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Pathways Recommended: MAPK/ERK Pathway
Results for "

cAMP/PKA pathway

" in MedChemExpress (MCE) Product Catalog:

37

Inhibitors & Agonists

6

Peptides

1

Inhibitory Antibodies

4

Natural
Products

4

Isotope-Labeled Compounds

Targets Recommended:
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-P991202
    Anti-TSHR Antibody (M22)

    		TSH Receptor PKA Metabolic Disease Inflammation/Immunology
    Anti-TSHR Antibody (M22) is a selective agonist targeting TSHR (thyroid-stimulating hormone receptor), acting through competitive binding to the extracellular domain of TSHR. Anti-TSHR Antibody (M22) can mimic the biological effects of thyroid-stimulating hormone (TSH), activating downstream cAMP-PKA and other signaling pathways. Anti-TSHR Antibody (M22) can stimulate the proliferation of thyroid follicular epithelial cells and human umbilical vein endothelial cells (HUVECs), promote angiogenesis and tube formation, cell migration, and also upregulate the expression of angiogenesis-related proteins such as PROX1. Anti-TSHR Antibody (M22) can be used in research areas such as the mechanisms of goiter formation in Graves' disease (GD), angiogenesis regulation, and TSHR antagonist screening .
    Anti-TSHR Antibody (M22)
  • HY-W012980
    Isovaleric acid
    1 Publications Verification

    		 Environmental Pollutants Endogenous Metabolite PKA AMPK Metabolic Disease
    Isovaleric acid is an oral active short-chain fatty acid that inhibits osteoclast differentiation by stimulating AMPK phosphorylation and promotes colonic smooth muscle relaxation by activating the cAMP/PKA pathway. Isovaleric acid can be used in research on skeletal diseases (such as osteoporosis) and intestinal disorders .
    Isovaleric acid
  • HY-B0327
    Irsogladine
    3 Publications Verification

    Dicloguamine

    		 Phosphodiesterase (PDE) NF-κB AP-1 TRP Channel Interleukin Related Inflammation/Immunology Cancer
    Irsogladine (Dicloguamine) is an orally active gastric mucosal protective agent. Irsogladine inhibits breast cancer recurrence and lung metastasis in nude mice . Irsogladine inhibits the transcriptional activities of NF-κB and AP-1, suppresses the activities of PDE and PDE4 to elevate intracellular cAMP levels, and activates TRPV1 and KATP channels. Irsogladine enhances iNOS expression, NO production, and the activation of cAMP-responsive elements. Irsogladine inhibits the development and progression of intestinal polyps in Apc-mutant mice. Irsogladine alleviates oxidative stress, increases gastric mucosal blood flow, and stimulates the production of endogenous prostaglandins. Irsogladine promotes insulin secretion in MIN6 cells. Irsogladine inhibits tumor angiogenesis, cancer cell proliferation, and the production of proinflammatory cytokines. Irsogladine exerts protective effects on astrocytes in ethanol/hydrochloric acid-induced gastric ulcers in mice. Irsogladine prevents colitis in IL-10 gene-deficient mice by reducing the production of IL-12 and IL-23. Irsogladine upregulates gap junction intercellular communication in pancreatic cancer cells via the PKA pathway. Irsogladine is applicable to research related to breast cancer, intestinal polyposis, gastric ulcer, spontaneous colitis, glioma, liver cancer, and pancreatic cancer [5][6] .
    Irsogladine
  • 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-103322
    6-Bnz-cAMP sodium salt

    		PKA Potassium Channel Metabolic Disease Cancer
    6-Bnz-cAMP sodium, a derivative of cyclic adenosine monophosphate (cAMP), is a selective PKA activator with inhibitory activity against the bTREK-1 K + channel. 6-Bnz-cAMP sodium does not activate the Epac signaling pathway. It inhibits the bTREK-1 K + channel via a voltage-independent, ATP-dependent mechanism that is independent of the PKA/Epac/calmodulin kinase/MAP kinase pathway. 6-Bnz-cAMP sodium activates CREB phosphorylation to regulate osteoblast-specific gene expression, induces osteoblast differentiation, promotes extracellular matrix mineralization, supports osteoblast proliferation, and shows no cytotoxicity toward osteoblasts. It can be used in studies related to bone tissue repair and regeneration .
    6-Bnz-cAMP sodium salt
  • HY-P10927A
    BRP TFA

