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Results for "

dual modulator

" in MedChemExpress (MCE) Product Catalog:

57

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1

Peptides

2

Natural
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1

Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-175742
    BMS-986470

    		Molecular Glues Ligands for E3 Ligase Histone Acetyltransferase Cardiovascular Disease
    BMS-986470, a HbF-activating CRBN E3 ligase modulator (CELMoD), is an orally active dual molecular glue degrader targeting ZBTB7A and WIZ. BMS-986470 has potent γ-globin induction activity. BMS-986470 can be used for sickle cell disease (SCD) research .
    BMS-986470
  • HY-109168
    Bersacapavir
    2 Publications Verification

    JNJ-6379; JNJ-56136379

    		 HBV DNA/RNA Synthesis Infection
    Bersacapavir (JNJ-6379) is an HBV capsid assembly modulator. Bersacapavir exerts a dual mechanism of action against both early and late stages of HBV infection by forming complete genome-free empty capsids and inhibiting de novo synthesis of cccDNA. Bersacapavir inhibits HBV replication. Bersacapavir can be used in the research of hepatitis B .
    Bersacapavir
  • HY-143712
    Allolithocholic acid
    1 Publications Verification

    		 Drug Metabolite G protein-coupled Bile Acid Receptor 1 ROR Metabolic Disease Inflammation/Immunology Cancer
    Allolithocholic acid is an orally active metabolite of Lithocholic acid (HY-B0172). Allolithocholic acid is a dual GPBAR1 agonist (EC50 = 2.7 μM) and RORγt inverse agonist (IC50 = 3.4 μM). Allolithocholic acid modulates immune and metabolic pathways, regulates immune cell polarization, prevents M1 macrophage and Th17 CD4 cell polarization. Allolithocholic acid improves insulin sensitivity, reduces liver lipid accumulation, reverses liver immunological, inflammatory and metabolic signaling dysregulation, restores bile acid homeostasis, adipose tissue histopathology/function, and intestinal microbiota composition, modulates intestinal immunity. Allolithocholic acid can be used for the researches of cancer, inflammayion, immunology and metabolic disease .
    Allolithocholic acid
  • HY-12502A
    Efonidipine hydrochloride monoethanolate
    1 Publications Verification

    NZ-105 hydrochloride monoethanolate; (±)-Efonidipine hydrochloride monoethanolate

    		 Calcium Channel SARS-CoV Cardiovascular Disease Neurological Disease Cancer
    Efonidipine (NZ-105) hydrochloride monoethanolate is an orally active dual L-type and T-type calcium channel blocker (CCB) with IC50 values of 1.8 and 350 nM, respectively. Efonidipine hydrochloride monoethanolate inhibits SARS-CoV-2 main protease. Efonidipine hydrochloride monoethanolate modulates adrenal steroidogenesis by increasing the expression of steroidogenic acute regulatory protein (StAR), dbcAMP-or angiotensin II-induced StAR mRNA expression and DHEA-S production, while suppressing the biosynthesis of aldosterone and cortisol. Efonidipine hydrochloride monoethanolate reduces plasma aldosterone levels in vivo. Efonidipine hydrochloride monoethanolate improves cardiac function in heart failure models by inhibiting T-type calcium channels (via both tonic and use-dependent blockade), independently of blood pressure reduction. Efonidipine hydrochloride monoethanolate can be used for research in hypertension, heart failure, and disorders involving dysregulated steroid hormone synthesis .
    Efonidipine hydrochloride monoethanolate
  • HY-163944
    LL-K12-18

    		DNA/RNA Synthesis Molecular Glues CDK Apoptosis RAD51 ATM/ATR PARP Cancer
    LL-K12-18 is a CDK12 kinase inhibitor and a dual-site molecular glue. LL-K12-18 inhibits human CDK12 with an IC50 value of 283.9 nM, and selectively degrades cyclin K via the ubiquitin-proteasome system by stabilizing the CDK12-DDB1 complex. LL-K12-18 downregulates DNA damage response genes, reduces the phosphorylation level of CTD Ser2 in RNA polymerase II, and modulates biomarkers such as ATM, RAD51, γ-H2AX and cleaved PARP, thereby effectively inducing apoptosis and inhibiting proliferation of breast cancer cells. LL-K12-18 exhibits high target selectivity and serves as a research tool for studies on triple-negative breast cancer .
    LL-K12-18
  • HY-12502
    Efonidipine
    1 Publications Verification

