1 phosphate Gly-Glu TFA is a cleavable linker designed for the synthesis of Antibody-Drug Conjugates (ADCs). This compound facilitates targeted drug delivery by linking cytotoxic agents to antibodies, enhancing therapeutic efficacy while minimizing off-target effects. Its ability to be cleaved under specific physiological conditions makes it a valuable tool in the development of precision medicine strategies. -
DPP-4/GPR119 Modulator
DPP-4/GPR119 Modulator 1 is a dual-functional compound that serves as an orally active dipeptidyl peptidase IV (DPP-IV) inhibitor and a GPR119 agonist. This compound exhibits significant blood glucose-lowering effects and demonstrates moderate hERG channel inhibition with an IC50 of 4.9 μM. DPP-4/GPR119 Modulator 1 is particularly valuable in diabetes research and functions as a click chemistry reagent, possessing an alkyne group that can participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions with azide-containing molecules. -
DPP-4/GPR119 Modulator
DPP-4/GPR119 modulator 2 is a dipeptidyl peptidase IV (DPP-IV) inhibitor and GPR119 agonist, exhibiting an IC50 of 0.22 μM for DPP-IV and an EC50 of 0.95 μM for GPR119. This compound is pertinent for diabetes research, facilitating studies on metabolic regulation and insulin secretion. Additionally, it features an alkyne group, enabling its use in click chemistry applications through copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. -
Estrogen Receptor Degrader
Rintodestrant is an orally active, non-steroidal selective estrogen receptor degrader. Its primary mechanism involves the degradation of estrogen receptors, leading to reduced estrogen signaling. Additionally, Rintodestrant functions as a CDK4/6 inhibitor, which may further enhance its therapeutic potential. This compound is relevant for research applications in breast cancer treatment and the study of estrogen receptor-related pathways. -
RORγ/DHODH Inhibitor
RORγ/DHODH-IN-2 is a potent dual inhibitor of RORγ and DHODH, exhibiting IC50 values of 11.9 nM and 90 nM, respectively. This compound demonstrates significant antiviral activity against multiple viruses, including SARS-CoV-2, HCMV, HAdV5, and MPXV, with IC50 values of 27 nM, 20 nM, 9.1 nM, and 1.8 nM, respectively. RORγ/DHODH-IN-2 is ideal for research applications targeting immune signaling pathways and viral infections. -
HGPRT/TBrHGPRT1 Inhibitor
HGPRT/TBrHGPRT1-IN-1 is a selective inhibitor of human hypoxanthine-guanine phosphoribosyltransferase (HGPRT) and Trypanosoma brucei HGPRT1 (TBrHGPRT1), with a Ki value of 3 nM for both targets. This compound effectively reduces cell growth through its targeted inhibition mechanism. HGPRT/TBrHGPRT1-IN-1 is particularly valuable for research applications in the fields of infectious diseases and oncology. -
HGPRT Inhibitor
2′-Deoxy-GDP trisodium is a potent inhibitor of hypoxanthine phosphoribosyltransferase (HGPRT), exhibiting an IC50 value of 12.5 μM. As a guanosine monophosphate (GMP) analogue, it plays a significant role in research related to purine metabolism and the recycling pathway in protozoan parasites. This reagent is valuable for studying HGPRT's function and its implications in parasitic diseases. -
Glucocorticoid Agonist
BI 653048 is a selective, orally active nonsteroidal glucocorticoid agonist, targeting the glucocorticoid receptor with an IC50 of 55 nM. It inhibits CYP enzyme isoforms including CYP1A2, CYP2D6, CYP2C9, CYP2C19, and CYP3A4, while exhibiting a reduced affinity for the hERG ion channel (IC50 > 30 μM). Additionally, BI 653048 serves as an HCV NS3 protease inhibitor, demonstrating potential for reducing viral loads in hepatitis C virus infections. This compound is valuable in studies related to glucocorticoid signaling and antiviral research. -
GPR39 Agonist
Glycolithocholic acid 3-sulfate disodium functions as a GPR39 agonist, exhibiting EC50 values of 47.9 and 66.8 μM in the absence of Zn2+, and 8 and 8.7 μM in the presence of Zn2+ in M39-20 and hGPR39-2 cell lines, respectively. This compound activates GPR39 receptors to promote intracellular calcium signaling without relying on Zn2+ binding sites H17 and H19. Additionally, it demonstrates the ability to inhibit HIV-1 replication in vitro. Glycolithocholic acid 3-sulfate disodium is a valuable tool for investigating HIV infection and gallbladder disease mechanisms. -