    BRINP2-related peptide TFA

    		 PKA AP-1 Metabolic Disease
    BRP (BRINP2-related peptide) TFA is a 12-peptide derived from BRINP2 that can cross the blood-brain barrier. BRP TFA induces the central activation of FOS in neuronal cells via the cAMP-PKA-CREB signaling pathway. BRP TFA exerts anorectic and anti-obesity effects without triggering nausea or aversive responses. The action of BRP TFA is independent of the leptin, GLP-1 receptor and melanocortin 4 receptor pathways. BRP TFA is applicable to obesity-related research .
    BRP TFA
  • HY-175232
    GL64

    		Nuclear Factor of activated T Cells (NFAT) Endogenous Metabolite Endocrinology
    GL64 is a selective agonist of ADGRD1 (EC50 = 3.98 μM). GL64 has low selectivity for ADGRD2, ADGRG5, ADGRG6, CELSR1, CELSR2, CELSR3, and ADGRG4 isoforms. GL64 activates ADGRD1 by mimicking the satchel sequence. GL64 regulates osteoclast maturation through the cAMP-PKA-NFATC1 pathway. GL64 effectively inhibits osteoclastogenesis and prevents bone loss both in vitro and in vivo. GL64 is useful in the study of osteoclast-related diseases .
    GL64
  • HY-P10927
    BRP

    BRINP2-related peptide

    		 AP-1 PKA Metabolic Disease
    BRP is a 12-peptide derived from BRINP2 that can cross the blood-brain barrier. BRP induces the central activation of FOS in neuronal cells via the cAMP-PKA-CREB signaling pathway. BRP exerts anorectic and anti-obesity effects without triggering nausea or aversive responses. The action of BRP is independent of the leptin, GLP-1 receptor and melanocortin 4 receptor pathways. BRP is applicable to obesity-related research .
    BRP
  • HY-P6292
    KS-133

    		PACAP Receptor PKA ERK PI3K Akt GSK-3 Neurological Disease Cancer
    KS-133 is a bicyclic peptide with VIPR2 antagonistic activity that can cross the blood-brain barrier. KS-133 selectively blocks VIPR2-mediated Gq/Ca, Gs/cAMP, cAMP/PKA/ERK and PI3K/AKT/GSK3β signaling pathways. KS-133 inhibits VIPR2 agonist-induced CREB phosphorylation in the prefrontal cortex of mice. KS-133 shifts the polarization direction of macrophages toward M1. KS-133 attenuates cancer cell proliferation and reduces the cell cycle distribution level at the S-M phase. KS-133 exerts antitumor effects in a mouse model of colorectal cancer. KS-133 reverses cognitive decline in mouse models of psychiatric disorders. KS-133 can be used for research related to schizophrenia, colorectal cancer and breast cancer .
    KS-133
  • HY-107544
    8-pCPT-2'-O-Me-cAMP-AM

    		PKA Metabolic Disease
    8-pCPT-2'-O-Me-cAMP-AM is a cyclic AMP analogue, selectively activates Epac-Rap signaling pathway. 8-pCPT-2'-O-Me-cAMP-AM protects renal function by activating Epac from ischemia injury. 8-pCPT-2'-O-Me-cAMP-AM also stimulates insulin secretion by interaction with PKA pathway .
    8-pCPT-2'-O-Me-cAMP-AM
  • 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-110218
    CW 008
    2 Publications Verification

    		 PKA Epigenetic Reader Domain Others
    CW 008, a derivative of pyrazole-pyridine, is a CREB or PKA pathway agonist. CW 008 also is a stem cell differentiating agent. CW 008 stimulates osteoblast differentiation of human MSCs and increases bone formation in ovariectomized mice. CW008 promotes osteogenesis by activating cAMP/PKA/CREB signaling pathway and inhibiting leptin secretion .
    CW 008
  • HY-P10336
    Serpinin