    NZ-105; (±)-Efonidipine

    		 Calcium Channel SARS-CoV Cardiovascular Disease Neurological Disease Cancer
    Efonidipine (NZ-105) is an orally active dual L-type and T-type calcium channel blocker (CCB) with IC50 values of 1.8 and 350 nM, respectively. Efonidipine inhibits SARS-CoV-2 main protease. Efonidipine modulates adrenal steroidogenesis by increasing the expression of steroidogenic acute regulatory protein (StAR), dbcAMP-or angiotensin II-induced StAR mRNA expression and DHEA-S production, while suppressing the biosynthesis of aldosterone and cortisol. Efonidipine reduces plasma aldosterone levels in vivo. Efonidipine improves cardiac function in heart failure models by inhibiting T-type calcium channels (via both tonic and use-dependent blockade), independently of blood pressure reduction. Efonidipine can be used for research in hypertension, heart failure, and disorders involving dysregulated steroid hormone synthesis .
    Efonidipine
  • HY-116273
    ML299

    		Phospholipase Cancer
    ML299 is a selective allosteric modulator and a dual inhibitor of phospholipases D1 and D2 (IC50 values are 6 and 12 nM, respectively). ML299 decreases invasive migration in U87-MG glioblastoma cells .
    ML299
  • HY-178281
    E0199

    		Potassium Channel Sodium Channel Neurological Disease
    E0199 is a novel potent dual-target KV7/NaV modulator that activates the KV7 channel (KV7.2/7.3 (EC50 = 12.78 nM), KV7.2 (EC50 = 0.50 μM), and KV7.5 (EC50 = 27.14 nM) channels) while simultaneously blocks the NaV1.7 (IC50 = 0.52 μM), NaV1.8 (IC50 = 0.24 μM), and NaV1.9 (IC50 = 0.16 μM) channels. E0199 shows a potent analgesic effect without affecting heart and skeletal muscle ion channels critically in a chronic constriction injury (CCI) mouse model. E0199 can be used for Neuropathic pain (NP) research .
    E0199
  • HY-170944
    BAG3/HSP70-IN-1

    		HSP Apoptosis Caspase Cancer
    BAG3/HSP70-IN-1 (compound 16) is the first-in-class BAG3 and HSP70 dual inhibitor. BAG3/HSP70-IN-1 binds to BAG3 full-length, BAG3-BD, and HSP70 proteins with Kds of 33.10 μM, 27.90 μM, and 33.80 μM, respectively. BAG3/HSP70-IN-1 inhibits HeLa cells with an IC50 of 49.46 μM. BAG3/HSP70-IN-1 induces apoptosis by activating caspase 3 and caspase 9 levels in HeLa cells. BAG3/HSP70-IN-1 elevates p21 levels while reduces FOXM1 expression in HeLa cells. BAG3/HSP70-IN-1 decreases ATPase activity .
    BAG3/HSP70-IN-1
  • HY-124478
    Ethyl gentisate

    Ethyl 2,5-dihydroxybenzoate

    		 Phosphatase Metabolic Disease
    Ethyl gentisate (Ethyl 2,5-dihydroxybenzoate) is a dual modulator for cell differentiation, that enhances the osteogenic differentiation of human mesenchymal stem cells (hMSCs) and alkaline phosphatase activity, inhibits RANKL-activated osteoclastogenesis in RAW264.7 cells, and balances the bone remodeling process .
    Ethyl gentisate
  • HY-144501
    D18

    		Toll-like Receptor (TLR) PD-1/PD-L1 Inflammation/Immunology Cancer
    D18 is an immune modulator. D18 acts as a TLR7/8 dual agonist (EC50 = 24 nM for hTLR7 and 10 nM for hTLR8, respectively). D18 increases PD-L1 expression through epigenetic regulation, thus sensitizing tumors to PD-1/PD-L1 blockade. D18 is a ADC cytotoxin uesd for the systhesis of ADC HE-S2 (HY-144497). D18 has strong immune activation and anti-tumor activity. D18 commonly used in cancer research, such as colon cancer .
    D18
  • HY-148629
    GDC-0134

