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Results for "

cAMP

" in MCE Product Catalog:

225

Inhibitors & Agonists

3

Biochemical Assay Reagents

54

Peptides

21

Natural
Products

4

Recombinant Proteins

5

Isotope-Labeled Compounds

5

Antibodies

Cat. No. Product Name Target Research Areas
  • HY-B1511
    Cyclic AMP

    Cyclic adenosine monophosphate; Adenosine cyclic 3', 5'-monophosphate; cAMP

    Endogenous Metabolite Cancer Metabolic Disease Neurological Disease
    Cyclic AMP (Cyclic adenosine monophosphate), adenosine triphosphate derivative, is an intracellular signaling molecule responsible for directing cellular responses to extracellular signals. Cyclic AMP is an important second messenger in many biological processes.
  • HY-131768
    2'-O-Succinyl-cAMP

    Cholinesterase (ChE) Others
    2'-O-Succinyl-cAMP is a cAMP analog that can be covalently coupled to acetylcholinesterase. 2'-O-Succinyl-cAMP conjugate has been used as tracers in a classical heterogeneous competitive enzyme immunoassay allowing the determination of cAMP.
  • HY-134321
    8-Azido-cAMP

    Fluorescent Dye Others
    8-Azido-cAMP is a fluorescent cAMP analog, acting as the model target of detecting cAMP.
  • HY-123396
    8-Chloro-cAMP

    PKA Cancer
    8-Chloro-cAMP is a cAMP analogue that induces growth arrest, and modulates cAMP-dependent PKA activity. 8-Chloro-cAMP has anticancer activity.
  • HY-B0764
    Bucladesine sodium

    Dibutyryl cAMP sodium salt; DBcAMP sodium salt

    PKA Phosphodiesterase (PDE) Inflammation/Immunology
    Bucladesine sodium salt (Dibutyryl-cAMP sodium salt) is a stabilized cyclic AMP (cAMP) analog and a selective PKA activator. Bucladesine sodium salt raises the intracellular levels of cAMP. Bucladesine sodium salt is also a phosphodiesterase (PDE) inhibitor. Bucladesine sodium salt has anti-inflammatory activity and can be used for impaired wound healing.
  • HY-103322
    6-Bnz-cAMP sodium salt

    PKA
    6-Bnz-cAMP sodium salt is a cell-permeable cAMP analog. 6-Bnz-cAMP selectively activates cAMP-dependent PKA but not Epac signaling pathways.
  • HY-12306
    8-Bromo-cAMP sodium salt

    8-Br-cAMP sodium salt

    PKA Cancer
    8-Bromo-cAMP sodium salt (8-Br-Camp sodium salt), a cyclic AMP analog, is an activator of cyclic AMP-dependent protein kinase (PKA).
  • HY-107543
    8-CPT-2Me-cAMP sodium

    Ras Others
    8-CPT-2Me-cAMP sodium is a selective activator of exchange proteins activated by cAMP (Epac), the cAMP sensitive guanine nucleotide exchange factors (GEFs) for the small GTPases Rap1 and Rap2. 8-CPT-2Me-cAMP sodium activates Epac1 (EC50 = 2.2 μM), but not PKA (EC50> 10 μM). 8-CPT-2Me-cAMP sodium stimulates Epac-mediated Ca 2+ release in pancreatic β-cells in vitro.
  • HY-B0764A
    Bucladesine calcium

    Dibutyryl cAMP calcium salt; DBcAMP calcium salt

    PKA Phosphodiesterase (PDE) Apoptosis Others
    Bucladesine calcium salt (Dibutyryl-cAMP calcium salt;DC2797 calcium salt) is a cell-permeable cyclic AMP (cAMP) analog and selectively activates cAMP dependent protein kinase (PKA) by increasing the intracellular level of cAMP. Bucladesine calcium salt acts as a phosphodiesterase (PDE) inhibitor.
  • 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.
  • HY-131763
    2'-O-MB-cAMP sodium

    2'-O-Monobutyryl cyclic AMP sodium

    Others Others
    2'-O-MB-cAMP (2'-O-Monobutyryl cyclic AM) sodium is an activatable proagent of Cyclic AMP (HY-B1511).
  • HY-111673
    8-CPT-Cyclic AMP sodium

    8-CPT-cAMP sodium; 8-(p-Chlorophenylthio)-cAMP sodium

    PKA Phosphodiesterase (PDE) Inflammation/Immunology
    8-CPT-Cyclic AMP (8-CPT-cAMP) sodium is a selective activator of cyclic AMP-dependent protein kinase (PKA). 8-CPT-Cyclic AMP sodium is also a potent inhibitor of the cyclic GMP-specific phosphodiesterase (PDE VA) with an IC50 of 0.9 μM. 8-CPT-Cyclic AMP sodium also inhibits PDE III and PDE IV with IC50Epac and is a potent Epac activator.
  • HY-120994A
    Rp-8-CPT-cAMPS

    PKA Inflammation/Immunology Neurological Disease
    Rp-8-CPT-cAMPS, a cAMP analog, is a potent and competitive antagonist of cAMP-induced activation of cAMP-dependent PKA I and II. Rp-8-CPT-cAMPS preferentially selects site A of RI compares to site A of RII and site B of RII compares to site B of RI.
  • HY-120994
    Rp-8-CPT-cAMPS sodium

    PKA Inflammation/Immunology Neurological Disease
    Rp-8-CPT-cAMPS sodium, a cAMP analog, is a potent and competitive antagonist of cAMP-induced activation of cAMP-dependent PKA I and II. Rp-8-CPT-cAMPS sodium preferentially selects site A of RI compares to site A of RII and site B of RII compares to site B of RI.
  • HY-100530D
    Rp-cAMPS sodium salt

    PKA Neurological Disease
    Rp-cAMPS sodium salt, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 µM and 4.5 µM, respectively) antagonist. Rp-cAMPS sodium salt is resistant to hydrolysis by phosphodiesterases.
  • HY-100530A
    Rp-cAMPS

    PKA Neurological Disease
    Rp-cAMPS, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 µM and 4.5 µM, respectively) antagonist. Rp-cAMPS is resistant to hydrolysis by phosphodiesterases.
  • HY-100530
    Rp-cAMPS triethylammonium salt

    PKA Neurological Disease
    Rp-cAMPS triethylammonium salt, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 µM and 4.5 µM, respectively) antagonist. Rp-cAMPS triethylammonium salt is resistant to hydrolysis by phosphodiesterases.
  • HY-P3770
    Phosphate acceptor peptide

    PKC Others
    Phosphate acceptor peptide is a substrate for cAMP-dependent protein kinase (PKA). phosphate acceptor peptide is also a weak PKC inhibitor.
  • HY-P3786
    H-Arg-Gly-Tyr-Ala-Leu-Gly-OH

    PKA PKC Cancer
    H-Arg-Gly-Tyr-Ala-Leu-Gly-OH is a competitive and CAMP dependent protein kinase inhibitor.
  • HY-100530B
    Sp-cAMPS

    PKA Phosphodiesterase (PDE) Metabolic Disease Neurological Disease
    Sp-cAMPS, a cAMP analog, is potent activator of cAMP-dependent PKA I and PKA II. Sp-cAMPS is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS binds the PDE10 GAF domain with an EC50 of 40 μM.
  • HY-100530C
    Sp-cAMPS sodium salt

    PKA Phosphodiesterase (PDE) Metabolic Disease Neurological Disease
    Sp-cAMPS sodium salt, a cAMP analog, is potent activator of cAMP-dependent PKA I and PKA II. Sp-cAMPS sodium salt is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS sodium salt binds the PDE10 GAF domain with an EC50 of 40 μM.
  • HY-110005
    Sp-cAMPS triethylamine

    PKA Phosphodiesterase (PDE) Metabolic Disease Neurological Disease
    Sp-cAMPS triethylamine, a cAMP analog, is potent activator of cAMP-dependent PKA I and PKA II. Sp-cAMPS triethylamine is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS triethylamine binds the PDE10 GAF domain with an EC50 of 40 μM.
  • HY-124151
    Adenosine-2'-monophosphate

    2'-AMP; Adenosine 2'-phosphate; AMP 2'-phosphate

    Adenosine Receptor Endogenous Metabolite Neurological Disease
    Adenosine-2'-monophosphate (2'-AMP) is converted by extracellular 2’,3'-CAMP. Adenosine-2'-monophosphate is further metabolized to extracellular adenosine (a mechanism called the extracellular 2’,3’-cAMP-adenosine pathway). Adenosine-2'-monophosphate inhibits LPS-induced TNF-α and CXCL10 production via A2A receptor activation.
  • HY-136172
    ESI-08

    Ras Cancer Metabolic Disease Cardiovascular Disease
    ESI-08 is a potent and selective EPAC antagonist, which can completely inhibit both EPAC1 and EPAC2 (IC50 of 8.4 μM) activity. ESI-08 selectively blocks cAMP-induced EPAC activation, but does not inhibit cAMP-mediated PKA activation.
  • HY-N3550
    Catalponol

    Others Cancer
    Catalponol is a naphthoquinone derivative. Catalponol enhances dopamine biosynthesis by inducing tyrosine hydroxylase activity. Catalponol also increases the levels of cAMP and tyrosine hydroxylase phosphorylation in PC12 cells.
  • HY-141495
    (Rac)-Razpipadon

    PW0464

    Dopamine Receptor Neurological Disease
    PW0464, a nanomolar potent complete G protein biased ligand, is a noncatechol D1R agonist, with an EC50 of 5.8 nM (Gs-cAMP).
  • HY-100927
    Ro 20-1724

    Ro 20-174

    Phosphodiesterase (PDE) Neurological Disease
    Ro 20-1724 (Ro 20-174) is a potent inhibitor of cAMP-specific phosphodiesterase (PDE4/PDE IV) with a Ki of 1930 nM. Neuroprotective effect.
  • HY-103180
    2'-MeCCPA

    Adenosine Receptor Neurological Disease
    2'-MeCCPA is a potent and selective A1 adenosine receptors (A1AR) agonist. 2'-MeCCPA efficiently inhibits cAMP modulation in both direct pathway medium spiny neurons (dMSNs) and indirect pathway medium spiny neurons (iMSNs).
  • HY-117656
    ESI-05

    NSC 116966

    Acyltransferase Metabolic Disease Neurological Disease
    ESI-05 is a specific exchange proteins directly activated by cAMP 2 (EPAC2) inhibitor. ESI-05 inhibits cAMP-mediated EPAC2 GEF activity with an IC50 of 0.43 μM. ESI-05 can be used for the research of diabetes, insulin secretion and neurological disorders.
  • HY-P2197
    ELA-11(human)