    		Serpin Neurological Disease Endocrinology
    Serpinin is an agonist of the protease inhibitor Nexin-1 (PN-1). Serpinin upregulates the expression of PN-1 through the cAMP-PKA-Sp1 signaling pathway, promoting granule biogenesis in endocrine cells. Serpinin is used in research related to the regulation of secretory function . Serpinin is a selective agonist for β-adrenergic receptors. Serpinin interacts with β1-adrenergic receptors to activate the AC-cAMP-PKA pathway, which regulates myocardial systolic and diastolic function. pGlu-serpinin upregulates Bcl2 mRNA transcription and exerts neuroprotective effects .
    Serpinin
  • HY-17457
    Levalbuterol hemitartrate

    Levosalbutamol hemitartrate

    		 Adrenergic Receptor PI3K Inflammation/Immunology
    Levalbuterol (Levosalbutamol) hemitartrate is a β2-adrenergic receptor agonist and PI3K inhibitor. Levalbuterol hemitartrate inhibits PI3K activity, reduces NF-κB and Rb protein expression, activates the cAMP/PKA pathway, and stimulates cAMP release. Levalbuterol hemitartrate relaxes airway smooth muscle, reduces intracellular calcium levels, and inhibits spasmogen-induced contractions. Levalbuterol hemitartrate can be used for the research of moderate-to-severe asthma .
    Levalbuterol hemitartrate
  • HY-W012980R
    Isovaleric acid (Standard)

    		Reference Standards Endogenous Metabolite AMPK PKA Metabolic Disease
    Isovaleric acid (Standard) is the analytical standard of Isovaleric acid. This product is intended for research and analytical applications. Isovaleric acid is an oral active short-chain fatty acid that inhibits osteoclast differentiation by stimulating AMPK phosphorylation and promotes colonic smooth muscle relaxation by activating the cAMP/PKA pathway. Isovaleric acid can be used in research on skeletal diseases (such as osteoporosis) and intestinal disorders .
    Isovaleric acid (Standard)
  • 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-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-Q40876
    BBT

    		Calcium Channel Metabolic Disease
    BBT is an enhancer of impaired glucose-stimulated insulin secretion (GSIS). BBT exhibits anti-hyperglycemia activity, and protects β-cells from cytokine- or streptozotocin (STZ (HY-13753))-induced cell death in type 2 diabetes models. BBT acts function via cAMP/PKA and long-lasting (L-type) voltage-dependent Ca2+ channel/CaMK2 pathway .
    BBT
  • HY-P10256A
    Kiss2 peptide acetate

    		Kisspeptin Receptor PKA PKC Endocrinology
    Kiss2 peptide acetate is the acetate form of Kiss2 pepride (HY-P10256). Kiss2 peptide acetate is a positive regulator of reproduction. Kiss2 peptide acetate binds with its cognate receptor Kiss2R (GPR54) in COS-7 cells, activates PKA and PKC signaling pathways through Gas and Gaq proteins, and thus enhances the activity of cAMP response element-dependent luciferase (CRE-luc) and serum response element-dependent luciferase (SRE-luc) .
    Kiss2 peptide acetate
  • 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-134263
    8-Br-cAMP-AM

    		PKA Ras Cardiovascular Disease
    8-Br-cAMP-AM is a cyclic adenosine monophosphate (cAMP) analog that activates two major signal transduction pathways in the heart by mimicking the effects of cAMP: protein kinase A (PKA) and guanosine nucleotide exchange factor (Epac), which is directly activated by cAMP. 8-Br-cAMP-AM can be used to study cardiac ischemia and reperfusion injury .
    8-Br-cAMP-AM
  • HY-179407
    LT-104A

    		Phosphodiesterase (PDE) Inflammation/Immunology
    LT-104A is a potent PDE4 inhibitor that elevates intracellular cAMP levels (EC50 = 1.9 μM) and inhibits PDE4D3 activity (IC50 = 9.3 μM). LT-104A activates the cAMP-PKA-CREB anti-inflammatory signaling pathway and suppresses NF-κB-related gene expression (Il1b and Nos2). LT-104A can be used for inflammation-related disease research .
    LT-104A
  • 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-137381
    6-Bnz-cAMP