    		JNK Neurological Disease
    GDC-0134 (RG6000) is a modulator targeting dual leucine zipper kinase (DLK) that can cross the blood-brain barrier. By inhibiting the kinase activity of DLK, GDC-0134 blocks the activation of the downstream JNK signaling pathway, suppresses DLK-dependent retrograde signal transduction of axon-to-soma degeneration, and exerts neuroprotective activity. GDC-0134 reduces TDP-43 protein aggregation and decreases the degree of neuromuscular junction denervation in motor neurons. GDC-0134 can be used in the research of amyotrophic lateral sclerosis (ALS), Alzheimer's disease and other DLK-related neurodegenerative diseases .
    GDC-0134
  • HY-152254
    CB2R/FAAH modulator-3

    		FAAH Cannabinoid Receptor Infection Neurological Disease Inflammation/Immunology Cancer
    CB2R/FAAH modulator-3 (compound 27) is a dual targeting modulator that acts as a CB2R agonist and FAAH inhibitor. The Ki values for CB2R/FAAH modulator-3 are 20.1 and 67.6 nM for CB2R and CB1R, respectively, and the IC50 value for FAAH is 3.4 μM. CB2R/FAAH modulator-3 can be used in studies related to cancer, deleterious inflammatory cascades occurring in neurodegenerative diseases, and COVID-19 infection .
    CB2R/FAAH modulator-3
  • HY-128677
    NCC007

    		Casein Kinase Neurological Disease
    NCC007 is a dual casein kinase Iα (CKIα) and δ (CKIδ) inhibitor with IC50s of 1.8 and 3.6 μM, respectively. NCC007 can be used in research of modulating mammalian circadian rhythms .
    NCC007
  • HY-177515
    IRAK4 modulator-2

    		IRAK STAT JAK NF-κB Inflammation/Immunology
    IRAK4 modulator-2 (Compound 5) is a selective dual Interleukin-1 Receptor Associated Kinase 4 (IRAK4) and IRAK1 inhibitor with IC50 values of 0.005 μM and 0.97 μM, erespectively. IRAK4 modulator-2 blocks IRAK-mediated signaling pathways (e.g., JAK-STAT, NF-κB pathways), reduces the production of pro-inflammatory cytokines (e.g., IL-1, TNF), and exerts anti-inflammatory activity. IRAK4 modulator-2 is promising for research of autoimmune diseases and inflammatory diseases, such as rheumatoid arthritis, psoriasis, inflammatory bowel disease .
    IRAK4 modulator-2
  • HY-149831
    ZLY28

    		FXR Metabolic Disease
    ZLY28 is the first-in-class intestinal restricted and orally active FXR and FABP1 dual modulator. ZLY28 also is a novel anti-NASH agent. ZLY28 can be used for the research of nonalcoholic steatohepatitis (NASH) .
    ZLY28
  • HY-155672
    JPC0323

    		5-HT Receptor Neurological Disease
    JPC0323 is a dual 5-HT2C/5-HT2A receptor positive allosteric modulator. JPC0323 has on-target properties, acceptable plasma exposure and brain penetration. JPC0323 can be used for the research of neurological disease .
    JPC0323
  • HY-176287
    ARN25657

    		Dopamine Receptor GSK-3 PKA P-glycoprotein Neurological Disease
    ARN25657 is a dual-acting D3R/GSK-3β modulator. ARN25657 has both partial D3R agonist activity (EC50 = 15.2 nM, Ki =1.5 nM) and potent GSK-3β inhibitor activity (IC50 = 19.3 nM). ARN25657 exhibits excellent GSK-3β selectivity over FYN, PKA, and CDK5/p35. ARN25657 inhibits P-glycoprotein (P-gP)-mediated acetoxymethyl calcein efflux and improves in vitro ADME properties while maintaining a balanced dual-target profile. ARN25657 is useful for studying bipolar disorder and related neuropsychiatric disorders .
    ARN25657
  • HY-176561
    IOR-160

