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Results for "

cAMP inhibition

" in MedChemExpress (MCE) Product Catalog:

42

Inhibitors & Agonists

4

Peptides

2

Natural
Products

4

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13749
    Sitagliptin
    Maximum Cited Publications
    30 Publications Verification

    MK-0431

    		 Dipeptidyl Peptidase GLP Receptor Endogenous Metabolite PKA ERK Metabolic Disease
    Sitagliptin (MK-0431) is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin can be used for the study of 1-type and 2-type diabetes .
    Sitagliptin
  • HY-13749A
    Sitagliptin phosphate
    Maximum Cited Publications
    30 Publications Verification

    MK-0431 phosphate

    		 Dipeptidyl Peptidase GLP Receptor Endogenous Metabolite PKA ERK Metabolic Disease
    Sitagliptin (MK-0431) phosphate is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin phosphate blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin phosphate can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin phosphate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate can be used for the study of 1-type and 2-type diabetes .
    Sitagliptin phosphate
  • HY-13749B
    Sitagliptin phosphate monohydrate
    Maximum Cited Publications
    30 Publications Verification

    MK-0431 phosphate monohydrate

    		 Dipeptidyl Peptidase GLP Receptor Endogenous Metabolite PKA ERK Metabolic Disease
    Sitagliptin (MK-0431) phosphate monohydrate is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin phosphate monohydrate blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin phosphate monohydrate can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin phosphate monohydrate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate monohydrate can be used for the study of 1-type and 2-type diabetes .
    Sitagliptin phosphate monohydrate
  • HY-P0172
    ATI-2341
    4 Publications Verification

    		 CXCR Inflammation/Immunology Endocrinology Cancer
    ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) .
    ATI-2341
  • HY-B1898
    Metadoxine

    		PKA Metabolic Disease
    Metadoxine blocks adipocyte differentiation in association with inhibition of the protein kinase A-cAMP response element binding protein (PKA-CREB) pathway.
    Metadoxine
  • HY-P0172A
    ATI-2341 TFA
    4 Publications Verification

    		 CXCR Inflammation/Immunology Endocrinology Cancer
    ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) .
    ATI-2341 TFA
  • HY-108648A
    2-MeSADP

    2-Methylthioadenosine diphosphate; 2-Methylthio-ADP

    		 P2Y Receptor Neurological Disease
    2-MeSADP is a P2Y receptor agonist, with an EC50 of 5 nM for human P2Y12, EC50 values of 19 nM and 13 nM for human P2Y13, and an EC50 of 6.2 nM for mouse P2Y13. It shows slightly higher selectivity for P2Y12 over human P2Y13. 2-MeSADP triggers increases in intracellular calcium levels, Gi-mediated cAMP inhibition, adenylate cyclase inhibition and downstream signal transduction. 2-MeSADP can be used in research related to glaucoma .
    2-MeSADP
  • HY-101189
    JNJ-39758979

    		Histamine Receptor Neurological Disease Endocrinology
    JNJ-39758979, a chemical probe, is a selective, orally active, and high-affinity histamine H4 receptor antagonist with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 shows good anti-inflammatory and antipruritic activity .
    JNJ-39758979
  • HY-13749AS
    Sitagliptin-d4 phosphate

    MK-0431-d4 phosphate

    		 Dipeptidyl Peptidase GLP Receptor Endogenous Metabolite PKA ERK Metabolic Disease
    Sitagliptin-d4 phosphate (MK-0431-d4) is the deuterium labeled Sitagliptin phosphate (HY-13749A). Sitagliptin phosphate is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin phosphate blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin phosphate can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin phosphate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate can be used for the study of 1-type and 2-type diabetes.
    Sitagliptin-d4 phosphate
  • HY-134299
    8-CPT-cAMP-AM