    Apelin Receptor (APJ) Arrestin Inflammation/Immunology
    ELA-11(human), a peptide, is a full agonist of human apelin receptor, with a pKi of 7.85. ELA-11(human) completely inhibits Forskolin-induced cAMP production and stimulates β-arrestin recruitment.
  • HY-P2249
    ELA-21 (human)

    Apelin Receptor (APJ) Arrestin Cardiovascular Disease
    ELA-21 (human) is an apelin receptor agonist with a pKi of 8.52. ELA-21 (human) completely inhibits Forskolin-induced cAMP production and stimulates β-arrestin recruitment with subnanomolar potencies. ELA-21 (human) is an agonist in G-protein-dependent and -independent pathways.
  • HY-131032
    KI-7

    Adenosine Receptor Others
    KI-7 is an A2B adenosine receptor positive allosteric modulator. KI-7 potentiates the cAMP accumulation induced by the non-selective A2B adenosine receptor agonist NECA (EC50=445.8 nM). KI-7 also potentiates the cAMP accumulation induced by the selective A2B adenosine receptor agonist BAY 60-6583 as well as by adenosine with EC50s of 2390 nM and 2550 nM, respectively.
  • HY-N2168
    Pinoresinol 4-O-β-D-glucopyranoside

    (+)-Pinoresinol 4-O-β-D-glucopyranoside

    Others Cardiovascular Disease
    Pinoresinol 4-O-β-D-glucopyranoside ((+)-Pinoresinol 4-O-β-D-glucopyranoside) is the major active furofuran type lignans in Fructus Forsythiae. Pinoresinol 4-O-β-D-glucopyranoside shows antioxidant, blood pressure reducing, and cyclic adenosine monophosphate (cAMP) phosphodiesterase inhibitory effects.
  • HY-N2658
    5,7-Diacetoxy-8-methoxyflavone

    Phosphodiesterase (PDE) Others
    5,7-Diacetoxy-8-methoxyflavone is a natural product that could come from scutellaria genus plants. 5,7-Diacetoxy-8-methoxyflavone has inhibitory activity for cAMP phosphodiesterase.
  • HY-134266
    8-Bromo-AMP

    8-Bromoadenosine 5'-monophosphate; 8-Bromoadenylic acid

    Others Cardiovascular Disease
    8-Bromo-AMP (8-Bromoadenosine 5'-monophosphate) is a membrane permeable cAMP analogue. 8-Bromo-AMP can improve the ability of the heart to recover from ischemia and reperfusion by increasing the levels of ATP, ADP, and total adenine nucleotides.
  • HY-B0392
    (S)-(+)-Rolipram

    (+)-Rolipram; (S)-Rolipram

    Phosphodiesterase (PDE) Apoptosis Cancer Inflammation/Immunology Neurological Disease
    (S)-(+)-Rolipram ((+)-Rolipram) is a cyclic AMP(cAMP)-specific phosphodiesterase 4 (PDE4) inhibitor, with an IC50 of 1100 nM. (S)-(+)-Rolipram can suppresse tumor necrosis factor-alpha (TNFα) production by human mononuclear cells.
  • HY-125791
    cis-Epoxysuccinic acid

    Succinate Receptor 1 Cardiovascular Disease
    cis-Epoxysuccinic acid is a succinate receptor (SUCNR1/GPR91) agonist. cis-Epoxysuccinic acid inhibits cAMP levels with an EC50 value of 2.7 µM. cis-Epoxysuccinic acid can be used for the research of cardiovascular system.
  • HY-18740A
    Trequinsin hydrochloride

    HL 725

    Phosphodiesterase (PDE) Metabolic Disease
    Trequinsin hydrochloride (HL 725) is an extremely potent inhibitor of platelet CAMP phosphodiesterase (PDE), with an IC50 of 0.25 nM. Trequinsin hydrochloride (HL 725) is an extremely potent inhibitor of the aggregation of human platelets induced in vitro by ADP, collagen, thrombin and epinephrine.
  • HY-P0252B
    α-MSH free acid

    α-Melanocyte-Stimulating Hormone free acid

    Melanocortin Receptor Neurological Disease
    α-MSH free acid (α-Melanocyte-Stimulating Hormone free acid) is an MC3R and MC4R agonist with EC50s of 0.16 nM and 5.6 nM, respectively. α-MSH free acid activates cAMP generation at MC3R and MC4R.
  • HY-139486
    AM-8123

    Apelin Receptor (APJ) Cardiovascular Disease
    AM-8123 is an orally active and potent APJ agonist. AM-8123 inhibits Forskolin-stimulated cAMP production and promotes Gα protein activation. AM-8123 can be used for the research of cardiovascular disease.
  • HY-108618
    BC11-38

    Phosphodiesterase (PDE) Endocrinology
    BC11-38 is a potent, selective, and biologically active PDE11 inhibitor, with IC50s of 0.28 µM and >100 µM for PDE11 and PDE1-10, respectively. BC11-38 elevates cAMP levels, PKA-mediated ATF-1 phosphorylation, and cortisol production in H295R cells.
  • HY-15371G
    Forskolin

    Coleonol; Colforsin; HL 362

    Adenylate Cyclase FXR Autophagy Cancer Endocrinology Metabolic Disease Inflammation/Immunology
    Forskolin (Coleonol) (GMP) is Forskolin (HY-15371) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Forskolin is a potent adenylate cyclase activator and inducer of intracellular cAMP formation.
  • 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.
  • HY-P1597
    Malantide

    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.
  • 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.
  • HY-103186
    MRS-1706

    Adenosine Receptor Inflammation/Immunology
    MRS-1706 is a potent and selective adenosine A2B receptor inverse agonist. MRS-1706 has Ki values of 1.39, 112, 157, and 230 nM for human A2B, A2A, A1 and A3 receptors respectively. MRS-1706 blocks adenosine-mediated cAMP induction.
  • HY-103178
    MRE3008F20

    Adenosine Receptor Inflammation/Immunology
    MRE3008F20 is a highly efficient, highly selective and radioactive adenosine A3 receptor (AA3R) antagonist (Ki=1.8 nM). MRE3008F20 effectively antagonises Cl-IB-MECA-induced cAMP production in resting lymphocytes with an IC50 value of 5 nM. MRE3008F20 can be used in the study of AA3R.
  • HY-115553
    DETQ

    Dopamine Receptor Neurological Disease
    DETQ is a selective, allosteric and orally active dopamine D1 receptor (Dopamine Receptor) potentiator. In HEK293 cells expressing the human D1 receptor, DETQ increases cAMP with an EC50 of 5.8 nM and a Kb of 26 nM. DETQ shows ~30-fold less potent at rat and mouse D1 receptors and is inactive at the human D5 receptor.
  • HY-117829
    UNC9994

    Dopamine Receptor 5-HT Receptor Histamine Receptor Arrestin Neurological Disease
    UNC9994, an analog of Aripiprazole, is a functionally selective β-arrestin-biased dopamine D2 receptor (D2R) agonist with EC50 <10 nM for β-arrestin-2 recruitment to D2 receptors. UNC9994 is simultaneously partial agonists of β-arrestin-2 translocation and antagonists of Gi-regulated cAMP production. Antipsychotic Activity.
  • HY-108621
    RS-25344 hydrochloride

    Phosphodiesterase (PDE) Cancer Metabolic Disease Inflammation/Immunology Neurological Disease
    RS-25344 hydrochloride is a selective cAMP-phosphodiesterase 4 (PDE 4; PDE IV) inhibitor with an IC50 of 0.28 nM in human lymphocytes. RS-25344 hydrochloride has only weak inhibitory effects on PDE I, II, III (IC50 of >100 μM, 160 μM, 330 μM, respectively). RS-25344 hydrochloride has anti-inflammatory, memory- and cognition enhancing, and antineoplastic effects.
  • HY-14340
    WAY-181187

    SAX-187

    5-HT Receptor Neurological Disease
    WAY-181187 (SAX-187) is a potent and selective full 5-HT6 receptor agonist with a Ki of 2.2 nM and an EC50 of 6.6 nM. WAY181187 mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist.
  • HY-110366
    WAY-181187 oxalate

    SAX-187 oxalate

    5-HT Receptor Neurological Disease
    WAY-181187 (SAX-187) oxalate is a potent and selective full 5-HT6 receptor agonist with a Ki of 2.2 nM and an EC50 of 6.6 nM. WAY-181187 oxalate mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist.
  • HY-136501
    MRS2395

    P2Y Receptor Cardiovascular Disease
    MRS2395, an dipivaloyl derivative, is a potent P2Y12 receptor antagonist. MRS2395 inhibits ADP-induced platelet activation with a Ki of 3.6 μM. MRS2395 inhibits cAMP induced by ADP in rat platelets in the presence of PGE1 with an IC50 of 7 µM. MRS2395 enhances platelet dense granule release in response to TRAP-6.
  • HY-P4497
    Prolylserine

    ERK Others Cancer
    Prolylserine, a dipeptide, is an inhibitor of melanogenesis production in Mel-Ab cells. Prolylserine decreases expression of microphthalmia-associated transcription factor (MITF) and tyrosinase, induces phorphosylation of ERK, but not cAMP response element binding protein (CREB).
  • HY-133529
    PA-8

    Others Inflammation/Immunology Neurological Disease
    PA-8 is a potent, selective and orally active PACAP type I (PAC1) receptor antagonist. PA-8 inhibits the phosphorylation of CREB induced by PACAP in PAC1-, but not VPAC1- or VPAC2-receptor. PA-8 also inhibits PACAP-induced cAMP elevation with an IC50 of 2 nM.
  • HY-144705
    GAT564

    Cannabinoid Receptor Neurological Disease
    GAT564 (Compound 15d) is a potent allosteric modulator of cannabinoid 1 receptor (CB1R) with EC50s of 87 and 320 nM respectively for cAMP and β-arrestin2. GAT564 markedly promotes orthosteric ligand binding to hCB1R. GAT564 is efficacious as a topical agent that significantly reduces intraocular pressure (IOP) in the ocular normotensive murine model of glaucoma.
  • HY-101189
    JNJ-39758979

    Histamine Receptor Neurological Disease Endocrinology
    JNJ-39758979 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.
  • 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.
  • HY-B0813
    Treprostinil diethanolamine

    UT-15C

    Prostaglandin Receptor Endocrinology
    Treprostinil (UT-15C) diethanolamine is a potent EP2, DP1 and IP agonist with Ki values of 3.6, 4.4, 32.1, 212, 826, 2505 and 4680 nM for EP2, DP1, IP, EP1, EP4, EP3 and FP, respectively. Treprostinil (UT-15C) diethanolamine increases upregulation of cAMP toward maintaining homeostasis within the vasculature. Treprostinil (UT-15C) diethanolamine can result in vasodilatation of human pulmonary arteries.
  • HY-120994B
    Sp-8-CPT-cAMPS