    		Casein Kinase HDAC Cancer
    IOR-160 is a dual inhibitor of casein kinase 2 (CK2) and HDACs. IOR-160 exhibits high selectivity for CK2 (IC50 = 1.7 nM) and broad inhibitory activity against HDAC (HDAC 1, 2, 3, and 6 with IC50s of 3.3 nM, 24.0 nM, 3.9 nM, and 13.0 nM, respectively, with low activity for HDAC8). IOR-160 modulates key cellular signaling pathways by inhibiting AKT phosphorylation and increasing acetylated α-tubulin. IOR-160 inhibits tumor growth and reduces tumor burden through dual CK2/HDAC inhibition. IOR-160 is indicated for use in triple-negative breast cancer research .
    IOR-160
  • HY-178716
    PTPN2/1-IN-4

    		Phosphatase IFNAR STAT JAK Cancer
    PTPN2/1-IN-4 (Compound WS35) is an orally active, dual-functional inhibitor of PTPN1 and PTPN2 with IC50s of 12.8 and 5.8 nM for PTPN1 and PTPN2, respectively. PTPN2/1-IN-4 modulates the IFNγ-JAK-STAT signaling pathway and significantly augments CD8+ T-cell tumor infiltration. PTPN2/1-IN-4 has potent anticancer activity, robustly inhibiting tumor growth both as a monotherapy and in combination with an anti-PD-1 antibody in B16-OVA syngeneic mouse models .
    PTPN2/1-IN-4
  • HY-114863
    PHCCC(4Me)

    THCCC

    		 mGluR Neurological Disease
    PHCCC(4Me) (THCCC), a PHCCC analog, is a dual mGluR2 (IC50 of 1.5 μM) negative allosteric modulator and mGluR3 (EC50 of 8.9 μM) positive allosteric modulator .
    PHCCC(4Me)
  • HY-147361
    LDCA

    		Apoptosis Lactate Dehydrogenase Cancer
    LDCA is a dual-hit metabolic modulator and inhibits LDH-A enzyme activity to stimulate apoptosis in the malignant population. LDCA can be used for the research of oncogenic progression .
    LDCA
  • HY-152253
    CB2R/FAAH modulator-2

    		FAAH Cannabinoid Receptor Infection Neurological Disease Inflammation/Immunology Cancer
    CB2R/FAAH modulator-2 (compound 26) is a dual targeting modulator that acts as a CB2R agonist and FAAH inhibitor. The Ki values for CB2R/FAAH modulator-2 are 10.8 and 152.9 nM for CB2R and CB1R, respectively, and the IC50 value for FAAH is 6.2 μM. CB2R/FAAH modulator-2 can be used in studies related to cancer, deleterious inflammatory cascades occurring in neurodegenerative diseases, and COVID-19 infection .
    CB2R/FAAH modulator-2
  • HY-117965
    Miricorilant

    CORT 118335

    		 Glucocorticoid Receptor Mineralocorticoid Receptor Endocrinology
    Miricorilant (CORT 118335) is a dual selective glucocorticoid (GR) modulator/mineralocorticoid (MR) antagonist. Miricorilant can be used for the research of hypothalamic-pituitary-adrenal (HPA) axis related disorders .
    Miricorilant
  • HY-176731
    MSK-9

    		P2X Receptor Neurological Disease
    MSK-9 is a positive allosteric modulator of the P2X4 receptor with dual activities of enhancing ion conductance and delaying receptor inactivation. MSK-9 stabilizes the open state of the P2X4 receptor through rigid 3-piperidinyl and hydrophobic menthyl substituents. MSK-9 can be used in the study of multiple sclerosis (MS) .
    MSK-9
  • HY-178470
    IDO1/TDO-IN-10

    		Indoleamine 2,3-Dioxygenase (IDO) Inflammation/Immunology Cancer
    IDO1/TDO-IN-10 (Compound G-14) is a dual IDO1 (EC50=3.07 μM) and TDO (EC50=9.7 μM) inhibitor. IDO1/TDO-IN-10 inhibits the conversion of tryptophan to kynurenine and modulates immune responses while reducing inflammatory reactions. IDO1/TDO-IN-10 is promising for research of cancers and inflammatory diseases .
    IDO1/TDO-IN-10
  • HY-143712S1
    Allolithocholic Acid-d4

