adenylyl

Adenylyl cyclase-IN-1 is a potential adenylyl cyclase inhibitor for ocular hypotonia research [1].

Adenylyl cyclase type 2 agonist-1 is a potent adenylyl cyclase type 2 (AC2) agonist (EC50: 90 nM), and it is a potential lead compound in the fight against respiratory diseases.

NKY80 regulates the adenylyl cyclase catalytic activity in heart and lung tissues. NKY80 is a non-competitive inhibitor of adenylyl cyclase type V isoform (IC50s: 8.3 µM, 132 µM, and 1.7 mM for type V, III and II, respectively).

Forskolin (Coleonol) is a natural product, an adenylate cyclase activator (EC50=0.5 μM). Forskolin increases cAMP levels, activates PXR and FXR, and induces autophagy. Forskolin produces positive inotropic effects in the heart, and has platelet anticoagulant and antihypertensive effects.

Fipexide (Attentil, Vigilor), a psychoactive drug of the piperazine chemical class, was developed in Italy in 1983. It was served as a nootropic drug in France and Italy, mainly for the therapy of senile dementia, but is no longer in common use because of the occurrence of rare drug side-effects including hepatitis and fever.

Theophylline (1,3-Dimethylxanthine) is a methyl xanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac, and central nervous system stimulant activities. It inhibits the 3', 5'-cyclic nucleotide phosphodiesterase that degrades cyclic AMP, thus potentiating the actions of agents that act through adenylyl cyclases and cyclic AMP.

Potent, selective agonist of Mu-opioid receptor. Antinociceptive. Stimulates calcium-activated adenylyl cyclases related cAMP production. Expresses chemokines and chemokine receptors through TGF-beta1. Increases food intake of rats.

NB001 (HTS 09836) is an adenyl cyclase 1 inhibitor that affects both neural and non-neural pain.

α-MSH (MSH, amide) is amide stimulates melanocortin 1 receptor that results in the activation of adenylyl cyclase.

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.

Adenosine 5'-monophosphate monohydrate (5'-AMP) , also known as 5'-adenylic acid, is a nucleotide that is used as a monomer in RNA. It is an ester of phosphoric acid and the nucleoside adenosine. Adenosine 5'-monophosphate monohydrate consists of a phosphate group, the sugar ribose, and the nucleobase adenine. As a substituent it takes the form of the prefix adenylyl-.

SQ22536 (9-(tetrahydrofuran-2-yl)-9h-purin-6-amine) , the adenosine analogue 9-(Tetrahydro-2-furyl)adenine, inhibited adenylate cyclase activity of crude membrane preparations from catfish (Ictalurus melas) and rat isolated hepatocytes in a non-competitive manner.

2',5'-Dideoxyadenosine is a potent and non-competitive adenylyl cyclase inhibitor, binding to the P-site with an IC50 of 3 μM.

ST034307 is an effective and selective inhibitor of adenylyl cyclase 1 (IC50: 2.3 μM).

BMS-986122 (BMS 986122) is a positive allosteric modulator of μ-opioid receptors that increases β-arrestin recruitment stimulated by endomorphin 1 in U2OS-OPRM1 human osteosarcoma cells expressing μ-opioid receptors (EC50 = 3 μM).

Deacetylforskolin is a diterpene and a derivative of forskolin that has been found inC. forskohliiand has diverse biological activities.1,2,3,4It activates rat adipocyte adenylyl cyclase (IC50= 20 μM) and inhibits glucose transport in rat adipocyte plasma membranes.2Deactylforskolin (30-1,000 μg/kg) reduces blood pressure in spontaneously hypertensive rats.3It also attenuates hypercapnia-induced impairments in the passive avoidance response in mice.4 1.Gabetta, B., Zini, G., and Danieli, B.Minor Diterpenoids of Coleus forskohliiPhytochemistry28(3)859-862(1989) 2.Joost, H.G., Habberfield, A.D., Simpson, I.A., et al.Activation of adenylate cyclase and inhibition of glucose transport in rat adipocytes by forskolin analogues: structural determinants for distinct sites of actionMol. Pharmacol.33(4)449-453(1988) 3.Bhat, S.V., Dohadwalla, A.N., Bajwa, B.S., et al.The antihypertensive and positive inotropic diterpene forskolin: Effects of structural modifications on its activityJ. Med. Chem.26(4)486-492(1983) 4.McCulloch, A.J., Thomson, T.A., and Deacon, R.Hypoxic amnesia and its reversal with forskolinBiochem. Soc. Trans.17(1)212-213(1988)

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.