    8-(4-Chlorophenylthio)-cAMP-AM

    		 Ras PKA Cardiovascular Disease Metabolic Disease Cancer
    8-CPT-cAMP-AM (8-(4-Chlorophenylthio)-cAMP-AM) is an Epac/PKA activator. 8-CPT-cAMP-AM potentiates glucose-dependent first- and second-phase insulin secretion, induces β-cell depolarization, modulates intracellular calcium via influx and ryanodine-sensitive store mobilization, and facilitates calcium-induced calcium release resistant to PKA inhibition. 8-CPT-cAMP-AM can be used for the research of cardiac hypertrophy, diabetic cardiomyopathy, and melanoma .
    8-CPT-cAMP-AM
  • HY-P1597
    Malantide
    1 Publications Verification

    		 PKA PKC Cancer
    Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide is a highly specific substrate for PKA with a Km of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts . Malantide is also an efficient substrate for PKC with a Km of 16 μM .
    Malantide
  • HY-163996
    DD202-114

    		GLP Receptor Potassium Channel Cytochrome P450 Metabolic Disease
    DD202-114 is a potent and selective GLP1R agonist. DD202-114 inhibits hERG with an IC50 of 15.9 μM. DD202-114 exhibits strong CYP2C8 inhibition with an IC50 of 0.22 μM. DD202-114 promotes cAMP accumulation. DD202-114 reduces blood glucose levels and food intake. DD202-114 has the potential to be used in the study of type 2 diabetes mellitus (T2DM) and obesity .
    DD202-114
  • HY-13749S1
    Sitagliptin-d4 hydrochloride

    MK-0431-d4 hydrochloride

    		 Isotope-Labeled Compounds Dipeptidyl Peptidase GLP Receptor Endogenous Metabolite PKA ERK Metabolic Disease
    Sitagliptin-d4 hydrochloride is the deuterium labeled Sitagliptin hydrochloride (HY-13749E). Sitagliptin hydrochloride is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin hydrochloride blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin hydrochloride can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin hydrochloride shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin hydrochloride can be used for the study of 1-type and 2-type diabetes.
    Sitagliptin-d4 hydrochloride
  • HY-N12378
    β-Patchoulene

    		NF-κB Toll-like Receptor (TLR) PKA Epigenetic Reader Domain Keap1-Nrf2 Sirtuin AMPK Caspase FASTK ERK ROCK Apoptosis Metabolic Disease Inflammation/Immunology Cancer
    β-Patchoulene is an orally active anti-inflammatory, antioxidant, and anti-apoptotic agent. β-Patchoulene inhibits the NF-κB, TLR4, and cAMP/PKA/CREB signaling pathways; activates the Sirt1/Nrf2 and AMPK signaling pathways; and targets Fas/FasL, Caspase-3, ERK1/2, ROCK1/MLC2 for inhibition. β-Patchoulene regulates cytokine secretion, inflammatory cell infiltration, lipid peroxidation, cell polarization, gut microbiota, and lipid metabolism, restores barrier function, mitochondrial function, and cell viability, and exhibits repellent activity against Spodoptera exigua larvae. β-Patchoulene can be used in research related to various inflammatory, ischemic, fibrosis-associated diseases, as well as hepatocellular carcinoma .
    β-Patchoulene
  • HY-111527
    PPZ2

    		Calcium Channel Neurological Disease
    PPZ2 is a diacylglycerol (DAG)-activated TRPC3/TRPC6/TRPC7 channel activator with activity in promoting neuronal development and survival. PPZ2 activates recombinant TRPC3/TRPC6/TRPC7 channels in a dose-dependent manner without affecting other TRPC channels. PPZ2 elicits cation currents and calcium ion (Ca(2+)) influx in cultured central neurons. PPZ2 is able to induce BDNF-like neurite outgrowth and neuroprotection, an effect that disappears after TRPC3/TRPC6/TRPC7 knockdown or inhibition. PPZ2 also increases the activation of the calcium-dependent transcription factor cAMP response element binding protein. The effects of PPZ2 suggest that calcium signaling mediated by activation of DAG-activated TRPC channels plays an important role in its neurotrophic effects .
    PPZ2
  • HY-125782
    15(R)​-​15-​Methyl prostaglandin D2