    3α-hydoxy-5α-Cholaoic Acid-d4, allo-LCA-d4

    		 Isotope-Labeled Compounds Drug Metabolite G protein-coupled Bile Acid Receptor 1 ROR Metabolic Disease Inflammation/Immunology Cancer
    Allolithocholic Acid-d4 (3α-hydoxy-5α-Cholaoic Acid-d4, allo-LCA-d4) is deuterium labeled Allolithocholic acid (HY-143712). Allolithocholic acid is an orally active metabolite of Lithocholic acid (HY-B0172). Allolithocholic acid is a dual GPBAR1 agonist (EC50 = 2.7 μM) and RORγt inverse agonist (IC50 = 3.4 μM). Allolithocholic acid modulates immune and metabolic pathways, regulates immune cell polarization, prevents M1 macrophage and Th17 CD4 cell polarization. Allolithocholic acid improves insulin sensitivity, reduces liver lipid accumulation, reverses liver immunological, inflammatory and metabolic signaling dysregulation, restores bile acid homeostasis, adipose tissue histopathology/function, and intestinal microbiota composition, modulates intestinal immunity. Allolithocholic acid can be used for the researches of cancer, inflammayion, immunology and metabolic disease .
    Allolithocholic Acid-d4
  • HY-12502B
    Efonidipine hydrochloride

    NZ-105 hydrochloride; (±)-Efonidipine hydrochloride

    		 Calcium Channel SARS-CoV Cardiovascular Disease Cancer
    Efonidipine (NZ-105) hydrochloride is an orally active dual L-type and T-type calcium channel blocker (CCB) with IC50 values of 1.8 and 350 nM, respectively. Efonidipine hydrochloride inhibits SARS-CoV-2 main protease. Efonidipine hydrochloride modulates adrenal steroidogenesis by increasing the expression of steroidogenic acute regulatory protein (StAR), dbcAMP-or angiotensin II-induced StAR mRNA expression and DHEA-S production, while suppressing the biosynthesis of aldosterone and cortisol. Efonidipine hydrochloride reduces plasma aldosterone levels in vivo. Efonidipine hydrochloride improves cardiac function in heart failure models by inhibiting T-type calcium channels (via both tonic and use-dependent blockade), independently of blood pressure reduction. Efonidipine hydrochloride can be used for research in hypertension, heart failure, and disorders involving dysregulated steroid hormone synthesis .
    Efonidipine hydrochloride
  • HY-165587
    BM-573

    		Prostaglandin Receptor Cardiovascular Disease
    BM-573 is an orally active dual thromboxane A₂ (TXA₂) modulator with an IC50 of 1.3 nM. BM-573 possesses both thromboxane synthase (TxAS) inhibition and thromboxane receptor (TP) antagonistic effects. BM-573 can completely inhibit platelet aggregation induced by Arachidonic acid (HY-109590) or U-46619 (TXA₂ analogues). BM-573 completely blocks the generation of TXB₂ (the stable metabolite of TXA₂) in human platelets and does not inhibit cyclooxygenase (COX-1/COX-2), thus avoiding interference with other prostaglandin synthesis. BM-573 has an inhibitory effect on U-46619-induced contractions in rat gastric fundus smooth muscle (ED₅₀ = 4.2 μM), but has no effect on contractions caused by PGE₂, PGF₂α, or PGI₂. BM-573 can be used in the study of atherosclerosis, myocardial infarction, pulmonary hypertension and shock .
    BM-573
  • HY-178332
    sEH/PPARδ modulator 1

    		Epoxide Hydrolase PPAR Cardiovascular Disease Metabolic Disease Inflammation/Immunology
    sEH/PPARδ modulator 1 is a sEH/PPARδ dual modulator. sEH/PPARδ modulator 1 can inhibit sEH with an IC50 of 0.46 μM and activate PPARδ with an EC50 of 0.12 μM. sEH/PPARδ modulator 1 can be used for the researches of inflammation, metabolic and cardiovascular disease .
    sEH/PPARδ modulator 1
  • HY-169964
    TSPO/Carbonic Anhydrase Modulator 1

    		Carbonic Anhydrase Neurological Disease
    TSPO/Carbonic Anhydrase Modulator 1 (Compound 3) is a dual modulator for mitochondrial translocator protein and Carbonic Anhydrase with a Ki of 1.340 μM for TSPO and a KA of 10.7 μM for CA VII. TSPO/Carbonic Anhydrase Modulator 1 promotes the production of neurosteroid, increases BDNF gene expression, exhibits neuroprotective efficacy .
    TSPO/Carbonic Anhydrase Modulator 1
  • HY-118397
    RB394