    PKA Inflammation/Immunology Neurological Disease
    Sp-8-CPT-cAMPS, a cAMP analog, is a potent and selective activator of the cAMP-dependent protein kinas A (PKA I and PKA II). Sp-8-CPT-cAMPS selects site A of RI compares to site A of RII by 153-fold and site B of RII compares to site B of RI by 59-fold.
  • HY-111385
    UNC9994 hydrochloride

    Dopamine Receptor 5-HT Receptor Arrestin Neurological Disease
    UNC9994 hydrochloride is a functionally selective, β-arrestin–biased dopamine D2 receptor (D2R) agonist that selectively activates β-arrestin recruitment and signaling. UNC9994 hydrochloride shows a binding affinity with a Ki of 79 nM for D2R. UNC9994 hydrochloride is also an antagonist of Gi-regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9994 hydrochloride shows antipsychotic-like activity.
  • HY-147395
    GPR52 agonist-1

    Others Neurological Disease
    GPR52 agonist-1 is a potent, orally active and blood-brain barrier (BBB) penetrant GPR52 agonist with an pEC50 value of 7.53. GPR52 agonist-1 affects cAMP accumulation through direct interaction with GPR52. GPR52 agonist-1 can significantly suppress Methamphetamine-induced hyperactivity in mice. Antipsychotic activity.
  • HY-B1639
    Enoximone

    Phosphodiesterase (PDE) Inflammation/Immunology Cardiovascular Disease
    Enoximone is an inotropic vasodilating agent and a selective and orally active phosphodiesterase III (PDE3) inhibitor with an IC50 of 5.9 μM. Enoximone induces vasodilatation and increases intracellular levels of cAMP by inhibiting cGMP-inhibited PDE. Enoximone also exhibits PDE4 inhibitory effect with an IC50 of 21.1 μM for myocardial PDE4A. Enoximone has the potential for congestive heart failure research and has bronchodilatory, antiasthma and anti-inflammatory effects.
  • HY-117958
    HJC0197

    Ras Cancer Metabolic Disease Cardiovascular Disease
    HJC0197 is a potent Epac1 (exchange protein directly activated by cAMP 1) and Epac2 (IC50=5.9 μM for Epac2) antagonist. HJC0197 selectively blocks cAMP-induced Epac activation. HJC0197 inhibits Epac1-mediated Rap1-GDP exchange activity at 25 μM in the presence of equal concentration of cAMP.
  • HY-15371
    Forskolin

    Coleonol; Colforsin; HL 362

    Adenylate Cyclase FXR Autophagy Cancer Endocrinology Metabolic Disease Inflammation/Immunology
    Forskolin (Coleonol) is a potent adenylate cyclase activator with an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase. Forskolin is also an inducer of intracellular cAMP formation. Forskolin induces differentiation of various cell types and activates pregnane X receptor (PXR) and FXR. Forskolin exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin also induces autophagy.
  • HY-150057
    CB1R Allosteric modulator 4

    Cannabinoid Receptor Others
    CB1R Allosteric modulator 4 is a positive allosteric modulator of cannabinoid type-1 (CB1R) with good biological activity. CB1R Allosteric modulator 4 inhibits cAMP production and shows robust activity in β-arrestin-2 recruitment.
  • HY-102076
    0990CL

    Others Others
    0990CL is a specific heterotrimeric Gαi subunit inhibitor by direct interaction with Gαi. 0990CL is able to block α2AR mediated regulation of cAMP.
  • HY-106739
    Motapizone

    NAT 05-239

    Phosphodiesterase (PDE) Inflammation/Immunology
    Motapizone (NAT 05-239) is a selective PDE3 inhibitor. Motapizone moderately inhibits cytokine release in lipopolysaccharide (LPS)-induced alveolar macrophages. Motapizone also inhibits human platelet aggregation by increasing intracellular cAMP.
  • HY-100936
    Etazolate hydrochloride

    SQ 20009; EHT 0202 hydrochloride

    Phosphodiesterase (PDE) GABA Receptor Inflammation/Immunology Neurological Disease
    Etazolate hydrochloride (SQ 20009) is an orally active, selective inhibitor of type 4 phosphodiesterase (PDE4) with an IC50 of 2 μM. Etazolate hydrochloride is a γ-aminobutyric acid A (GABAA) receptor regulator. Etazolate hydrochloride is an α-secretase activator and induced the production of soluble amyloid precursor protein (sAPPα). Etazolate hydrochloride, a pyrazolopyridine class derivative, increases cAMP levels. Etazolate hydrochloride has anxiolyticlike, antidepressant-like and anti-inflammatory effects.
  • HY-P0248
    Kemptide

    PKA Metabolic Disease
    Kemptide is a synthetic heptapeptide that acts as a specific substrate for cAMP-dependent protein kinase (PKA).
  • HY-P3930
    PKI (5-24),amide

    IP20-amide

    PKA Neurological Disease
    PKI (5-24),amide (IP20-amide) is a 20-residue peptide that corresponds to the active portion of the heat-stable inhibitor protein of cAMP-dependent protein kinase. PKI (5-24),amide is a potent cAMP-dependent protein kinase (PKA) (PKA) inhibitor with a Ki of 2.3 nM.
  • HY-N0113
    Hordenine

    Ordenina; Peyocactine

    Bacterial Antibiotic Infection Cardiovascular Disease
    Hordenine, an alkaloid found in plants, inhibits melanogenesis by suppression of cyclic adenosine monophosphate (cAMP) production.
  • HY-P0291
    Kemptide Phospho-Ser5

    PKA Others
    Kemptide (Phospho-Ser5) is a phosphate acceptor peptide that serves as a specific substrate for cAMP-dependent protein kinase (PKA).
  • HY-P0228
    Calcineurin substrate

    Autophagy Neurological Disease
    Calcineurin substrate is a peptide from the regulatory RII subunit of cAMP-dependent protein kinase. It can be used in the calcineurin activity assay.
  • 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.
  • HY-14773
    Mirabegron

    YM178

    Adrenergic Receptor Neurological Disease Endocrinology
    Mirabegron is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM.
  • HY-14773S
    (Rac)-Mirabegron-d5

    (Rac)-YM178-d5

    Adenosine Receptor Metabolic Disease
    (Rac)-Mirabegron-d5 is a deuterium labeled (Rac)-Mirabegron. (Rac)-Mirabegron is the racemate of Mirabegron. Mirabegron is a selective β3-adrenoceptor agonist[1].
  • HY-P3572
    Adipokinetic hormone I (Locusta migratoria)

    Lom-AKH-I

    Endogenous Metabolite Endocrinology
    Adipokinetic hormone I (Locusta migratoria) (Lom-AKH-I) is a insect adipokinetic hormone (AKH), enhances fat body cAMP levels in vitro. Insect adipokinetic hormones (AKHs) controls flight-directed mobilization of carbohydrate and lipid from fat body stores, which depends on AKH receptor(s) coupling to cAMP formation and glycogen phosphorylase activation via the stimulatory guanine nucleotide-binding protein (Gs).
  • HY-P3570
    Adipokinetic hormone II (Locusta migratoria)

    Lom-AKH-II

    Endogenous Metabolite Metabolic Disease
    Adipokinetic hormone II (Locusta migratoria) (Lom-AKH-II) is a insect adipokinetic hormone (AKH), enhances fat body cAMP levels in vitro. Insect adipokinetic hormones (AKHs) controls flight-directed mobilization of carbohydrate and lipid from fat body stores, which depends on AKH receptor(s) coupling to cAMP formation and glycogen phosphorylase activation via the stimulatory guanine nucleotide-binding protein (Gs).
  • HY-100013C
    2-PCCA hydrochloride

    GPR88 Neurological Disease
    2-PCCA hydrochloride is a GPR88 receptor agonist, and inhibits GPR88-mediated cAMP production, with an EC50 of 116 nM in HEK293 cells.
  • HY-N3324
    Mangostanol

    (+)-Mangostanol

    Phosphodiesterase (PDE) Others
    Mangostanol ((+)-Mangostanol) is a polyoxygenated xanthone mangostanol, which can be isolated from the shell of Garcinia mangostana, and has inhibitory effect on cAMP phosphodiesterase (PDE).
  • HY-137638
    Sp-5,6-DCl-cBIMPS

    PKA Metabolic Disease
    Sp-5,6-DCl-cBIMPS is a potent and specific cAMP-dependent protein kinases (cAMP-PK) activator. Sp-5,6-DCl-cBIMPS stimulates insulin release. Sp-5,6-DCl-cBIMPS inhibits U46619-induced activation of Rho, Gq and G12/G13 in platelets.
  • HY-16642A
    LY2828360

    Cannabinoid Receptor Neurological Disease
    LY2828360 is a slowly acting but efficacious G protein-biased cannabinoid (CB2) agonist, inhibiting cAMP accumulation and activating ERK1/2 signaling.
  • HY-P0228A
    Calcineurin substrate TFA

    Autophagy Metabolic Disease
    Calcineurin substrate (TFA) is a peptide from the regulatory RII subunit of cAMP-dependent protein kinase. Calcineurin substrate (TFA) can be used in the calcineurin activity assay.
  • HY-111896
    7-Methoxyrosmanol

    7-O-Methoxyrosmanol

    Others Others
    7-Methoxyrosmanol (7-O-Methoxyrosmanol), a phenolic diterpene isolated from rosemary, suppresses the cAMP responsiveness of PEPCK and G6Pase promoters.
  • HY-106358A
    Andolast

    CR 2039; Dizolast

    Phosphodiesterase (PDE) Inflammation/Immunology
    Andolast (CR 2039) is an anti-allergic agent. Andolast can inhibit cAMP-phosphodiesterase with an IC50 value of 50 μM. Andolast can be used for the research of asthma.
  • HY-107046
    UK-432097

    Adenosine Receptor Inflammation/Immunology
    UK-432097 is a highly potent and selective A2AAR agonist with a pKi of 8.4 for human A2AAR. UK-432097 has anti-inflammatory and anti-aggregatory properties. UK-432097 has the potential for COPD (Chronic Obstructive Pulmonary Disease) research.
  • HY-103547
    L-168049

    GCGR Metabolic Disease
    L-168049 is a potent, selective, orally active and non-competitive glucagon receptor antagonist with IC50s of 3.7 nM, 63 nM, and 60 nM for human, murine, and canine glucagon receptors, respectively.
  • HY-111082
    ISAM-140

    Adenosine Receptor Others
    ISAM-140 (22b) is a potent and highly selective A2B adenosine receptor antagonist with a Ki of 3.49 nM.
  • HY-P1291
    PKI 14-22 amide,myristoylated