GPR15 Antagonist
GPR15 antagonist-1 is a selective antagonist of the G protein-coupled receptor 15 (GPR15). This compound is implicated in critical biological processes related to HIV infection, colonic inflammation, and smoking-related diseases. GPR15 antagonist-1 serves as a valuable tool for research exploring the therapeutic potential of modulating GPR15 activity in various pathological contexts. -
Renin/HIV-1 Protease Inhibitor
PD 134922 is a potent inhibitor of renin and HIV-1 protease, exhibiting an IC50 of 15 nM against HIV-1 protease. This compound is valuable in studies focused on the modulation of blood pressure regulation through renin inhibition and provides insights into HIV-1 protease activity. Its application extends to research in antiviral therapies and blood pressure-related disorders, making it a useful tool for scientists in pharmacological studies. -
RORγ/DHODH Inhibitor
Izumerogant (IMU-935) is an orally active dual inhibitor of RORγ and DHODH, with IC50 values of 10 nM and 98 nM, respectively. This compound effectively disrupts the replication of various viruses, including SARS-CoV-2, HCMV, and HAdV5, demonstrated by EC50 values ranging from 3.6 to 17 nM. Izumerogant serves as a valuable tool for investigating antiviral mechanisms and therapeutic strategies against viral infections. -
Stable Isotope
Fluticasone propionate-d5 is a deuterium-labeled derivative of fluticasone propionate, a potent topical anti-inflammatory corticosteroid. This compound selectively binds to the glucocorticoid receptor, exhibiting an absolute affinity (KD) of 0.5 nM, and demonstrates minimal interaction with other steroid receptors. It is primarily utilized in research involving anti-inflammatory and potential antiviral activities, making it a valuable reagent for studies focused on corticosteroid receptor mechanism and function. -
Dexamethasone-Glucocorticoid Receptor Inhibitor
Collismycin B is a potent inhibitor of the dexamethasone-glucocorticoid receptor, exhibiting an IC50 value of 10 µM. This compound demonstrates notable antimicrobial activity, making it a valuable tool for research in microbial pathogenesis. Additionally, Collismycin B exhibits cytotoxic properties, offering potential applications in cancer research and therapeutic development. -
Androgen Receptor Inhibitor
Fenarimol is a selective androgen receptor inhibitor with an IC50 value of 19 µM. This compound has been shown to downregulate the mRNA expression of key genes, including PBP C3, ODC, and IGF-1. Fenarimol serves as a valuable tool in research investigating androgen signaling pathways and its role in various biological processes. Additionally, its fungicidal properties may provide insights into the interplay between hormonal regulation and fungal growth mechanisms. -
GPR120 Agonist
9-PAHSA is a potent endogenous agonist of the GPR120 receptor, demonstrating an EC50 of 18 μM. This compound effectively inhibits LPS-induced inflammatory responses by blocking the NF-κB pathway, showcasing its anti-inflammatory properties. Additionally, 9-PAHSA promotes adipocyte browning, enhances glucose uptake, and diminishes lipid accumulation, while supporting mitochondrial function in steatotic hepatocytes. It also exhibits neuroprotective effects by modulating the expression of REST and BDNF in the prefrontal cortex of diabetic mice, preventing cognitive deficits and abnormal social behaviors. 9-PAHSA is valuable for research into diabetes-related cognitive impairment, obesity, and non-alcoholic fatty liver disease. -
Renin Substrate
Renin FRET Substrate I is a selective substrate for human renin, featuring the specific cleavage site found in the N-terminal peptide of human angiotensinogen. This reagent facilitates the study of renin activity through FRET-based assays, enabling researchers to investigate the role of renin in the renin-angiotensin system and its implications in hypertension and cardiovascular diseases. Its use in enzymatic assays allows for the precise measurement of renin activity in biological samples. -
GPRC5A Agonist
7-Fluorotryptamine hydrochloride acts as a potent agonist of GPRC5A, promoting β-arrestin recruitment through GPRC5A activation. This compound is valuable for studying immune and cancer signaling pathways, providing insights into the mechanisms of GPRC5A in various biological contexts. Its role in modulating receptor activity makes it a useful tool for researchers investigating related biochemical processes. -
