Adenylate Cyclase Inhibitor

SQ22536 is an effective adenylate cyclase (AC) inhibitor.

2',5'-Dideoxyadenosine is a potent and non-competitive adenylyl cyclase inhibitor via binding the P-site with an IC₅₀ of 3 µM . 2',5'-Dideoxyadenosine is a nucleoside analog and exerts a potent antiadrenergic action in heart.

cGAS-IN-9 is a cyclic guanosine monophosphate-adenosine monophosphate synthase (cGAS) inhibitor, with IC₅₀ values of 27.5 nM and 5.15 μM against human and murine cGAS, respectively. cGAS-IN-9 shows weak inhibitory activity against human soluble adenylate cyclase, with an IC₅₀ of 26.4 μM. cGAS-IN-9 inhibits dsDNA-induced expression of IFNB1 and CXCL10, as well as activation of the NF-κB pathway, in human immune cells. cGAS-IN-9 can be used in research related to cGAS-dependent inflammatory diseases.

MDL12330A (RMI12330A) is an adenylyl cyclases inhibitor. MDL12330A can inhibit K_V channels, increases insulin secretion and Ca²⁺ levels. MDL12330A accentuates contractions in uterine rings and inhibits cardiac functions. MDL12330A can be used for the research of endocrinology, metabolic and cardiovascular disease .

ST034307 is a potent and selective adenylyl cyclase 1 (AC1) inhibitor, with IC₅₀ of 2.3 μM.

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

TDI-11861 is an orally active soluble sAC inhibitor optimized and designed based on TDI-10229 (HY-132298), with an IC₅₀ of 3.3 nM and a K_D of 1.4 nM. TDI-11861 has advantages such as high affinity, slow dissociation, and good pharmacokinetics. TDI-11861 can be used for research on male contraception and related sAC pharmacology.

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

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

Zelminemab (AMG-301) is a humanized monoclonal antibody that inhibits PACAP type I (PAC1) receptor.

CCPA (2-Chloro-N6-cyclopentyladenosine) a highly selective A1 adenosine receptors agonist with a K_i of 0.4 nM. CCPA inhibits adenylate cyclase with an IC₅₀ of 33 nM. CCPA exhibits anti-seizure and cardiacprotective activity. CCPA can be used for the research of seizure and myocardial infarction.

Fipexide, a parachloro-phenossiacetic acid derivative, is an orally active nootropic agent. Fipexide reduces striatal adenylate cyclase activity. Fipexide has positive effect on cognitive performance by dopaminergic neurotransmission. Fipexide is used for senile dementia research. Fipexide acts as a chemical inducer in callus formation, shoot regeneration and Agrobacterium infection.

Fipexide hydrochloride, a parachloro-phenossiacetic acid derivative, is an orally active nootropic agent. Fipexide hydrochloride reduces striatal adenylate cyclase activity. Fipexide hydrochloride has positive effect on cognitive performance by dopaminergic neurotransmission. Fipexide hydrochloride is used for senile dementia research. Fipexide hydrochloride acts as a chemical inducer in callus formation, shoot regeneration and Agrobacterium infection.

NB001 (HTS 09836) is an adenylcyclase 1 (AC1) inhibitor which has effect on neural and non-neural pain by modulating AC1 activity.

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

Guanosine 5'-O-(2-thiodiphosphate) trisodium (GDPβS trisodium) is a non-hydrolyzable derivative of GDP. Guanosine 5'-O-(2-thiodiphosphate) trisodium acts as an inhibitor of adenylyl cyclase (AC) with a K_i value of 600 nM. In the absence of glutamic-pyruvic transaminase (GPT) in cerebral cortex membranes of rodent models, Guanosine 5'-O-(2-thiodiphosphate) trisodium partially activates AC with an EC₅₀ of 400 nM. Guanosine 5'-O-(2-thiodiphosphate) trisodium prevents norepinephrine-induced nitric oxide release in ventricular myocytes.

9-Cyclopentyladenine monomethylsulfonate (9-CP-Ade mesylate) is a stable non-competitive adenylate cyclase inhibitor with cell permeable properties.

CB-7921220 is an adenylate cyclase inhibitor.

Angiopeptin TFA, a cyclic octapeptide analogue of somatostatin, is a weak sst₂/sst₅ receptor partial agonist with IC₅₀ values of 0.26 nM and 6.92 nM, respectively. Angiopeptin TFA is a potent inhibitor of growth hormone release and insulin-like growth factor-1 (IGF-1) production. Angiopeptin TFA inhibits adenylate cyclase or stimulates extracellular acidification. Angiopeptin TFA has the potential for coronary atherosclerosis research.

Hadacidin is a competitive inhibitor of adenylate synthase. Hadacidin binds to the active site of adenylate synthase, competitively inhibiting L-aspartate binding. Hadacidin can be used in drug design, to help develop new inhibitors or activators to regulate adenylate synthase activity, and to play a role in the study of related diseases.