    PKA Cancer
    PKI 14-22 amide,myristoylated is a potent cAMP-dependent PKA inhibitor. PKI 14-22 amide,myristoylated reduces the IgG-mediated phagocytic response and also inhibits neutrophil adhesion.
  • HY-106358
    Andolast free base

    CR 2039 free base; Dizolast free base

    Phosphodiesterase (PDE) Inflammation/Immunology
    Andolast (CR 2039) (free base) is an anti-allergic agent. Andolast can inhibit cAMP-phosphodiesterase with an IC50 value of 50 μM. Andolast can be used for the research of asthma.
  • HY-119168
    LP-471756

    GPR139 Neurological Disease
    LP-471756 is a potent GPR139 antagonist with an IC50 value of 640 nM. LP-471756 inhibits LP-360924-stimulated cAMP production.
  • HY-B1505
    Acefylline

    Theophyllineacetic acid; Theophylline-7-acetic acid

    Adenosine Receptor Protein Arginine Deiminase Phosphodiesterase (PDE) Cancer
    Acefylline (Theophyllineacetic acid), a xanthine derivative, is an adenosine receptor antagonist. Acefylline is a peptidylarginine deiminase (PAD) activator. Acefylline is also a bronchodilator, which inhibits rat lung cAMP phosphodiesterase isoenzymes.
  • HY-N0113S
    Hordenine-d6

    Ordenina-d6; Peyocactine-d6

    Isotope-Labeled Compounds Bacterial Antibiotic Infection Cardiovascular Disease
    Hordenine-d6 (Ordenina-d6) is the deuterium labeled Hordenine. Hordenine, an alkaloid found in plants, inhibits melanogenesis by suppression of cyclic adenosine monophosphate (cAMP) production.
  • HY-P1291A
    PKI 14-22 amide,myristoylated TFA

    PKA Cancer
    PKI 14-22 amide,myristoylated TFA is a potent cAMP-dependent PKA inhibitor. PKI 14-22 amide,myristoylated TFA reduces the IgG-mediated phagocytic response and also inhibits neutrophil adhesion.
  • HY-101572
    MHP

    Methyl caprooyl tyrosinate

    SphK Inflammation/Immunology Cancer
    MHP (Methyl caprooyl tyrosinate) is an activator of sphingosine kinase (SPHK1), and significantly stimulates CAMP mRNA and protein production. MHP (Methyl caprooyl tyrosinate) enhances antimicrobial defense and innate immunity.
  • HY-134598A
    653-47 hydrochloride

    Epigenetic Reader Domain Cancer
    653-47 hydrochloride, a potentiator, significantly potentiates the cAMP-response element binding protein (CREB) inhibitory activity of 666-15. 653-47 hydrochloride is also a very weak CREB inhibitor with IC50 of 26.3 μM.
  • HY-134598
    653-47

    Epigenetic Reader Domain Cancer
    653-47, a potentiator, significantly potentiates the cAMP-response element binding protein (CREB) inhibitory activity of 666-15. 653-47 is also a very weak CREB inhibitor with IC50 of 26.3 μM.
  • HY-108539
    CE3F4

    Ras Cardiovascular Disease
    CE3F4 is a selective antagonist of exchange protein directly activated by cAMP (Epac1), with IC50s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively.
  • HY-115769
    1,2-Didecanoylglycerol

    PKC Endocrinology
    1,2-Didecanoylglycerol, a synthetic diacylglycerol, is metabolized by platelets to 1,2-didecanoylphosphatidic acid (PA10) and activates protein kinase C (PKC).
  • HY-12525
    LGD-6972

    GCGR Metabolic Disease
    LGD-6972 is a selective and orally active glucagon receptor antagonist. LGD-6972 has the potential for type 2 diabetes research.
  • HY-112612A
    RTI-13951-33 hydrochloride

    GPR88 Neurological Disease
    RTI-13951-33 hydrochloride is a potent, selective, and brain-penetrant GPR88 agonist, with an EC50 of 25 nM in GPR88 cAMP functional assay. RTI-13951-33 hydrochloride reduces alcohol reinforcement and intake behaviors in rats.
  • HY-N8092
    Kushenol B

    Phosphodiesterase (PDE) Infection Inflammation/Immunology
    Kushenol B is an isoprenoid flavonoid isolated from S. flavescens, has antimicrobial, anti-inflammatory and antioxidant activities. Kushenol B has inhibitory activity against cAMP phosphodiesterase (PDE), with an IC50 of 31 µM.
  • HY-112612
    RTI-13951-33

    GPR88 Neurological Disease
    RTI-13951-33 is a potent, selective, and brain-penetrant GPR88 agonist, with an EC50 of 25 nM in GPR88 cAMP functional assay. RTI-13951-33 reduces alcohol reinforcement and intake behaviors in rats.
  • HY-P1290A
    PKA Inhibitor Fragment (6-22) amide TFA

    PKI-(6-22)-amide TFA

    PKA Neurological Disease
    PKA Inhibitor Fragment (6-22) amide TFA is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide TFA can significantly reverse antinociceptive tolerance in mice.
  • HY-116874
    SKF 83822

    Dopamine Receptor Neurological Disease
    SKF 83822 is an atypical agonist of dopamine D1 receptor. SKF 83822 activates adenylyl cyclase, but not PLC. SKF 83822 is also proved to stimulate AC via cAMP production. SKF 83822 can be used for research of schizophrenia.
  • HY-P1290
    PKA Inhibitor Fragment (6-22) amide

    PKI-(6-22)-amide

    PKA Neurological Disease
    PKA Inhibitor Fragment (6-22) amide is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide can significantly reverse low-level morphine antinociceptive tolerance in mice.
  • HY-118941
    BAY 73-1449

    Prostaglandin Receptor Cardiovascular Disease
    BAY 73-1449 is a selective antagonist of prostacyclin receptor (IP), with high potency (IC50 of less than 0.1 nM) in cAMP assays in Human HEL cells and rat DRG. BAY 73-1449 can be used in the research of lowering blood pressure.
  • HY-150073
    DS01080522

    Others Cancer
    DS01080522 is a Protein Kinase cAMP-Activated Catalytic Subunit Alpha (PRKACA) inhibitor. DS01080522 inhibits PRKACA kinase activity and CREB phosphorylation with IC50s of 0.8 nM and 66 nM, respectively. DS01080522 can be used for the research of cancer.
  • HY-P0222
    PKI(5-24)

    PKA Others
    PKI(5-24) is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor.
  • HY-103194
    KH7

    Adenylate Cyclase Others
    KH7 is a soluble adenylyl cyclase (sAC)-specific inhibitor, with IC50s of 3-10 μM toward both recombinant purified human sACt protein and heterologously expressed sACt in cellular assays. KH7 is also a cAMP inhibitor.
  • HY-103254
    ML221

    Apelin Receptor (APJ) Arrestin Neurological Disease
    ML221 is a potent apelin (APJ) functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC50s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC80 of 10 nM in both assays.
  • HY-147751
    APJ receptor agonist 6

    Apelin Receptor (APJ) Arrestin Cardiovascular Disease
    APJ receptor agonist 6 (compound 9) is a potent APJ (apelin receptor) agonist, with Ki of 1.3 μM. APJ receptor agonist 6 has EC50 values of 0.070 , 0.097, and 0.063 μM for calcium, cAMP, and β-arrestin, respectively.
  • HY-P0222A
    PKI(5-24) TFA

    PKA Others
    PKI(5-24) TFA is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) TFA corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor.
  • HY-108258
    PSN 375963

    GPR119 Endocrinology
    PSN 375963 is a potent GPR119 agonist, with EC50s of 8.4 and 7.9 μM for human and mouse GPR119, respectively. PSN 375963 shows similar potency to the endogenous agonist oleoylethanolamide (OEA).
  • HY-18978
    GR79236

    Adenosine Receptor Inflammation/Immunology
    GR79236 is a highly potent, selective and orally active adenosine A1 receptor agonist with a Kis of 3.1 nM and 1300 nM for A1 and A2 receptors, respectively. GR79236 has anti-nociceptive and anti-inflammatory actions.
  • HY-120687
    A68930

    Dopamine Receptor Cancer
    A68930, as a dopamine D1 receptor agonist, can be used for the research of bronchiectasis.
  • HY-116530
    9-Cyclopentyladenine monomethanesulfonate

    9-CP-Ade mesylate

    Adenylate Cyclase Neurological Disease Others
    9-Cyclopentyladenine monomethylsulfonate (9-CP-Ade mesylate) is a stable non-competitive adenylate cyclase inhibitor with cell permeable properties.
  • HY-P2285
    AC 253

    Amyloid-β Neurological Disease
    AC 253, an amylin antagonist, inhibits 125I-adrenomedullin binding, with an IC50 of 25 nM.
  • HY-103431
    A68930 hydrochloride

    Dopamine Receptor Others
    A68930 hydrochloride, as a dopamine D1 receptor agonist, can be used for the research of bronchiectasis.
  • HY-108258A
    PSN 375963 hydrochloride

    GPR119 Endocrinology
    PSN 375963 hydrochloride is a potent GPR119 agonist, with EC50s of 8.4 and 7.9 μM for human and mouse GPR119, respectively. PSN 375963 hydrochloride shows similar potency to the endogenous agonist oleoylethanolamide (OEA).
  • HY-123820
    LY3020371 hydrochloride

    mGluR Neurological Disease
    LY3020371 hydrochloride is a potent, selective metabotropic glutamate 2/3 receptor (mGlu2/3) antagonist with Ki of 5.3 and 2.5 nM, potently blocks cAMP formation with IC50 of 16.2 nM. LY3020371 hydrochloride exerts an antidepressant-like signature in vivo.
  • HY-126250
    NPD-1335

    Phosphodiesterase (PDE) Parasite Infection Inflammation/Immunology
    NPD1335 is a Trypanosoma brucei phosphodiesterase B1 (TbrPDEB1) inhibitor with submicromolar activities against T. brucei parasites. NPD1335 displays a greatly improved cytotoxicity profile. NPD1335 increases intracellular cAMP levels and results in the distortion of the cell cycle and cell death.
  • HY-120879
    PF2562

    Dopamine Receptor Neurological Disease
    PF2562 (Example 6), a dopamine D1 ligand, ascts as a dopamine D1 agonist or partial agonist. PF2562 binds to human D1 receptor with a Ki of 113 nM. PF2562 exhibits activity against human D1 cAMP with an EC50 of 568 nM in HTRF assay.
  • HY-108742
    Abaloparatide

    BA 058; BIM 44058

    Thyroid Hormone Receptor Arrestin Metabolic Disease
    Abaloparatide (BA 058) is a parathyroid hormone receptor 1 (PTHR1) analog. Abaloparatide also is a selective PTHR1 activator. Abaloparatide enhances Gs/cAMP signaling and β-arrestin recruitment. Abaloparatide enhances bone formation and cortical structure in mice. Abaloparatide has the potential for the research of osteoporosis.
  • HY-B1481A
    Isoetharine