    15(R)-15-Methyl PGD2

    		 Prostaglandin Receptor Metabolic Disease
    15(R)-15-Methyl prostaglandin D2 (15(R)-15-methyl PGD2) is a metabolically stable synthetic analog of PGD2. The physiological actions of PGD2 include regulation of sleep, lowering of body temperature, inhibition of platelet aggregation and relaxation of vascular smooth muscle. PGD2 mediates its effects by 2 distinct G-protein-coupled receptors, DP1and CRTH2/DP2. 15(R)-15-Methyl prostaglandin D2 is a potent, selective agonist for the CRTH2/DP2 receptor. The EC50 values for eosinophil CD11b expression, actin polymerization, and chemotaxis are 1.4, 3.8, and 1.7 nM, respectively, each of which is approximately 3-5 fold lower than those for PGD2. In contrast the EC50 for the DP1-mediated increase in platelet cAMP by 15(R)-15-methyl PGD2 is >10 μM.
    15(R)​-​15-​Methyl prostaglandin D2
  • HY-177122
    Raxlaprazine etomoxil

    		Dopamine Receptor Neurological Disease
    Raxlaprazine etomoxil is a small molecule compound with dopamine D2 and D3 receptor modulating activity, which has potential application value in research related to mental illnesses. Raxlaprazine etomoxil exhibits high affinity for human recombinant D2L receptors, with an inhibition constant (Ki) of 1.95 nM. Raxlaprazine etomoxil effectively inhibits forskolin-stimulated cAMP accumulation, with an half maximal effective concentration (EC50) of 3.72 nM in functional activity experiments .
    Raxlaprazine etomoxil
  • HY-120826
    A2AAR/hMAO-B-IN-1

    		Monoamine Oxidase Adenosine Receptor Neurological Disease
    A2AAR/hMAO-B-IN-1 (compoudn 17) is a non-xanthine dual-target inhibitor targeting the A2A adenosine receptor (A2AAR) (IC50: 34.9 nM) andMAO-B (Ki: 39.5 nM, human). A2AAR/hMAO-B-IN-1 inhibits A2AAR-induced cAMP accumulation and exhibits competitive, reversible inhibition of MAO-B. A2AAR/hMAO-B-IN-1 can be used in the study of neurodegenerative diseases such as Parkinson's disease (PD) .
    A2AAR/hMAO-B-IN-1
  • HY-13749E
    Sitagliptin hydrochloride

    MK-0431 hydrochloride

    		 Dipeptidyl Peptidase GLP Receptor Endogenous Metabolite PKA ERK Metabolic Disease
    Sitagliptin (MK-0431) hydrochloride is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin hydrochloride blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin hydrochloride can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin hydrochloride shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin hydrochloride can be used for the study of 1-type and 2-type diabetes .
    Sitagliptin hydrochloride
  • HY-123534
    CYT-1010

    		Opioid Receptor Neurological Disease
    CYT-1010 is a mu-opioid receptor agonist extracted from patent WO2013173730A2, with EC50s of 13.1 nM and 0.0053 nM on beta-arrestin recruitment and inhibition of cAMP production, respectively .
    CYT-1010
  • HY-123534A
    CYT-1010 hydrochloride

    		Opioid Receptor Neurological Disease
    CYT-1010 hydrochloride is a mu-opioid receptor agonist extracted from patent WO2013173730A2, with EC50s of 13.1 nM and 0.0053 nM on beta-arrestin recruitment and inhibition of cAMP production, respectively .
    CYT-1010 hydrochloride
  • HY-116540A
    L 858051 dihydrochloride

