ap 5

α1A-adrenoceptor antagonist

AP5 is a potent and selective agonist for the GPR40 receptor with positive allosteric modulation of endogenous ligands (AgoPAM). AP5 demonstrates a rat hIP1 EC50 of 0.49 nM against the GPR40 receptor.

T-5224 is a transcription factor c-Fos AP-1 inhibitor that specifically inhibits the DNA-binding activity of c-Fos c-Jun without affecting other transcription factors.

AP-C2 is a potent small molecule guanosine 3',5'-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII) inhibitor with a pIC50 of 5.2 for cGKII.

NPEC-caged-D-AP5 is a NMDA receptor antagonist.

AP-C3 is a potent inhibitor of guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII), with a pIC50 value of 6.3, and demonstrates only weak inhibition of cGKII-dependent anion secretion [1].

12(S)-HpETE is a monohydroperoxy polyunsaturated fatty acid (PUFA) produced by the action of platelet or leukocyte 12-lipoxygenase (12-LO) on arachidonic acid. It activates human blood leukocyte 5-LOE. 12(S)-HpETE is the mediator of many biological functions, including induction of c-fos and c-jun, activation of AP-1, and endothelium-dependent vasoconstriction. It mediates the inhibitory synaptic response to FMRF-amide in Aplysia sensory neurons and inhibits Ca2+ calmodulin-dependent protein kinase II from rat brain cortex.

1,3,5-Trihydroxy-4-prenylxanthone is a relatively potent inhibitor of phosphodiesterase type 5 (PDE5) with an IC50 of 3.0 μM; it exhibits in vitro inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with IC50 values of 56.3plusmn;0.4 and 46.0plusmn;0.3 M, respectively. It also inhibits LPS-induced NF-κB and AP-1 activations by interfering with the posttranslational modification (phosphorylation and or ubiquitinylation) of IRAK-1, disrupting TAK1-mediated activation of IKK and MAPKs signal transduction.

DL-AP5 Sodium salt is a NMDA receptor antagonist.

L-AP5 is a NMDA antagonist.

AP-C5 is a compound with selective inhibition of guanosine 3',5' cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII), with a Pic50 value of 7.2 for cGMP, and can be used in the study of diarrheal diseases.

BGC-20-1531 hydrochloride(1186532-61-5 free base) (GTPL3380 hydrochloride) is a EP4 antagonist for the treatment of acute migraine.

Torilin is an inhibitor of testosterone 5 alpha-reductase, it (IC50 = 31.7 + - 4.23 microM) shows a stronger inhibition of 5 alpha-reductase than alpha-linolenic acid (IC50 = 160.3 + - 24.62 microM) but is weaker than finasteride (IC50 = 0.38 + - 0.06 microM). Torilin has immunomodulatory, hepatoprotective, and anti-inflammatory properties, it inhibits inflammation by limiting TAK1-mediated MAP kinase and NF-κB activation, it can attenuate arthritis severity, modify leukocyte activations in dLNs or joints, and restore serum and splenocyte cytokine imbalances. Torilin inhibits melanin production in alpha-melanocyte stimulating hormone-activated B16 melanoma cells, with an IC(50) value of 25 microM. Torilin shows excellent antimicrobial activity against Bacillus subtilis ATCC 6633 spores and vegetative cells. Torilin has a potent anti-angiogenic activity both in vivo and in vitro, and it may have a strong activity to suppress tumorigenesis by inhibition of tumor invasion, it reverses multidrug-resistance in cancer cells, it can potentiate the cytotoxicities of adriamycin, vinblastine, taxol and colchicine against multidrug-resistant KB-V1 and MCF7 ADR cells.

AP521 is an agonist of the human 5-HT1A receptor (IC50: 94 nM).

3-O-Methylgallic acid (3,4-Dihydroxy-5-methoxybenzoic acid) reduces cell proliferation in Caco-2 cells (IC50 = 24.1 μM) more effectively than anthocyanins and may offer protection against colon cancer after its formation in the gut. It inhibits transcription factors NF-κB, AP-1, STAT-1, and OCT-1, which are known to be activated in colorectal cancer.

DL-AP5 is the racemic form of a selective N-methyl-D-aspartate (NMDA) receptor antagonist with anticonvulsant effects.

D-AP5 (D-APV) is an NMDA receptor antagonist.

AP-521, a 5-HT1A receptor antagonist, is used potentially for the treatment of anxiety.

AP-C4 is a selective inhibitor targeting guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII), exhibiting a pIC50 value of 5.2. Conversely, AP-C3 does not inhibit cGKII-mediated anion secretion [1].

AP-C6 is a potent inhibitor of guanosine 3',5'-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII), with a pIC50 of 6.5. It inhibits human cGKII activity in vitro in a concentration-dependent manner and potentiates cAMP signaling through phosphodiesterase (PDE) inhibition [1].