    Isoetarine

    Adrenergic Receptor Inflammation/Immunology Cardiovascular Disease
    Isoetharine (Isoetarine) is an orally active selective agonist of β-adrenergic receptors. Isoetharine is a catechol-like agent and catechol O-methyltransferase (COMT) mediates its methylation. Isoetharine can promote the production of cAMP which stimulates the relaxation of smooth muscle cells and can be used as an emphysema, bronchitis and bronchodilator.
  • HY-113689
    GAT211

    Cannabinoid Receptor Neurological Disease
    GAT211 is a cannabinoid 1 receptor (CB1R) positive allosteric modulator (PAM). GAT211 activates cAMP and β-arrestin2 with EC50 values of 260 nM and 650 nM, respectively. GAT211 inhibits GAT211 can be used for neuropathic and/or inflammatory pain research.
  • HY-B1481
    Isoetharine mesylate

    Isoetarine mesylate

    Adrenergic Receptor Inflammation/Immunology Cardiovascular Disease
    Isoetharine (Isoetarine) mesylate is an orally active selective agonist of β-adrenergic receptors. Isoetharine mesylate is a catechol-like agent and catechol O-methyltransferase (COMT) mediates its methylation. Isoetharine mesylate can promote the production of cAMP which stimulates the relaxation of smooth muscle cells and can be used as an emphysema, bronchitis and bronchodilator.
  • HY-N6901
    Luteolin 7-sulfate

    Epigenetic Reader Domain Metabolic Disease
    Luteolin 7-sulfate is isolated from Phyllospadix iwatensis Makino, a marine plant. Luteolin 7-sulfate attenuates TYR gene expression through the intervention of a cAMP-responsive element binding protein (CREB)- and microphthalmia-associated transcription factor (MITF)-mediated signaling pathway, leading to the decreased melanin synthesis.
  • HY-129421
    PA-9

    Others Inflammation/Immunology Neurological Disease
    PA-9 is a pituitary adenylate cyclase-activating polypeptide (PACAP) type I (PAC1) receptor antagonist. PA-9 dose dependently inhibits PACAP-induced cAMP elevation with an IC50 of 5.6 nM. PA-9 can be used for the research of neuropathic and/or inflammatory pain.
  • HY-110161
    sst2 Receptor agonist-1

    Somatostatin Receptor Endocrinology Cardiovascular Disease
    sst2 Receptor agonist-1 is a potent somatostatin receptor subtype 2 (sst2) agonist with a Ki value of 0.025 nM and a cAMP IC50 value of 4.8 nM. sst2 Receptor agonist-1 can inhibit rat growth hormone (GH) secretion and ocular neovascular lesion formation. Antiangiogenic effect.
  • HY-P2197A
    ELA-11(human) TFA

    Apelin Receptor (APJ)
    ELA-11(human) TFA is a high affinity apelin receptor agonist (Ki=14 nM). ELA-11(human) TFA is a bioactive fragment of ELA-32. ELA-11(human) TFA inhibits forskolin-induced cAMP production and stimulates β-arrestin recruitment in vitro.
  • HY-19026
    Siguazodan

    SKF 94836

    Phosphodiesterase (PDE) Cardiovascular Disease
    Siguazodan (SKF 94836) is a potent, selective and orally active phosphodiesterase III (PDE-III) inhibitor with an IC50 of 117 nM. Siguazodan increases cAMP accumulation in intact platelets with an EC50 of 18.88 μM. Siguazodan also inhibits phenylephrine-induced 5-HT release with an IC50 value of 4.2 μM.
  • HY-125957
    A-3 hydrochloride

    PKA Casein Kinase CaMK PKC Others
    A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
  • HY-50906
    LY404039

    mGluR Neurological Disease
    LY404039 is a potent, selective and orally active mGluR2 and mGluR3 agonist with Kis of 149 nM and 92 nM for recombinant human mGluR2 and mGluR3, respectively. LY404039 shows >100-fold selectivity for mGluR2/3 over other receptors/transproters. LY404039 has antipsychotic and anxiolytic effects.
  • HY-12887
    Piclamilast

    RP 73401; RPR 73401

    Phosphodiesterase (PDE) Cancer Inflammation/Immunology
    Piclamilast (RP 73401) is a phosphodiesterase 4 (PDE4) inhibitor, with IC50 values of 16 nM and 2 nM in pig aorta and eosinophil soluble, respectively.
  • HY-14899
    Taprenepag

    CP-544326

    Prostaglandin Receptor Endocrinology
    Taprenepag (CP-544326) is a potent and selective prostaglandin EP(2) agonist with IC50s of 10 and 15 nM for human and rat EP2, respectively. Taprenepag shows selectivity for EP2 over other EP receptors (IC50s>3200 nM for EP1, EP3, and EP4) and a panel of 37 G protein-coupled receptors.
  • HY-N6256
    Ilexsaponin B2

    Phosphodiesterase (PDE) Cardiovascular Disease
    Ilexsaponin B2 is a saponin isolated from the root of Ilex pubescens Hook. et Arn. Ilexsaponin B2 is a potent phosphodiesterase 5 (PDE5) and PDEI inhibitor with IC50 values of 48.8 μM and 477.5 μM, respectively.
  • HY-10301
    MK-3207

    CGRP Receptor Neurological Disease
    MK-3207 is an orally active, highly selective and species-specific CGRP receptor antagonist (for human CGRP receptor: IC50=0.12 nM; Ki=0.024 nM). MK-3207 can be used for migraine studies.
  • HY-100543
    Zenidolol

    ICI-118551

    Adrenergic Receptor Inflammation/Immunology
    Zenidolol (ICI-118551) is a selective β2 adrenergic receptor antagonist. Zenidolol inhibits β2-, β1- and β3-adrenergic receptor with Ki values of 0.7, 49.5 and 611 nM, respectively. Zenidolol can be used as an ocular hypotensive agent used for ophthalmic disease research.
  • HY-18286
    NCGC00229600

    TSH Receptor Endocrinology
    NCGC00229600 is an allosteric inverse agonist of thyrotropin receptor (TSHR). NCGC00229600 inhibits both TSH and stimulating antibody activation of TSHRs endogenously expressed in Graves' disease.
  • HY-100984
    HA-100

    PKA PKC Myosin ROCK Cancer
    HA-100 is a potent protein kinase inhibitor, with IC50s of 4 μM, 8 μM, 12 μM and 240 μM for cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase, respectively. HA-100 also used as a ROCK inhibitor.
  • HY-N1860
    3-O-Methylquercetin

    Phosphodiesterase (PDE) Inflammation/Immunology
    3-O-Methylquercetin (3-MQ), a main constituent of Rhamnus nakaharai, inhibits total cAMP and cGMP-phosphodiesterase (PDE) of guinea pig trachealis. 3-O-Methylquercetin (3-MQ) exhibits IC50 values ranging from 1.6-86.9 μM for PDE isozymes (PDE1-5).
  • HY-100984A
    HA-100 hydrochloride

    PKA PKC Myosin ROCK Cancer
    HA-100 hydrochloride is a potent protein kinase inhibitor, with IC50s of 4 μM, 8 μM, 12 μM and 240 μM for cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase, respectively. HA-100 hydrochloride also used as a ROCK inhibitor.
  • HY-14302
    Salmeterol

    GR33343X

    Adrenergic Receptor Endocrinology Inflammation/Immunology
    Salmeterol (GR33343X) is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively.
  • HY-P1250
    RFRP-3(human)

    Neuropeptide VF(124-131)(human)

    Neuropeptide Y Receptor Neurological Disease
    RFRP-3 (Neuropeptide VF(124-131))(human), a human GnIH peptide homolog, is a potent inhibitor of gonadotropin secretion by inhibiting Ca 2+ mobilization. RFRP-3(human) is a NPFF1 receptor agonist, it inhibits forskolin-induced production of cAMP with an IC50 of 0.7 nM.
  • HY-17453
    Salmeterol xinafoate

    GR 33343X xinafoate

    Adrenergic Receptor Inflammation/Immunology Endocrinology
    Salmeterol (GR 33343X) xinafoate is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively.
  • HY-P2867
    Phosphodiesterase II

    Phosphodiesterase (PDE) Neurological Disease
    Phosphodiesterase II, namely phosphodiesterase 2, is mainly involved in the hydrolysis of the important second messengers cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP), and is often used in biochemical research. Phosphodiesterase II is expressed in a variety of tissues, such as the adrenal medulla, brain, heart, platelets, macrophages and endothelial cells, and is involved in the regulation of many different intracellular processes.
  • HY-108742A
    Abaloparatide TFA

    BA 058 TFA; BIM 44058 TFA

    Thyroid Hormone Receptor Arrestin Metabolic Disease Endocrinology
    Abaloparatide TFA (BA 058 TFA) is a parathyroid hormone receptor 1 (PTHR1) analogue. Abaloparatide TFA also is a selective PTHR1 activator. Abaloparatide TFA enhances Gs/cAMP signaling and β-arrestin recruitment. Abaloparatide TFA enhances bone formation and cortical structure in mice. Abaloparatide TFA has the potential for the research of osteoporosis.
  • HY-P4823
    pTH (1-37) (human)

    Thyroid Hormone Receptor Metabolic Disease
    pTH (1-37) (human) is a fragment of parathyroid hormone (PTH). pTH (1-37) (human) induces the cAMP formation and increases alkaline phosphatase activity. pTH (1-37) (human) increases growth, bone calcium content, and bone mineral density (BMD) in uremic animals. pTH (1-37) (human) has the potential for the research of osteoporosis.
  • HY-103193
    NKH477

    Colforsin dapropate hydrochloride

    Adenylate Cyclase Cardiovascular Disease
    NKH477 (Colforsin dapropate hydrochloride) directly activates the catalytic unit of adenylate cyclase and increases intracellular cAMP. NKH477 is a forskolin derivative that improves cardiac failure mainly through its beneficial effects on diastolic cardiac function. NKH477 exerts an antiproliferative effect in vivo with an altered cytokine profile to inhibit the acute rejection of rat orthotopic lung allografts.
  • HY-128932
    Cefminox sodium

    MT-141

    Bacterial PPAR Prostaglandin Receptor Antibiotic Infection Cardiovascular Disease Endocrinology
    Cefminox sodium (MT-141) is a semisynthetic cephamycin, which exhibits a broad spectrum of antibacterial activity. Cefminox sodium (MT-141) also acts as a dual agonist of prostacyclin receptor (IP) and PPARγ, upregulates cAMP production and PTEN expression and inhibits Akt/mTOR signaling. Cefminox sodium (MT-141) also prevents pulmonary arterial hypertension.
  • HY-P1250A
    RFRP-3(human) TFA