    7DMB-Forskolin

    		 Adenylate Cyclase Cardiovascular Disease
    L 858051 (7DMB-Forskolin) dihydrochloride, an analog of Forskolin (HY-15371), is an adenylyl cyclase stimulator. L 858051 dihydrochloride directly activates adenylyl cyclase to increase intracellular, cellular, and ciliary cAMP levels. L 858051 dihydrochloride activates recombinant cyclic nucleotide-gated (E583M CNGA2) channels to induce a non-selective, Mg 2+-sensitive current in adult rat ventricular myocytes. L 858051 dihydrochloride maximally stimulates L-type Ca 2+ current in adult rat ventricular myocytes. L 858051 dihydrochloride increases total PDE3 and PDE4 activities in adult rat ventricular myocytes, with effects insensitive to PKA inhibition. L 858051 dihydrochloride serves as a tool to elevate intracellular cAMP for studying subsarcolemmal cAMP dynamics and compartmentation in adult rat ventricular myocytes .
    L 858051 dihydrochloride
  • HY-132993
    Hcyb1

    		Phosphodiesterase (PDE) Neurological Disease
    Hcyb1 is a highly selective, orally active PDE2 inhibitor. Hcyb1 has a highly selective inhibition of PDE2A (IC50=0.57 μM) and over 250-fold selectivity against other recombinant PDE family members. Hcyb1 produces neuroprotective and antidepressant‐like effects most likely mediated by cAMP/cGMP-CREB-BDNF signaling .
    Hcyb1
  • HY-119114
    E-2508 free base

    		CRFR Neurological Disease
    E-2508 free base is an orally active and highly selective corticotropin-releasing factor type 1 receptor (CRF1) antagonist with anxiolytic effects (Ki=11 nM). E-2508 free base blocks CRF-induced cAMP accumulation via CRF1 receptor inhibition. E-2508 free base is promising for research of stress-related psychiatric disorders, such as anxiety and depression .
    E-2508 free base
  • HY-13749R
    Sitagliptin (Standard)

    MK-0431 (Standard)

    		 Reference Standards Dipeptidyl Peptidase GLP Receptor Endogenous Metabolite PKA ERK Metabolic Disease
    Sitagliptin (Standard) is the analytical standard of Sitagliptin (HY-13749). This product is intended for research and analytical applications. Sitagliptin is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin can be used for the study of 1-type and 2-type diabetes.
    Sitagliptin (Standard)
  • HY-150056
    CB1R Allosteric modulator 3

    		Cannabinoid Receptor Arrestin Neurological Disease
    CB1R Allosteric modulator 3 is a CB1R positive allosteric modulator. CB1R Allosteric modulator 3 has potent inhibition of cAMP and β-Arrestin with EC50 values of 0.018 μM and 1.241 μM, respectively .
    CB1R Allosteric modulator 3
  • HY-116540
    L 858051

    7DMB-Forskolin free base

    		 Adenylate Cyclase Cardiovascular Disease
    L 858051 (7DMB-Forskolin free base), an analog of Forskolin (HY-15371), is an adenylyl cyclase stimulator. L 858051 directly activates adenylyl cyclase to increase intracellular, cellular, and ciliary cAMP levels. L 858051 activates recombinant cyclic nucleotide-gated (E583M CNGA2) channels to induce a non-selective, Mg 2+-sensitive current in adult rat ventricular myocytes. L 858051 maximally stimulates L-type Ca 2+ current in adult rat ventricular myocytes. L 858051 increases total PDE3 and PDE4 activities in adult rat ventricular myocytes, with effects insensitive to PKA inhibition. L 858051 serves as a tool to elevate intracellular cAMP for studying subsarcolemmal cAMP dynamics and compartmentation in adult rat ventricular myocytes .
    L 858051
  • HY-153542
    AP-C6

    		PKG Others
    AP-C6 is a potent inhibitor of guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII) with a pIC50 of 6.5. AP-C6 concentration-dependently inhibits human cGKII activity in vitro. AP-C6 potentiate cAMP signaling by PDE inhibition .
    AP-C6
  • HY-P1597A
    Malantide TFA

    		PKA PKC Cancer
    Malantide TFA is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide TFA is a highly specific substrate for PKA with a Km of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts . Malantide TFA is also an efficient substrate for PKC with a Km of 16 μM .
    Malantide TFA
  • HY-101189B
    JNJ-39758979 dihydrochloride

