ca inhibitor 1

CA inhibitor 1 (GS-6207 analog) is a potent inhibitor of the HIV capsid.

NLRP3-IN-NBC6 is a potent, selective NLRP3 inflammasome inhibitor with an IC50 of 574 nM. It acts independently of Ca 2+ and inhibits Nigericin-induced inflammasome activation in THP-1 cells, as well as Imiquimod-induced IL-1β release from LPS-primed bone marrow-derived macrophages (BMDMs) [1].

Verapamil hydrochloride (Verapamil HCl) is a calcium channel blocker that is a class IV anti-arrhythmia agent.

I-XW-053 is a micromolar affinity inhibitor of capsid-targeted HIV-1 replication, utilizing a hybrid structure-based method to block the interface between CA N-terminal domains (NTD-NTD interface).

Verapamil (CP-16533-1) is a calcium channel blocker and an orally active and effective inhibitor of P-gp. Verapamil inhibits CYP3A4 and can be used in studies about the treatment of high blood pressure, heart arrhythmias, and angina research.

Halofuginone specifically inhibits collagen type I gene expression and matrix metalloproteinase 2 (MMP-2) gene expression, which may result in the suppression of angiogenesis, tumor stromal cell development, and tumor cell growth. Halofuginone Hydrobromide is the hydrobromide salt of halofuginone, a semisynthetic quinazolinone alkaloid anticoccidial derived from the plant Dichroa febrifuga, with antifibrotic and potential antineoplastic activities. These effects appear to be due to halofuginone-mediated inhibition of the collagen type I and MMP-2 promoters. Collagen type I and MMP-2 play important roles in fibroproliferative diseases.

Ziconotide Acetate (107452-89-1 free base) (Prialt) is an analgesic agent and has been used to treat neuropathic and non-neuropathic pain. Ziconotide Acetate (107452-89-1 free base) acts by binding to N-type calcium channels situated on the terminal part of primary afferent neurons of the nociceptive pathway therefore reducing synaptic transmission with potent antinociceptive effects.

Ca2+ channel agonist 1 is an agonist of N-type Ca2+ channel and an inhibitor of Cdk2 (EC50s: 14.23 μM and 3.34 μM) and is used as a potential treatment for motor nerve terminal dysfunction.

Cav 2.2 blocker 1 is an N-type calcium channel (Cav 2.2; IC50: 1 nM) blocker for the treatment of pain.

PF-3450074 (PF-74) acts at an early stage of HIV-1 infection inhibits viral replication by directly competing with the binding of CPSF6 (nuclear host factors cleavage and polyadenylation specific factor 6) and NUP153 (nucleoporin 153), and blocks the uncoating, assembly, and the reverse transcription steps of the viral life cycle. PF-3450074 is a specifical inhibitor of HIV-1 capsid protein (CA) and shows a broad-spectrum inhibition of HIV isolates with submicromolar potency (EC50=8-640 nM).

Enpp Carbonic anhydrase-IN-1 (compound 1e) is a potent inhibitor of Enpp and carbonic anhydrase, exhibiting IC50s of 1.36, 1.35, 3.00, 0.88, and 1.02 µM for NPP1, NPP2, NPP3, CA-II, and CA-IX respectively. Enpp Carbonic anhydrase-IN-1 also demonstrates selective antiproliferative activity for cancer cells.

4-(benzyloxy)benzene-1-sulfonamide is inhibitor of human recombinant CA-7.

Fasudil (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK.

Norverapamil hydrochloride (D591 hydrochloride) ((±)-Norverapamil hydrochloride) is an N-demethylated metabolite of Verapamil and it is an L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.

SERCA2a activator 1 is a sarco endoplasmic reticulum Ca2+-dependent ATPase 2a activator. SERCA2a activator 1 decreases phospholamban inhibition and enhances the systolic and diastolic functions of the heart.

TGR5 is a potent TGR5(GPCR19) agonist.

CAⅡ-IN-1 (compound 2i) is an inhibitor of the CA Ⅱ isozyme, exhibiting an IC50 of 0.44 µM. This compound is utilized in metabolic research.

AChE CA I-IN-1 (Compound 2g) acts as an inhibitor for both AChE and hCA I, with Ki values of 1.85 µM and 0.53 µM, respectively. It has shown potential applications in the research of Alzheimer's disease, glaucoma, and epilepsy.

AChE hCA I-IN-1 (Compound L3) is an inhibitor of acetylcholinesterase (AChE) and carbonic anhydrase (CA), effectively inhibiting AChE, hCA I, and hCA II with IC50 values of 302 nM, 265 nM, and 283 nM, respectively.

PACOCF3 (Palmityltrifluoromethylketone) (Palmityltrifluoromet hylketone) is an inhibitor of Ca(2+)-independent phospholipase A2(PLA2) with an IC 50 of 3.8 μM. PACOCF3 alters Ca 2+ signaling in renal tubular cells [1] [2].

OBAA is a potent inhibitor of phospholipase A2 (PLA2) with an IC 50 of 70 nM. OBAA blocks Melittin-induced Ca 2+ influx in Trypanosoma brucei with an IC 50 of 0.4 μM [1] [2] [3].

Almorexant (ACT 078573) is a potent and competitive dual orexin 1 receptor (OX1) orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively.

N-desethyl Brinzolamide is an active metabolite of the carbonic anhydrase (CA) inhibitor brinzolamide .1It inhibits CAII and CAIV activities (IC50s = 1.28 and 128 nM, respectively). 1.Kim, C.-Y., Whittington, D.A., Chang, J.S., et al.Structural aspects of isozyme selectivity in the binding of inhibitors to carbonic anhydrases II and IVJ. Med. Chem.45(4)888-893(2002)

O-desmethyl Brinzolamide is an active metabolite of the carbonic anhydrase (CA) inhibitor brinzolamide .1,2It inhibits CAII and CAIV (IC50s = 0.136 and 165 nM, respectively).1 1.Huang, Q., Rui, E.Y., Cobbs, M., et al.Design, synthesis, and evaluation of NO-donor containing carbonic anhydrase inhibitors to lower intraocular pressureJ. Med. Chem.58(6)2821-2833(2015) 2.Lo Faro, A.F., Tini, A., Gottardi, M., et al.Development and validation of a fast ultra-high-performance liquid chromatography tandem mass spectrometry method for determining carbonic anhydrase inhibitors and their metabolites in urine and hairDrug Test Anal.13(8)1552-1560(2021)