    Neuropeptide VF(124-131)(human) TFA

    Neuropeptide Y Receptor Neurological Disease
    RFRP-3 (Neuropeptide VF(124-131))(human) TFA, a human GnIH peptide homolog, is a potent inhibitor of gonadotropin secretion by inhibiting Ca 2+ mobilization. RFRP-3(human) is a NPFF1 receptor agonist, it inhibits forskolin-induced production of cAMP with an IC50 of 0.7 nM.
  • HY-15478
    WZ811

    CXCR Cancer Endocrinology
    WZ811 is an orally active, highly potent competitive antagonist of CXCR4. WZ811 efficiently inhibits CXCR4/SDF-1 (or CXCL12)-mediated modulation of cAMP levels (EC50=1.2 nM) and SDF-1 induced Matrigel invasion in cells (EC50=5.2 nM).
  • HY-135119
    Salmeterol-D3

    Adrenergic Receptor Endocrinology Inflammation/Immunology
    Salmeterol-d3 is a deuterium labeled Salmeterol. Salmeterol is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively[1].
  • HY-19436
    Solabegron

    GW 427353

    Adrenergic Receptor Metabolic Disease Endocrinology
    Solabegron (GW 427353) is a selective β3-adrenergic receptor agonist, stimulating cAMP accumulation in Chinese hamster ovary cells expressing the human β3-AR, with an EC50 value of 22 nM. Solabegron (GW 427353) is being developed for the treatment of overactive bladder and irritable bowel syndrome.
  • HY-17034B
    Medetomidine hydrochloride

    MPV785

    Adrenergic Receptor Endocrinology Neurological Disease
    Medetomidine hydrochloride is an orally active α2-adrenoceptor agonist (Ki: 1.08 nM). Medetomidine hydrochloride has sedative and analgesic effects. Medetomidine hydrochloride can cause peripheral vasoconstriction through the activation of α2 adrenoceptors on blood vessels.
  • HY-101232
    Tiotidine

    ICI 125211

    Histamine Receptor Cardiovascular Disease
    Tiotidine (ICI 125211) is a potent and selective antagonist of histamine H2-receptor (pA2=7.3-7.8 for guinea-pig right atrium). Tiotidine has low affinity for both the H1 and the H3 receptors.
  • HY-17034
    Medetomidine

    Adrenergic Receptor Neurological Disease Endocrinology
    Medetomidine is an orally active α2-adrenoceptor agonist (Ki: 1.08 nM). Medetomidine has sedative and analgesic effects. Medetomidine can cause peripheral vasoconstriction through the activation of α2 adrenoceptors on blood vessels.
  • HY-P3544
    Lys-[Hyp3]-Bradykinin

    Bradykinin Receptor Inflammation/Immunology
    Lys-[Hyp3]-Bradykinin a Bradykinin (HY-P0206) agonist. Lys-[Hyp3]-Bradykinin is a kinin, it can be isolated from human urine. Lys-[Hyp3]-Bradykinin can be used for the research of inflammation.
  • HY-U00341
    ST4206

    Adenosine Receptor Neurological Disease
    ST4206 is a potent and orally active adenosine A2A receptor antagonist, with Kis of 12 nM and 197 nM for adenosine A2A receptor and adenosine A1 receptor, respectively. ST4206 has the potential for Parkinson׳s disease research.
  • HY-148867
    UCM-1306

    2-(Fluoromethoxy)-4'-(S-methylsulfonimidoyl)-1,1'-biphenyl

    Dopamine Receptor Neurological Disease
    UCM-1306 is a potent and orally active human dopamine D1 receptor allosteric modulator (PAM). UCM-1306 increases the endogenous dopamine (DA) maximal effect both in human and mouse D1 receptors. UCM-1306 is not only for improving motor symptoms but also for addressing the key comorbid cognitive impairment associated with long-term Parkinson’s disease (PD).
  • HY-P1845A
    PACAP-38 (31-38), human, mouse, rat TFA

    ERK EGFR Reactive Oxygen Species Calcium Channel Neurological Disease
    PACAP-38 (31-38), human, mouse, rat TFA is a PAC1 receptor activator and increases the α-secretase activity. PACAP-38 (31-38), human, mouse, rat TFA elevates cytosolic Ca 2+, increases proliferation and increases phosphorylation of extracellular regulates kinase (ERK) and the epidermal growth factor receptor (EGFR). PACAP-38 (31-38), human, mouse, rat TFA demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production. PACAP-38 (31-38), human, mouse, rat TFA can be used for neurotrophic and neuroprotective research.
  • HY-124696
    PU139

    Histone Acetyltransferase Cancer
    PU139 is a potent pan-histone acetyltransferase (HAT) inhibitor. PU139 blocks the HATs Gcn5, p300/CBP-associated factor (PCAF), CREB (cAMP response element-binding) protein (CBP) and p300 with IC50s of 8.39, 9.74, 2.49 and 5.35 μM, respectively.
  • HY-P0036B
    Octreotide pamoate

    SMS 201-995 pamoate

    Somatostatin Receptor Apoptosis Cancer Endocrinology Inflammation/Immunology Cardiovascular Disease
    Octreotide (SMS 201-995) pamoate is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue. Octreotide pamoate can bind to the somatostatin receptors which are mainly subtypes 2, 3 and 5. Octreotide pamoate increases Gi activity and reduces intracellular cAMP production. Octreotide pamoate has antitumor activity, mediates apoptosis and may also be used in disease studies in acromegaly.
  • HY-P0036
    Octreotide

    SMS 201-995

    Somatostatin Receptor Apoptosis Cancer Endocrinology Inflammation/Immunology Cardiovascular Disease
    Octreotide (SMS 201-995) is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue. Octreotide (SMS 201-995) can bind to the somatostatin receptor and mainly subtypes 2, 3, and 5, increases Gi activity, and reduces intracellular cAMP production. Octreotide (SMS 201-995) has antitumor activity, mediates apoptosis and may also be used in disease studies in acromegaly.
  • 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.
  • HY-P2878
    Phosphodiesterase

    PDE

    Phosphodiesterase (PDE) Neurological Disease
    Phosphodiesterase (PDE) is an enzyme that can catalyze the hydrolysis of the 3' ring phosphate bond of cyclic nucleotides, and is often used in biochemical research. Phosphodiesterase acts as an important regulator of signal transduction mediated by the second messenger molecules cAMP and cGMP. According to their specificity to cyclic nucleotides, they can also be divided into different types, such as PDE1-PDE11, which also have certain potential in various diseases.
  • HY-17453S
    Salmeterol-d3 xinafoate

    GR 33343X-d3 (xinafoate)

    Adrenergic Receptor Inflammation/Immunology Endocrinology
    Salmeterol-d3 (xinafoate) is the deuterium labeled Salmeterol xinafoate. Salmeterol (GR 33343X) xinafoate is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively[1].
  • HY-128656
    LML134

    Histamine Receptor Neurological Disease Endocrinology
    LML134 (compound 18b) is an orally active and high selective Histamine 3 receptor (H3R) inverse agonist with Kis of 0.3 nM and 12 nM for hH3R cAMP and hH3R bdg. LML134 penetrates the brain rapidly, leading to high H3R occupancy, and disengages its target with a fast kinetic profile. LML134 has the potential for excessive sleep disorders.
  • HY-130304
    8-Isoprostaglandin E2

    iPE2-III

    Prostaglandin Receptor Cardiovascular Disease
    8-Isoprostaglandin E2 (iPE2-III) is a member of the isoprostane class of prostanoids. 8-Isoprostaglandin E2 acts at the receptor for thromboxane A2 (the TP) in vivo to induce vasoconstriction and platelet aggregation. 8-Isoprostaglandin E2 enhances receptor-activated NFkappa B ligand (RANKL)-dependent osteoclastic potential of marrow hematopoietic precursors via the cAMP pathway.
  • HY-N6727
    Gliotoxin

    Aspergillin

    Apoptosis PKA NF-κB Bacterial Fungal Antibiotic Infection Inflammation/Immunology
    Gliotoxin is a secondary metabolite, the most abundant mycotoxin secreted by A. fumigatus, inhibits the phagocytosis of macrophages and the immune functions of other immune cells . Gliotoxin inhibits inducible NF-κB activity by preventing IκB degradation, which consequently induces host-cell apoptosis. Gliotoxin activates PKA and increases intracellular cAMP concentration; modulates actin cytoskeleton rearrangement to facilitate A. fumigatus internalization into lung epithelial cells.
  • HY-P4817
    Human PTH-(1-31)

    Thyroid Hormone Receptor Metabolic Disease
    Human PTH-(1-31) is the 1-31 fragment of human PTH. Human PTH-(1-31) stimulates the release of cAMP and also is a weaker stimulator of the 25-hydroxyvitamin D-1α-hydroxylase. Human PTH-(1-31) induces bone formation without inducing bone resorption. Human PTH-(1-31) has the potential for the research of osteoporosis.
  • HY-17453S1
    Salmeterol-13C6 xinafoate

    GR 33343X-13C6 (xinafoate)

    Adrenergic Receptor Inflammation/Immunology Endocrinology
    Salmeterol- 13C6 (xinafoate) is the 13C6 labeled Salmeterol (xinafoate). Salmeterol (GR 33343X) xinafoate is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively.
  • HY-17592
    Bithionol

    Parasite Bacterial Cancer Infection
    Bithionol is an antibacterial, anthelmintic, and algaecide agent. Bithionol is also a potent inhibitor of soluble adenylyl cyclase through binding to the allosteric activator site (IC50: 4 μM).
  • HY-P1296
    Urocortin, rat

    Urocortin (Rattus norvegicus); Rat urocortin;

    CRFR Neurological Disease Endocrinology
    Urocortin, rat (Urocortin (Rattus norvegicus)) is a neuropeptide and a potent endogenous CRFR agonist with Kis of 13 nM, 1.5 nM, and 0.97 nM for human CRF1, rat CRF and mouse CRF, respectively.
  • HY-124571
    ZQ-16

    GPR84 Inflammation/Immunology
    ZQ-16 is a potent and selective GPR84 agonist with an EC50 value of 0.213 μM. ZQ-16 has no activity on the other free fatty acid receptors (FFARs), including GPR40, GPR41, GPR119 and GPR120.
  • HY-142972
    19(S)-HETE

    Prostaglandin Receptor Cardiovascular Disease
    19(S)-HETE is an arachidonic acid metabolite produced by cytochrome P450 enzymes. 19(S)-HETE is a full orthosteric agonist of the prostacyclin (IP) receptor with an EC50 value of 567 nM. 19(S)-HETE inhibits platelet activation and relaxation of vessels.
  • HY-149247
    Antipsychotic agent-2