    		Histamine Receptor Inflammation/Immunology
    JNJ-39758979 dihydrochloride is a selective, orally active, and high-affinity histamine H4 receptor antagonist, with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 dihydrochloride functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 dihydrochloride shows good anti-inflammatory and antipruritic activity .
    JNJ-39758979 dihydrochloride
  • HY-130176
    UFP-512

    		Opioid Receptor ERK Adenylate Cyclase Neurological Disease
    UFP-512 is a selective and potent σ-opioid receptor (DOP receptor) peptidic agonist with antidepressant- and anxiolytic-like effects. UFP-512 exhibits as a potent agonist on adenylyl cyclase inhibition and Erk1/2 activation. UFP-512 induces phosphorylation of DOP receptors on Ser 363 with a low desensitization of the cAMP pathway. UFP-512 is promising for research of mood disorders .
    UFP-512
  • HY-114539
    L-750667 triHydrochloride

    		Dopamine Receptor Neurological Disease
    L-750667 triHydrochloride is a selective antagonist for the D4 dopamine receptor, with a Ki value of 0.51 nM. The radiolabeled form of L-750667, [ 125I]L-750,667, has a Kd value of 0.16 nM for the D4 receptor. L-750667 triHydrochloride can reverse dopamine-induced inhibition of cAMP accumulation. It can be used to study the distribution and function of D4 dopamine receptors in the central nervous system and has potential applications in the fields of neuroscience and psychiatry .
    L-750667 triHydrochloride
  • HY-171069
    FFA2 agonist-1

    		Free Fatty Acid Receptor Metabolic Disease
    FFA2 agonist-1 (Compound 4) is the agonist for Free fatty acid receptor 2 (FFA2/GPR43) with an EC50 of 81 nM. FFA2 agonist-1 exhibits activity in β-arrestin-2 recruitment assay and cAMP inhibition assay with EC50 of 1.2 μM and 0.53 μM. FFA2 agonist-1 leads to appetite regulating peptide YY (PYY) mucosal responses, inhibits the fat accumulation, intestinal functions and food intake, and can be used for obesity research .
    FFA2 agonist-1
  • HY-13749AR
    Sitagliptin phosphate (Standard)

    MK-0431 phosphate (Standard)

    		 Reference Standards Dipeptidyl Peptidase GLP Receptor Endogenous Metabolite PKA ERK Metabolic Disease
    Sitagliptin (MK-0431) phosphate (Standard) is the analytical standard of Sitagliptin phosphate (HY-13749A). This product is intended for research and analytical applications. Sitagliptin phosphate is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin phosphate blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin phosphate can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin phosphate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate can be used for the study of 1-type and 2-type diabetes.
    Sitagliptin phosphate (Standard)
  • HY-13749S2
    Sitagliptin-d4

    MK-0431-d4

    		 Isotope-Labeled Compounds Dipeptidyl Peptidase GLP Receptor Endogenous Metabolite PKA ERK Metabolic Disease
    Sitagliptin-d4 (MK-0431-d4) is deuterium labeled Sitagliptin (HY-13749). Sitagliptin is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin can be used for the study of 1-type and 2-type diabetes.
    Sitagliptin-d4
  • HY-13749S3
    Sitagliptin-d6

    MK-0431-d6

    		 Isotope-Labeled Compounds Dipeptidyl Peptidase GLP Receptor Endogenous Metabolite PKA ERK Metabolic Disease
    Sitagliptin-d6 (MK-0431-d6) is deuterium labeled Sitagliptin (HY-13749). Sitagliptin is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin can be used for the study of 1-type and 2-type diabetes.
    Sitagliptin-d6
  • HY-13749BR
    Sitagliptin phosphate monohydrate (Standard)

    MK-0431 phosphate monohydrate (Standard)