    N6-Benzoyl-cAMP

    		 PKA Potassium Channel Metabolic Disease
    6-Bnz-cAMP, a derivative of cyclic adenosine monophosphate (cAMP), is a selective PKA activator with inhibitory activity against the bTREK-1 K + channel. 6-Bnz-cAMP does not activate the Epac signaling pathway. 6-Bnz-cAMP inhibits the bTREK-1 K + channel via a voltage-independent, ATP-dependent mechanism that is independent of the PKA/Epac/calmodulin kinase/MAP kinase pathway. 6-Bnz-cAMP activates CREB phosphorylation to regulate osteoblast-specific gene expression, induces osteoblast differentiation, promotes extracellular matrix mineralization, supports osteoblast proliferation, and shows no cytotoxicity toward osteoblasts. 6-Bnz-cAMP can be used in studies related to bone tissue repair and regeneration .
    6-Bnz-cAMP
  • HY-P10256
    Kiss2 peptide

    		Kisspeptin Receptor PKA PKC Endocrinology
    Kiss2 peptide is a positive regulator of reproduction. Kiss2 peptide binds with its cognate receptor Kiss2R (GPR54) in COS-7 cells, activates PKA and PKC signaling pathways through Gas and Gaq proteins, and thus enhances the activity of cAMP response element-dependent luciferase (CRE-luc) and serum response element-dependent luciferase (SRE-luc) .
    Kiss2 peptide
  • HY-178478
    PDE1-IN-11

    		Phosphodiesterase (PDE) Metabolic Disease
    PDE1-IN-11 (Compound 5cc) is an orally active and highly selective PDE1A1 inhibitor. PDE1-IN-11 increases intracellular cAMP and cGMP levels, activating the PKA-CREB and NO-cGMP-PKG signaling pathways, promoting osteoblast differentiation and bone formation, while suppressing osteoclastogenesis and bone resorption. PDE1-IN-11 is promising for research of postmenopausal osteoporosis (PMO) and other bone metabolism disorders .
    PDE1-IN-11
  • 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-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-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-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-179518
    Antifungal agent 140

    		Fungal PKA Ras Infection
    Antifungal agent 140 (compound 5p) is a potent antifungal agent with broad-spectrum antifungal activity. Antifungal agent 140 exerts a dual mechanism by targeting the Ras/cAMP/PKA pathway to inhibit hyphal formation and the ergosterol biosynthesis pathway. Antifungal agent 140 enhances survival, reduces fungal load in the kidneys, and strengthens host immune responses in a murine model of systemic candidiasis. Antifungal agent 140 can be used for research of resistant fungal infections .
    Antifungal agent 140
  • HY-179645
    Phosphodiesterase-IN-5

    		Phosphodiesterase (PDE) PKA Interleukin Related TNF Receptor Collagen Inflammation/Immunology
    Phosphodiesterase-IN-5 is a potent, orally active and selective phosphodiesterase 10A (PDE10A) inhibitor with an IC50 of 6.2 nM. Phosphodiesterase-IN-5 shows >1612-fold selectivity over other PDEs. Phosphodiesterase-IN-5 exhibits potent antifibrotic efficacy in a Bleomycin (BLM) (HY-108345)-induced murine model of pulmonary fibrosis (PF) by blocking myofibroblast differentiation via the cAMP/PKA/CREB signaling pathway. Phosphodiesterase-IN-5 can be used for the research of PF .
    Phosphodiesterase-IN-5
  • 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
  • HY-181088
    PDE3/4-IN-4

    		Phosphodiesterase (PDE) Interleukin Related Metabolic Disease
    PDE3/4-IN-4 is an orally active PDE3A and PDE4B inhibitor with IC50 values of 10 nM and 9.4 nM, respectively. PDE3/4-IN-4 shows selective activity relative to most other PDE family members. PDE3/4-IN-4 modulates the cAMP/PKA/CREB signaling pathway. PDE3/4-IN-4 inhibits pro-inflammatory factor IL-6. PDE3/4-IN-4 reduces expression of inflammatory markers in liver tissue. PDE3/4-IN-4 attenuates liver fibrosis. PDE3/4-IN-4 limits liver damage in cholestatic and sepsis-induced liver disease mice models. PDE3/4-IN-4 can be used for the research of liver injury, cholestatic liver diseases, sepsis-induced liver injury .
    PDE3/4-IN-4

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