GPR35 Agonist
GPR35 Agonist 2 is a highly effective compound that specifically activates the GPR35 receptor, demonstrating EC50 values of 26 nM and 3.2 nM in β-arrestin recruitment and Ca2+ release assays, respectively. This agonist plays a significant role in advancing research related to GPR35 signaling pathways and their implications in various physiological processes. Its potent activity makes it suitable for studies investigating the therapeutic potential of targeting GPR35 in metabolic and inflammatory conditions. -
GPR183 Inverse Agonist
GPR183 inverse agonist-1 is a potent inverse agonist targeting the G protein-coupled receptor GPR183. It effectively inhibits GPR183-mediated Gi activation and prevents β-arrestin2 recruitment, thereby blocking the migration of peripheral blood mononuclear cells (PBMCs). This compound is valuable for research into inflammatory, autoimmune, and neoplastic disorders, enabling scientists to explore its therapeutic potential in these fields. -
GPR18 Agonist
PSB-KK1415 is a selective agonist for the human orphan G protein-coupled receptor GPR18, exhibiting an EC50 value of 19.1 nM. This compound has been identified to modulate receptor activity and can be utilized in various biological research applications, including studies of neurological processes and potential therapeutic pathways. Its specificity for GPR18 makes it a valuable tool for exploring receptor signaling mechanisms and their implications in health and disease. -
GPR18 Agonist
PSB-KK1445 is a potent and selective GPR18 agonist, exhibiting EC50 values of 45.4 nM for human GPR18 and 124 nM for mouse GPR18. It demonstrates over 200-fold selectivity against both cannabinoid receptor subtypes, GPR55, and GPR183. This compound is valuable for research applications exploring the physiological roles of GPR18 in various biological processes and potential therapeutic uses related to the endocannabinoid system. -
GPR55 Antagonist
PSB-SB-487 is a potent antagonist of GPR55, exhibiting an IC50 value of 0.113 µM, and acts as an agonist for the CB2 receptor with a Ki value of 0.292 µM. This compound is valuable for investigating various biological processes and disease states, including diabetes, Parkinson’s disease, neuropathic pain, and cancer. Its dual activity makes it a significant tool for understanding the role of cannabinoid receptors in disease mechanisms and potential therapeutic interventions. -
GPR55 Fluorescent Ligand
Tocrifluor 1117 is a selective fluorescent ligand targeting the GPR55 receptor. This compound serves as a valuable tool in research for visualizing the cellular distribution of cannabinoid receptors, including GPR55, in live tissues. With excitation and emission maxima at 543 nm and 590 nm, respectively, Tocrifluor 1117 enhances the understanding of cannabinoid receptor localization and function in various biological contexts. -
GPR18 Agonist
PSB-KD107 is an agonist of the GPR18 receptor, a cannabinoid-activated orphan G-protein-coupled receptor. This compound exhibits anti-inflammatory activity and is applicable in research related to Duchenne muscular dystrophy, making it a valuable tool for investigating inflammation-related pathways and therapeutic interventions in muscle degeneration. -
GPR133 Agonist
AP-503 is a selective agonist of GPR133 (also known as ADGRD1), exhibiting an EC50 value of 1.21 nM. This compound is of significant interest in research focused on mitigating muscle-related diseases and addressing vestibular dysfunction. Its precise modulation of GPR133 activity presents opportunities for elucidating the receptor's role in associated physiological pathways. -
GPER Agonist
(3aS,4R,9bR)-G-1 is a selective agonist of the G protein-coupled receptor GPR30, exhibiting a Ki value of approximately 7 nM. This compound activates rapid signaling pathways, including intracellular calcium mobilization and PI3K signaling, which are implicated in promoting uterine epithelial cell proliferation and exhibiting antidepressant effects. (3aS,4R,9bR)-G-1 holds potential for research applications in breast cancer and depression studies. -
Androgen Receptor Inhibitor