    		PPAR Others
    RB394 is a potent dual sEH/PPARγ modulator isoform that promotes adipocyte browning and exhibits cardioprotective activity, and can be used to suppress metabolic syndrome.
    RB394
  • HY-151963
    PPARγ/GR modulator 1

    		PPAR Glucocorticoid Receptor Metabolic Disease
    PPARγ/GR modulator 1 is an orally active dual agonist of PPARγ and glucocorticoid receptor (GR), with Kis of 3.3 and 33.6 μM, respectively. PPARγ/GR modulator 1 can be used for the research of metabolic diseases, such as diabetes .
    PPARγ/GR modulator 1
  • HY-172231
    Hexolame

    		Estrogen Receptor/ERR Cardiovascular Disease Cancer
    Hexolame is an estrogen receptors agonist with dual anticoagulant and estrogenic properties. Hexolame binds to estrogen receptors to induce anticoagulant effects by modulating clotting factors or platelet activity. Hexolame is promising for research of prostatic cancer and prevention of thrombosis .
    Hexolame
  • HY-159484
    Hsp110/sGC-modulator-1

    		HSP Guanylate Cyclase Cardiovascular Disease
    Hsp110/sGC-modulator-1 (compound 17i), an orally active Hsp110/sGC dual-target regulator, exhibits optimal Hsp110 and sGC molecular activities as well as remarkable cell malignant phenotypes inhibitory and vasodilatory effects. Hsp110/sGC-modulator-1 (compound 17i) attenuates pulmonary vascular remodeling and right ventricular hypertrophy via Hsp110 suppression .
    Hsp110/sGC-modulator-1
  • HY-121736
    AGI-12026

    AGI-026

    		 Isocitrate Dehydrogenase (IDH) Neurological Disease
    AGI-12026 is brain-penetrant dual inhibitor of mutant IDH1 and 2. AGI-12026 shows partial inhibition of the IDH1-R132H homodimer as allosteric modulators. AGI-12026 has the potential for research of glioma .
    AGI-12026
  • HY-163065
    σ1 Receptor/μ Opioid receptor modulator 2

    		Opioid Receptor Sigma Receptor Neurological Disease
    σ1 Receptor/μ Opioid receptor modulator 2 (compound 4x) is a dual μOR agonist/σ1R antagonist, and displays picomolar μOR agonism activity (EC50: 0.6 ± 0.2 nM) and good σ1R inhibitory activity (Ki: 363.7 ± 5.6 nM). σ1 Receptor/μ Opioid receptor modulator 2 exhibits robust analgesic effects in various pain models .
    σ1 Receptor/μ Opioid receptor modulator 2
  • HY-123773
    SR-16157

    NSC 732011; HLX-801

    		 Steroid Sulfatase Estrogen Receptor/ERR Cancer
    SR-16157 (NSC 732011; HLX-801) is a dual-action steroid sulfatase (STS) inhibitor (IC50 = 0.1 uM) and selective ERα modulator. SR-16157 exhibits STS inhibitory and anti-estrogenic effects in breast cancer cells. SR-16157 may be used in breast cancer research .
    SR-16157
  • HY-158627
    JPC0323 Oleate

    		5-HT Receptor Others
    JPC0323 Oleate is a derivative of JPC0323 (HY-155672). JPC0323 is a dual 5-HT2C/5-HT2A receptor positive allosteric modulator. JPC0323 has on-target properties, acceptable plasma exposure and brain penetration. JPC0323 can be used for the research of neurological disease .
    JPC0323 Oleate
  • HY-117459
    E-3030 free acid

    		PPAR Metabolic Disease
    E-3030 free acid is a potent dual activator of peroxisome proliferator-activated receptor (PPAR) alpha and PPARgamma, exhibiting significant antidiabetic and lipid-modulating effects. E-3030 decreases blood glucose, triglyceride, non-esterified fatty acids, and insulin levels, while increasing blood adiponectin levels. E-3030 improves glucose tolerance and shows remarkable triglyceride- and non-high-density lipoprotein cholesterol-lowering effects in animal models.
    E-3030 free acid
  • HY-P11259
    UPG-111