Human PTH-(1-31) amide, an analog of PTH, effectively stimulates phosphatidylcholine hydrolysis and promotes the release of adenylyl cyclase [1].

Mant-GTPγS, an effective GTP analog, displays strong competitive inhibition of adenylyl cyclase (AC). Additionally, it acts as a potent inhibitor of YdeH.

Lysipressin ([Lys8]-Vasopressin), Induces contraction of the rabbit urinary bladder smooth muscle, activate adenylate-cyclase. Lysipressin is Antidiuretic hormone that have been found in pigs and some marsupial families.

Carsatrin succinate is the salt form of Carsatin, a purinylpiperazine derivative used as a cardiotonic and antiarrhythmic. Carsatrin acts as positive inotropic agent that increases twitch tension and prolongs the action potential (AP) duration of ventricular muscle without affecting the Na+, K+-ATPase, adenylyl cyclase, phosphodiesterase isozymes, or cardiac myofilaments. Carsatrin’s positive inotropic effect can be prevented by tetrodotoxin but not by the adrenergic antagonists timolol, yohimbine, or prazosin.

Non-hydrolyzable AMP analog. Kir6 (KATP) channel blocker. Inhibits fast axonal transport and stabilizes the interaction of membranous organelles with microtubules. Brady (1985) A novel brain ATPase with properties expected for the fast axonal transport motor. Nature 317 73 PMID:2412134 |Yount et al (1971) Adenylyl imidodiphosphate, an adenosine triphosphate analog containing a P-N-P linkage. Biochemistry 10 2484 PMID:4326768 |Hehl and Neumcke (1994) KATP channels of mouse skeletal muscle: mechanism of channel blockage by AMP-PNP. Eur.Biophys.J. 23 231 PMID:7805625

LRE1 is a specific and allosteric inhibitor of soluble adenylyl cyclase (sAC).

OS-3-106 is a novel arylamide phenylpiperazines, as partial agonists at the D3R in the adenylyl cyclase inhibition assay.

CB7833407 is a selective Adenylyl Cyclase isoform-2 (AC2) inhibitor.

Carsatrin is purinylpiperazine derivative. as cardiotonic and antiarrhythmic. Carsatrin acts as positive inotropic agent that increases twitch tension and prolongs the action potential (AP) duration of ventricular muscle without affecting the Na+, K+-ATPase, adenylyl cyclase, phosphodiesterase isozymes, or cardiac myofilaments. Carsatrin’s positive inotropic effect can be prevented by tetrodotoxin but not by the adrenergic antagonists timolol, yohimbine, or prazosin

RU-0207148 is a novel allosteric soluble adenylyl cyclase (sAC) inhibitor.

CB-6673567 is a selective inhibitor of adenylyl cyclase.

TDI-11861, a second-generation soluble Adenylyl Cyclase (sAC, ADCY10) inhibitor, demonstrates slow dissociation rates and effectively inhibits sAC activity in cells, evidenced by an IC50 value of 5.5 nM.

Potent and selective GPR171 partial agonist (EC50 = 90 nM; 28% inhibition of forskolin activated adenylyl cyclase activity in rat hypothalamic memebranes). Exhibits minimal binding to a panel of ~70 GPCRs and 10 other receptors (<22% of radioligand displaced from the target receptors). Increases neuronal activity in the paraventricular nucleus. Increases food intake and body weight in mice. Wardman et al (2016) Identification of a small-molecule ligand that activates the neuropeptide receptor GPR171 and increases food intake Sci.Signal. 9 PMID:27245612

guanylyl cyclase (GC) and adenylyl cyclase (AC) inhibitor

SKF-83566 is a blood-brain permeable and orally active antagonist of D1-like dopamine receptor and a weaker competitive 5-HT2 receptor antagonist with Ki of 11 nM

CFM 1571 is the free base of CFM 1571 Hydrochloride (C291720), which acts as a soluble guanylyl cyclase (sGC) activator while ignoring adenylyl cyclase.

Glucagon receptor antagonist (pA2 = 7.2 for inhibition of glucagon-induced adenylyl cyclase activation in rat liver membranes); displays no agonist activity. Enhances glucose-stimulated pancreatic insulin release in vitro. Blocks added glucagon-induced hy

AC1-IN-1 is a selective inhibitor of adenylyl cyclase type 1 (AC1, IC50 = 0.54 µM).

The compound is an inactive analog of forskolin(an adenylyl cyclase activator).