    5-HT Receptor Dopamine Receptor Neurological Disease
    Antipsychotic agent-2 (Compound 11) is a potent antipsychotic agent. Antipsychotic agent-2 shows affinities for 5-HT1A, 5-HT2A, 5-HT2C, D2 and H1 receptors with Kis of 56.6, 66.7, 552, 596 and 1140 nM, respectively. Antipsychotic agent-2 has BBB permeability.
  • HY-119486A
    (Rac)-Tavapadon

    (Rac)-PF-06649751; (Rac)-CVL-751

    Dopamine Receptor Arrestin Neurological Disease
    (Rac)-Tavapadon ((Rac)-PF-06649751) is a potent and selective noncatechol dopamine D1 receptor agonist. (Rac)-Tavapadon displays potent full agonism in the GS activation assay as well as partial agonism in the β-arrestin2 recruitment assay (GS-cAMP, EC50=0.8 nM; β-arrestin2, EC50=68 nM). (Rac)-Tavapadon has antiparkinsonian activity.
  • HY-103565
    AMN082

    mGluR Neurological Disease
    AMN082, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects.
  • HY-16558
    Butein

    2’,3,4,4’-tetrahydroxy Chalcone

    EGFR Autophagy Apoptosis Phosphodiesterase (PDE) Cancer
    Butein is a cAMP-specific PDE inhibitor with an IC50 of 10.4 μM for PDE4. Butein is a specific protein tyrosine kinase inhibitor with IC50s of 16 and 65 μM for EGFR and p60 c-src in HepG2 cells. Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a. Butein is a SIRT1 activator (STAC).
  • HY-W127485
    cis-9,10-Methyleneoctadecanoic Acid

    DIHYDROSTERCULIC ACID

    Biochemical Assay Reagents Others
    cis-9,10-Methyleneoctadecanoic acid is a cyclopropane fatty acid that has been found in bacteria and in the digestive glands of P. globosa. It is a component of the cell membrane of Staphylococcus aureus, and levels were reduced after treatment with carvacrol. cis-9,10-Methyleneoctadecanoic acid is secreted by H. pylori and enhances histamine- and dibutyryl cAMP-stimulated acid secretion in isolated guinea pig parietal cells. It also activates protein kinase C (PKC) in a calcium-dependent manner.
  • HY-P1106
    K41498

    CRFR Cardiovascular Disease
    K41498 is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF, CRF and CRF1 receptors respectively. K41498 is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF- and hCRF-expressing cells. K41498 can be used for hypotension study.
  • HY-P0097A
    Nonapeptide-1 acetate salt

    Melanostatine-5 acetate salt

    Melanocortin Receptor Cancer Endocrinology Metabolic Disease
    Nonapeptide-1 (Melanostatine-5) acetate salt, a peptide hormone, is a selective antagonist of MC1R (Ki: 40 nM). Nonapeptide-1 acetate salt is a competitive α-MSH antagonist that potently inhibits intracellular cAMP and melanosome dispersion induced by α-MSH in melanocytes (IC50: 2.5 nM and 11 nM, respectively). Nonapeptide-1 acetate salt inhibits melanin synthesis, and can be used in the research of skin pigmentation and regulation of steroid production in the adrenal gland, skin cancer.
  • HY-108539A
    (R)-CE3F4

    Ras Metabolic Disease
    (R)-CE3F4 is a potent and selective inhibitor of exchange protein directly activated by cAMP isoform 1 (Epac1), with an IC50 of 4.2 μM, with 10-fold selectivity for Epac1 over Epac2 (IC50, 44 μM). (R)-CE3F4 is more potent than racemic CE3F4 and (S)-CE3F4.
  • HY-103565A
    AMN082 free base

    mGluR Neurological Disease
    AMN082 free base, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 free base potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 free base shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects.
  • HY-P0097
    Nonapeptide-1

    Melanostatine-5

    Melanocortin Receptor Cancer Endocrinology Metabolic Disease
    Nonapeptide-1 (Melanostatine-5), a peptide hormone, is a selective antagonist of MC1R (Ki: 40 nM). Nonapeptide-1 is a competitive α-MSH antagonist that potently inhibits intracellular cAMP and melanosome dispersion induced by α-MSH in melanocytes (IC50: 2.5 nM and 11 nM, respectively). Nonapeptide-1 inhibits melanin synthesis, and can be used in the research of skin pigmentation and regulation of steroid production in the adrenal gland, skin cancer.
  • HY-105118A
    Zaldaride maleate

    CGS-9343B; KW 5617

    nAChR Metabolic Disease Inflammation/Immunology Neurological Disease
    Zaldaride maleate (CGS-9343B) is a potent, orally active and selective inhibitor of calmodulin. Zaldaride maleate (CGS-9343B) inhibits CaM (calmodulin)-stimulated cAMP phosphodiesterase activity, with an IC50 of 3.3 nM. Zaldaride maleate (CGS-9343B) prevents estrogen-induced transcription activation by ER, reversibly blocks voltage-activated Na +, Ca 2+ and K + currents in PC12 cells and inhibits nAChR.
  • HY-N2118
    Bilobetin

    PPAR PKA Metabolic Disease
    Bilobetin, an active component of Ginkgo biloba, can reduce blood lipids and improve the effects of insulin. Bilobetin ameliorated insulin resistance, increased the hepatic uptake and oxidation of lipids, reduced very-low-density lipoprotein triglyceride secretion and blood triglyceride levels, enhanced the expression and activity of enzymes involved in β-oxidation and attenuated the accumulation of triglycerides and their metabolites in tissues. Bilobetin also increased the phosphorylation, nuclear translocation and activity of PPARα accompanied by elevated cAMP level and PKA activity.
  • HY-N3773
    Dodoviscin A

    Tyrosinase Cancer
    Dodoviscin A is a pigmentation-altering agent, which can be isolated from the aerial parts of Dodonaea viscosa. Dodoviscin A inhibits melanin production in B16-F10 melanoma cells. Dodoviscin A suppresses mushroom tyrosinase activity, and tyrosinase activity induced by 3-isobutyl-1-methylxanthine. Dodoviscin A also inhibits the phorphosylation of cAMP response element binding protein, induced by 3-isobutyl-1-methylxanthine and forskolin.
  • HY-P1065
    Apelin-36(rat, mouse)

    HIV Infection Metabolic Disease Cardiovascular Disease
    Apelin-36(rat, mouse) is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-36(rat, mouse) binds to APJ receptors with an IC50 of 5.4 nM, and potently inhibits cAMP production with an EC50 of 0.52 nM. Apelin-36(rat, mouse) blocks entry of some HIV-1 and HIV-2 strains into NP-2/CD4 cells expressing APJ.
  • HY-P1845
    PACAP-38 (31-38), human, mouse, rat

    ERK EGFR Reactive Oxygen Species Calcium Channel Neurological Disease
    PACAP-38 (31-38), human, mouse, rat is a PAC1 receptor activator and increases the α-secretase activity. PACAP-38 (31-38), human, mouse, rat elevates cytosolic Ca 2+, increases proliferation and increases phosphorylation of extracellular regulates kinase (ERK) and the epidermal growth factor receptor (EGFR). PACAP-38 (31-38), human, mouse, rat demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production. PACAP-38 (31-38), human, mouse, rat can be used for neurotrophic and neuroprotective research.
  • HY-14550
    TP-10

    Phosphodiesterase (PDE) Neurological Disease Cardiovascular Disease
    TP-10 is a selective PDE10A inhibitor with an IC50 value of 0.8 nM. TP-10 shows an antioxidant activity with IC50s of 31.72 and 16.04 μg/ml for DPPH and CUPRAC, respectively. TP-10 can be used for the research of neuropathy.
  • HY-P1296A
    Urocortin, rat TFA

    Urocortin (Rattus norvegicus) (TFA); Rat urocortin TFA

    CRFR Endocrinology Neurological Disease
    Urocortin, rat TFA (Urocortin (Rattus norvegicus) TFA) is a neuropeptide and a potent endogenous CRFR agonist with Kis of 13 nM, 1.5 nM, and 0.97 nM for human CRF1, rat CRF and mouse CRF, respectively.
  • HY-103302
    SUN B8155

    CGRP Receptor Endocrinology
    SUN B8155, a non-peptide agonist of calcitonin (CT) receptor, selectively mimics the biological actions of calcitonin. Calcitonin, a 32-amino acid peptide hormone secreted mainly from the thyroid gland, plays an important role in maintaining bone homeostasis.
  • HY-149164
    BTB09089

    Others Inflammation/Immunology Neurological Disease
    BTB09089 is a T cell death-associated gene 8 (TDAG8/GPR65) specific agonist. BTB09089 increases TDAG8 expression and regulates the cytokine production of T cells and macrophages.
  • HY-P0172
    ATI-2341

    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).
  • HY-P2847
    Urocortin II, mouse

    CRFR Endocrinology Metabolic Disease
    Urocortin II, mouse is a potent and selective endogenous peptide agonist of type-2 corticotropin-releasing factor (CRF2) receptor with Ki values of 0.66 nM and ﹥100 nM for CRFR2 and CRFR1, respectively. Urocortin II, mouse activates CRF2 receptors in a cAMP/PKA- and Ca 2+/CaMKII-dependent manner.Urocortin II, mouse is expressed in discrete areas of the central nervous system, and activates central neurons involved in the processing of visceral sensory information, and in modulating autonomic outflow.
  • HY-P0172A
    ATI-2341 TFA

    CXCR Cancer Inflammation/Immunology Endocrinology
    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).
  • HY-P1106A
    K41498 TFA

    CFTR Cardiovascular Disease
    K41498 TFA is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF, CRF and CRF1 receptors respectively. K41498 TFA is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF- and hCRF-expressing cells. K41498 TFA can be used for hypotension study.
  • HY-P1065A
    Apelin-36(rat, mouse) TFA

    HIV Infection Metabolic Disease Cardiovascular Disease
    Apelin-36(rat, mouse) TFA is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-36(rat, mouse) TFA binds to APJ receptors with an IC50 of 5.4 nM, and potently inhibits cAMP production with an EC50 of 0.52 nM. Apelin-36(rat, mouse) TFA blocks entry of some HIV-1 and HIV-2 strains into NP-2/CD4 cells expressing APJ.
  • HY-129658
    TT-OAD2 free base

    GCGR Metabolic Disease
    TT-OAD2 free base is a non-peptide glucagon-like peptide-1 (GLP-1) receptor agonist with an EC50 of 5 nM. TT-OAD2 free base has the potential for diabetes treatment.
  • HY-100403
    Ro 67-7476

    mGluR Cancer
    Ro 67-7476 is a potent positive allosteric modulator of mGluR1 and potentiates glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a with an EC50 of 60.1 nM. Ro 67-7476 is a potent P-ERK1/2 agonist and activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC50=163.3 nM).
  • HY-103369
    PG01

