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GPCR/G Protein

Cholecystokinin Receptor

Melanin-concentrating Hormone Receptor (MCHR)

(11)

Melanocortin Receptor

Neuropeptide Y Receptor

Prostaglandin Receptor

(199)

Protease-activated Receptor

cAMP

Cyclic adenosine monophosphate (cAMP, cyclic AMP, or 3',5'-cyclic adenosine monophosphate) is a second messenger important in many biological processes. cAMP is a derivative of adenosine triphosphate (ATP) and used for intracellular signal transduction in many different organisms, conveying the cAMP-dependent pathway. It should not be confused with 5'-AMP-activated protein kinase (AMP-activated protein kinase).

Filter HomeSignaling PathwaysGPCR/G ProteincAMP

Eriocalyxin B

TN162084745-95-9

Eriocalyxin B induces apoptosis and cell cycle arrest in pancreatic adenocarcinoma cells through caspase- and p53-dependent pathways, should be considered a candidate for pancreatic cancer treatment; it is a specific inhibitor of STAT3, it directly target

$313

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MRE3008F20

T16132252979-43-4In house

MRE3008F20 is a species-selective and potent adenosine A3 receptor (AA3R) antagonist that inhibits Cl-IB-MECA-induced cAMP production and can be used in glaucoma and asthma studies.13483-88-88-9

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UNC0006

T290611354030-14-0In house

UNC0006 is a beta-inhibitory protein biased D(2)R ligand, and is also an antagonist of G(i)-regulated cAMP production and a partial agonist of D(2)R beta-arrestin-2 interaction. It has antipsychotic activity and is used in the study of neurological disorders.

$293

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TDI-10229

T643552810887-45-5

TDI-10229 is a potent and orally available inhibitor of soluble adenylyl cyclase (sAC, ADCY10), displaying nanomolar inhibition of sAC in both biochemical and cellular assays (IC50 = 195 nM). TDI-10229 exhibits mouse pharmacokinetic properties sufficient to warrant its use as an in vivo tool compound.

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CE3F4

T12616L143703-25-7

CE3F4 is a selective antagonist of exchange protein directly activated by cAMP (Epac1; IC50s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively).

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Torbafylline

T67965105102-21-4In house

Torbafylline, a xanthine derivative, is a phosphodiesterase (PDE) inhibitor that attenuates burn-induced protein hydrolysis in rat skeletal muscle through activation of the PDE4 cAMP EPAC PI3K Akt pathway, and inhibits the enhanced ubiquitin-proteasome-dependent protein hydrolysis in skeletal muscle of cancer- and sepsis-prone rats.

$130

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7-Methoxyrosmanol

TN1334113085-62-4

7-Methoxyrosmanol (7-O-Methylrosmanol) can effectively suppress FSK-induced luciferase expression under the control of the CRE, PEPCK-C and G6Pase gene promoters, it may contribute to its antihyperglycemic activity.

$118

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ESI-09

T2244263707-16-0

ESI-09 is a new-typel noncyclic nucleotide EPAC antagonist.The IC50 values of ESI-09 for EPAC1 and EPAC2 is 3.2 and 1.4 μM, respectively.

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Cited

I942

T24154868145-09-9

I942 is a novel, selective ACyclic nucleotide (NCN) EPAC1 agonist that activates exchange proteins to regulate inflammatory gene expression in human umbilical blood tubes and inhibit pro-inflammatory cytokine signaling associated with cardiovascular disease.

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Rp-cAMPS sodium

T36679142439-94-9

Rp-cAMPS sodium is a phosphorothioate analog of cAMP, a protein kinase A inhibitor and a membrane-permeable cAMP antagonist that inhibits cAMP-dependent protein kinases by blocking cAMP-induced conformational transitions, and can be used in the study of cardiovascular diseases.

$299

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GLP-1R modulator L7-028

T402792648317-95-5

GLP-1R modulator L7-028 is a variant that enhances affinity for GLP-1 and (cAMP) signaling.

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Bithionol

T083097-18-7

Bithionol (Actamer), formerly marketed as an active ingredient in various topical drug products, was shown to be a potent photosensitizer with the potential to cause serious skin disorders. Approvals of the NDA's for bithionol drug products were withdrawn on October 24, 1967.

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3-O-Methylquercetin

TN12661486-70-0

3-O-Methylquercetin is a selective and competitive PDE3 PDE4 inhibitor, and inhibits PDE3 than PDE4 with a low K(m) value; it inhibits total cAMP- and cGMP-phosphodiesterase (PDE) of guinea pig trachealis at low concentrations.

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KH7

T15658330676-02-3

KH7 is a soluble inhibitor of adenylyl cyclase (sAC)-specific. It has 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.

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Cited

0990CL

T13983511514-03-7In house

0990CL is an effective heterotrimer Gαi subunit specific inhibitor, which can interact with purified Go± in GDP-bound state, and can block α2AR mediated cAMP regulation. In the cell model, low concentration of 0990CL could partially restore cAMP level, and high concentration of 0990CL (10μM) began to have negative effects on cell viability.

$213

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Evocarpine

TN112115266-38-3

Evocarpine shows antimycobacterial, and vasorelaxant effects, it can inhibit Ca2+ influx through voltage-dependent calcium channels.

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Lactacystin

T15702133343-34-7

Lactacystin is a natural non-peptide proteasome inhibitor and highly specific anticancer drug that controls the UPS of cellular protein turnover and inhibits alkaline cell proliferation, and is able to be used as a model for studying dementia, induces neurite outgrowth and transiently elevated levels of cAMP, inhibits angiogenesis, triggers apoptosis in glioma cells, and can penetrate the blood-brain barrier (BBB).

$185

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Atherosperminine

TN34665531-98-6

Atherosperminine shows cholinesterase inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Atherosperminine shows strong anti-plasmodial activity against Plasmodium falciparum, with the IC50 value of 5.80 uM, it also s

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HJC0350

T6536885434-70-8

HJC0350 is an effective and specific EPAC2 inhibitor (IC50: 0.3 μM), and no inhibition of Epac1.

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ESI-05

T152475184-64-5

ESI-05 (NSC-116966) is a specific EPAC2 (exchange protein directly activated by cAMP 2) antagonist (IC50: 0.4 μM). ESI-05 inhibits cAMP-mediated activation of EPAC2, as well as EAPC2, mediated Rap1 activation.

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HJC0197

T154851383539-73-8

HJC0197 selectively blocks cAMP-induced Epac activation. HJC0197 is an effective exchange protein. Which straightly activated by cAMP (Epac) antagonist (IC50=5.9 μM for Epac2).

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GAT211

T27405102704-40-5

GAT211 (AZ-4) is a selective and potent cannabinoid 1 receptor (CB1R) orthosteric modulator (PAM) with high affinity for cAMP and β-arrestin2.GAT211 has IOP-lowering and antipsychotic effects and can be used in the study of epilepsy.

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Adenosine receptor A1 antagonist 5

T2246685872-53-3In house

Adenosine receptor A1 antagonist 5 acts as an adenosine antagonist, is an oxypurine, acts as an insecticide and pest control agent, and has an inhibitory effect on elevated blood pressure.

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2-PCCA hydrochloride

T806661609563-70-3In house

2-PCCA hydrochloride, a racemate, is a potent and selective GPR88 receptor agonist showing inhibition of GPR88-mediated cAMP production in HEK293 cells with an EC50 value of 116 nM.

$112

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