    		Urotensin Receptor Cardiovascular Disease Metabolic Disease Inflammation/Immunology Cancer
    UPG-111 is a peptide compound that acts as a negative allosteric modulator of the Urotensin II receptor (UTR). UPG-111 exhibits a dual inhibitory effect on the vasoconstriction induced by UTR agonists - it reduces both the maximum response intensity and the sensitivity of the agonist. UPG-111 does not induce calcium release or cause contraction of the endothelium-deprived rat aortic rings. UPG-111 can be used for the study of various diseases related to the angiotensinergic system .
    UPG-111
  • HY-143712R
    Allolithocholic acid (Standard)

    		Reference Standards Drug Metabolite G protein-coupled Bile Acid Receptor 1 ROR Metabolic Disease Inflammation/Immunology Cancer
    Allolithocholic acid (Standard) is the analytical standard of Allolithocholic acid (HY-143712). This product is intended for research and analytical applications. Allolithocholic acid is an orally active metabolite of Lithocholic acid (HY-B0172). Allolithocholic acid is a dual GPBAR1 agonist (EC50 = 2.7 μM) and RORγt inverse agonist (IC50 = 3.4 μM). Allolithocholic acid modulates immune and metabolic pathways, regulates immune cell polarization, prevents M1 macrophage and Th17 CD4 cell polarization. Allolithocholic acid improves insulin sensitivity, reduces liver lipid accumulation, reverses liver immunological, inflammatory and metabolic signaling dysregulation, restores bile acid homeostasis, adipose tissue histopathology/function, and intestinal microbiota composition, modulates intestinal immunity. Allolithocholic acid can be used for the researches of cancer, inflammayion, immunology and metabolic disease .
    Allolithocholic acid (Standard)
  • HY-12502AR
    Efonidipine hydrochloride monoethanolate (Standard)

    NZ-105 hydrochloride monoethanolate (Standard); (±)-Efonidipine hydrochloride monoethanolate (Standard)

    		 Reference Standards Calcium Channel SARS-CoV Cardiovascular Disease
    Efonidipine (NZ-105) hydrochloride monoethanolate (Standard) is the analytical standard of Efonidipine hydrochloride monoethanolate (HY-12502AR). This product is intended for research and analytical applications. Efonidipine (NZ-105) hydrochloride monoethanolate is an orally active dual L-type and T-type calcium channel blocker (CCB) with IC50 values of 1.8 and 350 nM, respectively. Efonidipine hydrochloride monoethanolate inhibits SARS-CoV-2 main protease. Efonidipine hydrochloride monoethanolate modulates adrenal steroidogenesis by increasing the expression of steroidogenic acute regulatory protein (StAR), dbcAMP-or angiotensin II-induced StAR mRNA expression and DHEA-S production, while suppressing the biosynthesis of aldosterone and cortisol. Efonidipine hydrochloride monoethanolate reduces plasma aldosterone levels in vivo. Efonidipine hydrochloride monoethanolate improves cardiac function in heart failure models by inhibiting T-type calcium channels (via both tonic and use-dependent blockade), independently of blood pressure reduction. Efonidipine hydrochloride monoethanolate can be used for research in hypertension, heart failure, and disorders involving dysregulated steroid hormone synthesis .
    Efonidipine hydrochloride monoethanolate (Standard)
  • HY-134483
    5-HT7/5-HT2A receptor antagonist 1

    		5-HT Receptor Neurological Disease
    5-HT7/5-HT2A receptor antagonist 1 is a high-affinity, orally active, brain-penetrant 5-HT7 and 5-HT2A receptor ligand having a pKi = 8.1 at both receptors. 5-HT7/5-HT2A receptor antagonist 1 behaves as an antagonist in an in vitro functional assay for 5-HT2A and as an inverse agonist in an in vitro functional assay for 5-HT7. 5-HT7/5-HT2A receptor antagonist 1 blockade of 5-Carboxamidotryptamine (5-CT) (HY-135555) induced hypothermia in rats, and blockade of 2,5-dimethoxy-4-iodoamphetamine (DOI) induced head-twitches in mice. 5-HT7/5-HT2A receptor antagonist 1 occupied 5-HT2A receptor binding sites in the frontal cortex of the rat brain. 5-HT7/5-HT2A receptor antagonist 1 can be used for the study of Neurological diseases .
    5-HT7/5-HT2A receptor antagonist 1
  • HY-181616
    p53-Y220C/PLK1 modulator-1