    		 Reference Standards Dipeptidyl Peptidase GLP Receptor Endogenous Metabolite PKA ERK Metabolic Disease
    Sitagliptin (MK-0431) phosphate monohydrate (Standard) is the analytical standard of Sitagliptin phosphate monohydrate (HY-13749B). This product is intended for research and analytical applications. Sitagliptin phosphate monohydrate is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin phosphate monohydrate blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin phosphate monohydrate can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin phosphate monohydrate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate monohydrate can be used for the study of 1-type and 2-type diabetes.
    Sitagliptin phosphate monohydrate (Standard)
  • HY-105101
    Osutidine

    		Histamine Receptor Inflammation/Immunology
    Osutidine is a selective histamine H2 receptor antagonist, can effectively inhibit histamine-stimulated gastric acid secretion. Osutidine does not affect [ 14C]aminopyrine accumulation stimulated by carbachol or dibutyryl-cAMP. Osutidine is insurmountable and includes non-competitive inhibition. Osutidine can be used for the study of gastric mucosal injury .
    Osutidine
  • HY-179376
    Anti-virulence factor-IN-3

    		Bacterial Infection
    Anti-virulence factor-IN-3 (Compound 21) is a covalent β-aminosulfinyl type anthrax edema factor (EF) inhibitor, with a Ki value of 0.44 μM. Anti-virulence factor-IN-3 generates an active ethylene sulfinyl intermediate, which forms an irreversible covalent bond with the Lys residue at the active center of EF, permanently inhibiting the adenylate cyclase activity of EF. Anti-virulence factor-IN-3 effectively inhibits the cAMP production induced by EF, with an EC50 value of 0.15 μM. Anti-virulence factor-IN-3 can be used for research on anthrax Infection .
    Anti-virulence factor-IN-3
  • HY-182503
    GP515

    		Adenosine Kinase Others Inflammation/Immunology
    GP515 is a potent and selective adenosine kinase inhibitor with a human IC50 of 4 nM. GP515 exerts tissue protective effects, produces long-lasting hepatic microcirculation effects after hemorrhagic shock, and induces dose- and time-related VEGF mRNA and protein expression in normoxic rat myocardial myoblasts, with additive VEGF increases during mild hypoxia and no effect during severe hypoxia. GP515 suppresses IFNγ synthesis and CD69 expression in DSS-induced colitis. GP515 also shows a dose-dependent suppression of TNF-α production with an IC50 of 80 μM and can be reversed in the presence of the cAMP antagonist (Rp)-cAMPS. Combinations of GP515 with either adenosine or rolipram led to an additive inhibition of TNF-α synthesis. GP515 can be used for the research of hemorrhagic shock .
    GP515
  • HY-101189R
    JNJ-39758979 (Standard)

    		Histamine Receptor Reference Standards Neurological Disease Endocrinology
    JNJ-39758979 (Standard) is the analytical standard of JNJ-39758979 (HY-101189). This product is intended for research and analytical applications. JNJ-39758979, a chemical probe, is a selective, orally active, and high-affinity histamine H4 receptor antagonist with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 shows good anti-inflammatory and antipruritic activity .
    JNJ-39758979 (Standard)
  • HY-N12378A
    α-Patchoulene

    		AMPK FASTK Sirtuin ROCK Keap1-Nrf2 Toll-like Receptor (TLR) Apoptosis PKA ERK NF-κB Epigenetic Reader Domain Caspase Metabolic Disease Inflammation/Immunology Cancer
    α-Patchoulene is an orally active anti-inflammatory, antioxidant, and anti-apoptotic agent. α-Patchoulene inhibits the NF-κB, TLR4, and cAMP/PKA/CREB signaling pathways; activates the Sirt1/Nrf2 and AMPK signaling pathways; and targets Fas/FasL, Caspase-3, ERK1/2, ROCK1/MLC2 for inhibition. α-Patchoulene regulates cytokine secretion, inflammatory cell infiltration, lipid peroxidation, cell polarization, gut microbiota, and lipid metabolism, restores barrier function, mitochondrial function, and cell viability, and exhibits repellent activity against Spodoptera exigua larvae. α-Patchoulene can be used in research related to various inflammatory, ischemic, fibrosis-associated diseases, as well as hepatocellular carcinoma .
    α-Patchoulene

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