    CFTR Endocrinology
    PG01 is a potent CFTR Cl - channel potentiator. PG01 can correct gating defects of CFTR mutants, is effective on b>E193K, G970R and G551D (CFTR mutants) with Kd values of 0.22 μM, 0.45 μM and 1.94 μM, respectively. PG01 is also effective on ΔF508 (Ka of 0.3 μM). PG01 increases ΔF508-CFTR Cl - current after adding Forskolin.
  • HY-124717
    YC-001

    Endogenous Metabolite Others
    YC-001 is an inverse agonist and antagonist of rod opsin. YC-001 reversibly binds rod opsin and stabilizes the rod opsin structure. YC-001 protects mice from bright light-induced retinal degeneration. YC-001 has the potential for the research of retinal degeneration.
  • HY-14973
    Vidupiprant

    AMG 853

    Prostaglandin Receptor Inflammation/Immunology
    Vidupiprant (AMG 853) is a phenylacetic acid derivative. Vidupiprant is a potent and orally active CRTH2 (DP2) and prostanoid D receptor (DP or DP1) dual antagonist with IC50s of 3 nM and 4 nM in buffer, and 8 nM and 35 nM in human plasma, respectively. Vidupiprant has the potential for asthma treatment.
  • HY-16635
    Setipiprant

    ACT-129968; KYTH-105

    Prostaglandin Receptor Inflammation/Immunology Endocrinology
    Setipiprant (ACT-129968) is an orally active and selective CRTH2 antagonist. Setipiprant interacts with hCRTH2 receptor with an IC50 value of 6 nM. Setipiprant inhibits prostanoid receptors hDP1 and hEP2 with IC50 values of 1290 and 2600 nM, respectively. Setipiprant can be used for the research of asthma and rhinitis.
  • HY-128358
    MR-L2

    Phosphodiesterase (PDE) Neurological Disease
    MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4), activates representative PDE4 long-isoform variants (PDE4A4, PDE4B1, PDE4C3, PDE4D5). MR-L2 suppresses PGE2-induced MDCK cell cyst formation with an EC50 of 1.2 µM.
  • HY-129658A
    TT-OAD2

    GCGR Metabolic Disease
    TT-OAD2 is a non-peptide glucagon-like peptide-1 (GLP-1) receptor agonist with an EC50 of 5 nM. TT-OAD2 has the potential for diabetes treatment.
  • HY-109139
    Taminadenant

    NIR178; PBF509

    Adenosine Receptor Cancer Neurological Disease
    Taminadenant (NIR178; PBF509) is a highly potent and orally active adenosine A2A receptor (A2AR) antagonist. Taminadenant can antagonize A2AR agonist-mediated cAMP accumulation and impedance responses with KB values of 72.8 nM and 8.2 nM, respectively. Taminadenant reverses motor impairments in several rat models of movement disorders, including catalepsy, tremor, and hemiparkinsonism. Taminadenant can also inhibit tumor growth when combined with Spartalizumab (HY-P9972). Taminadenant reactivate the antitumor immune response.
  • HY-N2038
    3,​5,​6,​7,​8,​3',​4'-​Heptemthoxyflavone

    Phosphodiesterase (PDE) Cancer Neurological Disease
    3,5,6,7,8,3',4'-heptamethoxyflavone, a flavonoid in Citrus reticulata peels, exhibits anti-tumor-initiating effect and Anti-neuroinflammatory activity. 3,5,6,7,8,3',4'-heptamethoxyflavone inhibits collagenase activity and increased type I procollagen content in HDFn cells. 3,5,6,7,8,3',4'-heptamethoxyflavone induces brain-derived neurotrophic factor (BDNF) expression via cAMP/ERK/CREB signaling and reduces phosphodiesterase activity in C6 cells.
  • HY-116818
    Crebinostat

    HDAC Neurological Disease
    Crebinostat is a potent histone deacetylase (HDAC) inhibitor with IC50 values of 0.7 nM, 1.0 nM, 2.0 nM and 9.3 nM for HDAC1, HDAC2, HDAC3 and HDAC6, respectively. Crebinostat potently induces acetylation of both histone H3 and histone H4 as well as enhances the expression of the cAMP response element-binding protein (CREB) target gene Egr1. Crebinostat increases the density of synapsin-1 punctae along dendrites in cultured neurons. Crebinostat can modulate chromatin-mediated neuroplasticity and exhibits enhanced memory in mice.
  • HY-N3945
    Glaucine

    O,O-Dimethylisoboldine; S-(+)-Glaucine; NSC 34396

    Phosphodiesterase (PDE) Calcium Channel Adrenergic Receptor Dopamine Receptor Influenza Virus Infection Inflammation/Immunology
    Glaucine (O,O-Dimethylisoboldine) is an alkaloid isolated from Glaucium flavum with antitussive, bronchodilation and anti-inflammatory properties. Glaucine is a selective and orally active phosphodiesterase 4 (PDE4) inhibitor with Kis of 3.4 µM in human bronchus and polymorphonuclear leukocytes. Glaucine is also a non-selective α-adrenoceptor antagonist, a Ca 2+ entry blocker, and a weak dopamine D1 and D2 receptor antagonist. Glaucine has antioxidative and antiviral activities.
  • HY-P1913A
    Calcitonin Gene Related Peptide (CGRP) II, rat TFA

    CGRP Receptor Cardiovascular Disease
    Calcitonin Gene Related Peptide (CGRP) II, rat TFA, a CGRP receptor activator, is a potent and long-lasting vasodilator. Calcitonin Gene Related Peptide (CGRP) II TFA can be used in the research of cardiovascular diseases.
  • HY-P1913
    Calcitonin Gene Related Peptide (CGRP) II, rat

    CGRP Receptor Cardiovascular Disease
    Calcitonin Gene Related Peptide (CGRP) II, rat, a CGRP receptor activator, is a potent and long-lasting vasodilator. Calcitonin Gene Related Peptide (CGRP) II can be used in the research of cardiovascular diseases.
  • HY-101317
    TAN-67 dihydrobromide

    SB-205607 dihydrobromide

    Opioid Receptor Neurological Disease
    TAN-67 (SB-205607) dihydrobromide is a potent and selective nonpeptidic δ-opioid receptor agonist with a Ki value of 0.647 nM. TAN-67 dihydrobromide has neuroprotective effect. TAN-67 dihydrobromide can be used in research of ischemic stroke.
  • HY-P1471
    Adrenomedullin (AM) (22-52), human

    22-52-Adrenomedullin (human)

    CGRP Receptor Cardiovascular Disease
    Adrenomedullin (AM) (22-52), human, an NH2 terminal truncated adrenomedullin analogue, is an adrenomedullin receptor antagonist, and also antagonizes the calcitonin generelated peptide (CGRP) receptor in the hindlimb vascular bed of the cat.
  • HY-P1471A
    Adrenomedullin (AM) (22-52), human TFA

    22-52-Adrenomedullin (human) (TFA)

    CGRP Receptor Cardiovascular Disease
    Adrenomedullin (AM) (22-52), human (22-52-Adrenomedullin human) TFA, an NH2 terminal truncated adrenomedullin analogue, is an adrenomedullin receptor antagonist. Adrenomedullin (AM) (22-52), human also antagonizes the calcitonin generelated peptide (CGRP) receptor in the hindlimb vascular bed of the cat.
  • HY-N9539
    Phanginin A

    Salt-inducible Kinase (SIK) Metabolic Disease
    Phanginin A is a potent and orally active SIK1 (salt-induced kinase 1) activator. Phanginin A inhibited gluconeogenesis. Phanginin A increases the expression of p-SIK1 and decreases the expression of p-CREB. Phanginin A reduces blood glucose levels and improves glucose tolerance and dyslipidemia. Phanginin A has the potential for the research of type 2 diabetes.
  • HY-10797
    CJ-42794

    CJ-042794

    Prostaglandin Receptor Inflammation/Immunology Endocrinology
    CJ-42794 (CJ-042794) is a potent, orally active, selective prostaglandin E receptor 4 (EP4) antagonist with an IC50 value of 10 nM, which is 200-fold more selective than EP1, EP2 and EP3. CJ-42794 can be used in research of gastric ulcers.
  • HY-107506
    Ro 67-4853

    mGluR Neurological Disease
    Ro 67-4853 is a positive allosteric modulator (PAM) of mGluR1 (pEC50=7.16 for rmGlu1a receptor). Ro67-4853 exhibits activity at all group I mGlu receptors including hmGlu1, rmGlu1, and rmGlu5. Ro 67-4853 enhances the potency of L-Glu by interacting with the transmembrane domain (TMD) of the receptor. Ro 67-4853 potentiates sensory synaptic responses to repetitive vibrissa stimulation.
  • HY-147946
    PDE1-IN-4

    Phosphodiesterase (PDE) Calcium Channel Inflammation/Immunology
    PDE1-IN-4 (compound 2g) is a potent and selective PDE1 (phosphodiesterase-1) inhibitor, with IC50 values of 10, 145, and 354 nM for PDE1C, PDE1A, and PDE1B, respectively. PDE1-IN-4 inhibits myofibroblast differentiation of human lung fibroblasts induced by TGF-β1. PDE1-IN-4 shows anti-fibrosis effects through the regulation of cAMP (3′,5′-cyclic adenosine monophosphate) and cGMP (3′,5′-cyclic guanosine monophosphate). PDE1-IN-4 can be used for idiopathic pulmonary fibrosis (IPF) research.
  • HY-151392
    LPA5 antagonist 2

    Others Inflammation/Immunology Neurological Disease
    LPA5 antagonist 2 (compound 65) is a high aqueous solubility LPA5 (lysophosphatidic acid receptor 5) antagonist. LPA5 antagonist 2 significantly attenuates nociceptive hypersensitivity and it can be used for the research of inflammatory and neuropathic pains.
  • HY-112363
    Aloisine A

    RP107

    CDK GSK-3 ERK JNK CFTR Cancer Inflammation/Immunology
    Aloisine A (RP107) is a a potent cyclin-dependent kinase (CDK) inhibitor with IC50s of 0.15 μM, 0.12 μM, 0.4 μM, 0.16 μM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK5/p35, respectively. Aloisine A ininhibits GSK-3α (IC50=0.5 μM) and GSK-3β (IC50=1.5 μM). Aloisine A stimulates wild-type CFTR and mutated CFTR, with submicromolar affinity by a cAMP-independent mechanism. Aloisine A has the potential for CFTR-related diseases, including cystic fibrosis research.