    		MDM-2/p53 Polo-like Kinase (PLK) Cancer
    p53-Y220C/PLK1 modulator-1 (compound15) is a dual modulator targeting p53-Y220C and PLK1. p53-Y220C/PLK1 modulator-1 can be used in the cancer .
    p53-Y220C/PLK1 modulator-1
  • HY-183309
    FXR/HSD17B13-modulator-2

    		FXR 17β-HSD Inflammation/Immunology
    FXR/HSD17B13-modulator-2 is a dual FXR activator and HSD17B13 inhibitor with human FXR EC50 of 128 nM, human HSD17B13 IC50 of 0.18 μM, high selectivity over related nuclear receptors and HSD17B isoforms, and oral effectiveness.FXR/HSD17B13-modulator-2 alleviates fatty liver, regulates lipid metabolism, reduces inflammation, and attenuates hepatic fibrosis.FXR/HSD17B13-modulator-2 is the first non-carboxylic acid dual FXR/HSD17B13 modulator.FXR/HSD17B13-modulator-2 can be used for the research of metabolic dysfunction-associated steatohepatitis .
    FXR/HSD17B13-modulator-2
  • HY-180585
    LOXL2/sGC modulator-2

    		Monoamine Oxidase Guanylate Cyclase PKG Collagen Cardiovascular Disease
    LOXL2/sGC modulator-2 (Compound 9k) is a selective and orally active lysyl oxidase-like 2 (LOXL2) and soluble guanylate cyclase (sGC) dual-target regulator. LOXL2/sGC modulator-2 shows inhibitory activity for LOXL2 with an IC50 of 0.1 μM and can activate sGC. LOXL2/sGC modulator-2 can ameliorate vascular remodeling and reduce pulmonary artery pressure. LOXL2/sGC modulator-2 can downregulate PKG1, PCNA, α-SMA, collagen I and fibronectin levels. LOXL2/sGC modulator-2 can be used for the research of pulmonary arterial hypertension .
    LOXL2/sGC modulator-2
  • HY-182905
    SSTR5/TGR5-modulator-1

    		Somatostatin Receptor G protein-coupled Bile Acid Receptor 1 Metabolic Disease
    SSTR5/TGR5-modulator-1 is an orally active and dual-target small molecule, balanced in vitro activity at human TGR5 and human SSTR5. SSTR5/TGR5-modulator-1 activates human TGR5 to promote cAMP accumulation. SSTR5/TGR5-modulator-1 blocks human SSTR5 to inhibit agonist-induced calcium mobilization. SSTR5/TGR5-modulator-1 improves glucose tolerance in mice. SSTR5/TGR5-modulator-1 alleviates gallbladder filling in mice at pharmacologically relevant doses. SSTR5/TGR5-modulator-1 has suboptimal physicochemical and metabolic properties.SSTR5/TGR5-modulator-1 can be used for the research of type 2 diabetes mellitus .
    SSTR5/TGR5-modulator-1
  • HY-175742A
    (R)-BMS-986470

    		Drug Isomer Cardiovascular Disease
    (R)-BMS-986470 is the enantiomer of BMS-986470 (HY-175742). BMS-986470, a HbF-activating CRBN E3 ligase modulator (CELMoD), is an orally active dual molecular glue degrader targeting ZBTB7A and WIZ .
    (R)-BMS-986470
  • HY-122686
    USP25/28-IN-2

    		Deubiquitinase Apoptosis c-Myc Cancer
    USP25/28-IN-2 is a selectivity dual USP25/28 inhibitor with IC50 values of 0.88 and 1.1 μM, respectively. USP25/28-IN-2 modulates USP25 and USP28 activity to affect downstream pathways, modulates c-Myc oncoprotein total levels and half-life, induces apoptosis, reduces cell viability. USP25/28-IN-2 can be used for the research of colorectal carcinoma, colorectal adenocarcinoma .
    USP25/28-IN-2

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