AZD9750 is an orally bioavailable proteolysis-targeting chimera (PROTAC) that acts as an androgen receptor (AR) inhibitor. It facilitates the proteasome-dependent degradation of both wild-type AR and the ARL702H resistance mutant by targeting and binding to AR and cereblon (CRBN). In in vitro studies, AZD9750 effectively inhibits AR signaling and demonstrates significant anti-tumor activity in mouse prostate cancer xenograft models. This compound is valuable for research focused on prostate cancer. -
GPR17 Modulator
ASN02563583 is a GPR17 modulator that exhibits an IC50 value of 0.64 nM in the [35S]GTPγS binding assay, indicating its potency in regulating GPR17 receptor activity. This compound is particularly relevant for research focused on neurological diseases, providing insights into the role of GPR17 in related pathophysiological processes. -
GPR17 Antagonist
GPR17 Antagonist 1 is a selective antagonist of the GPR17 receptor, which is involved in various physiological processes. This compound exhibits significant inhibitory activity on GPR17, making it a valuable tool for studying metabolic disorders such as diabetes and obesity. Its application in pharmacological research contributes to the understanding of GPR17's role in these diseases and may aid in the development of therapeutic strategies. -
GPR17 Agonist
ASN04421891 is a potent GPR17 agonist, exhibiting nanomolar EC50 and high specificity. This compound facilitates the maturation of oligodendrocyte precursor cells into mature myelinating oligodendrocytes, making it a valuable tool for investigating neurodegenerative diseases. ASN04421891 is applicable in research related to cerebral and cardiac ischemia, multiple sclerosis, schizophrenia, depression, Alzheimer's disease, Parkinson's disease, Huntington's chorea, amyotrophic lateral sclerosis (ALS), and various neuroinflammatory disorders. -
GPR110 Agonist
GPR110 peptide agonist P12 is an agonist targeting the GPR110 receptor. This peptide significantly enhances the initial rate of G protein GTPγS binding stimulated by GPR110, effectively mimicking natural ligands. By inducing dissociation between the receptor's extracellular domain and its seven transmembrane domains, P12 exposes the β-strand-13/stalk region of the 7TM domain, facilitating G protein signaling activation. This compound is valuable for research into developmental disorders and cancers associated with GPR110 pathways. -
GPR17 Modulator
GPR17 modulator-1 is a potent modulator of the G protein-coupled receptor GPR17, exhibiting an IC50 of less than 10 nM for human GPR17 in CHO cells. This compound demonstrates moderate pharmacokinetic properties in murine models and is capable of crossing the blood-brain barrier. GPR17 modulator-1 is valuable for research focused on neuroinflammatory disorders and central nervous system-related applications. -
Metabolite of Hydrocortisone
20β-Dihydrocortisol is a metabolite of Hydrocortisone that acts as a weak endogenous agonist of the glucocorticoid receptor (GR). This compound is generated from Hydrocortisone through the action of carbonyl reductase 1 (CBR1) in an NADPH-dependent process. Its unique properties make 20β-Dihydrocortisol valuable for investigating metabolic disorders such as obesity and its impact on glucocorticoid signaling pathways. -
Glucocorticoid Receptor Antagonist
CP-394531 is a highly selective non-steroidal antagonist of the glucocorticoid receptor (GR), exhibiting a Ki value of 0.1 nM. It demonstrates minimal binding to the androgen receptor (AR) (Ki = 130 nM) and negligible effects on the progesterone receptor and estrogen receptors (ERα, ERβ). CP-394531 effectively inhibits the agonistic effects of Dexamethasone with a Kif of 4.1 nM. This compound is valuable for researching a variety of conditions, including diabetes, obesity, depression, neurodegenerative disorders, glaucoma, and Cushing's disease. -
Nasal Spray
Fluticasone furoate is a synthetic trifluorinated corticosteroid that targets the glucocorticoid receptor with a high affinity (Kd of 0.3 nM). It exhibits significant anti-inflammatory and anti-asthmatic properties while maintaining low systemic exposure. This compound is primarily utilized in the treatment of allergic rhinitis, providing effective relief from nasal inflammation and associated symptoms.
