Ionizable Lipid Products

PF 05089771 is a Nav1.7 channel blocker extracted from patent WO/2010/079443 A1, compound example 788, has an IC50 of 8.6 nM.

Pyridoxal isonicotinoyl hydrazone (PIH) is a lipophilic, tridentate Fe-chelating agent that shows high Fe chelation efficacy[1].

HM30181 mesylate is a competitive and potent P-glycoprotein inhibitor.

A novel, potent, orally active liver X receptor β (LXRβ) agonist with Ki/EC50 of 3/21 nM, displays 27-fold selectivity over LXRα; also exhibits excellent selectivity against other nuclear hormone receptors (>3,000-fold); induces the expression of LXR target genes in vitro and in vivo.

ASP3026 is a novel and selective inhibitor for ALK (anaplastic lymphoma kinase) with IC50 of 3.5 nM.

Bisantrene is a highly effective antitumor drug, targets eukaryotic type II topoisomerases.

AMD-070 is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively.

GRL0617 is a potent, selective and competitive noncovalent inhibitor of severe acute respiratory syndrome (SARS-CoV) papain-like protease (PLpro)/deubiquitinase, with an IC50 of 0.6 μM, and with a Ki of 0.49 μM[1].

BAY 61-3606 (dihydrochloride) is a potent, ATP-competitive, reversible, and highly selective inhibitor of Syk tyrosine kinase (IC50=10 nM) with no inhibitory effect on Btk, Fyn, Itk, Lyn, and Src.

A potent PD-1/PD-L1 interaction inhibitor with IC50 of 2.25 nM in a homogenous time-resolved fluorescence binding assay.

Asunaprevir is a potent hepatitis C virus (HCV) NS3 protease inhibitor, with IC50 of 0.2 nM-3.5 nM.

GSK-199 hydrochloride is a potent, highly selective and reversible protein arginine deiminase PAD4 inhibitor with IC50 of 250 nM in FP binding assay (0.2 mM Ca), 200 nM in PAD4 NH3 release inhibition assay; shows high specificity for PAD4 over PAD1/2/3/6; affects cellular citrullination and mimic the deficiency in NET production in mice; significantly decreases in complement C3 deposition in both synovium and cartilage in mice.

CA-074 methyl ester is a specific inhibitor of Cathepsin B, which has potent bioactivities such as neuroprotective, anti-cancer, and anti-inflamatory effects.

GR-127935 potent and selective 5-HT1B/1D receptor antagonist with pKi of 8.5 for both guinea pig 5-HT1D and rat 5-HT1B receptor.

Desmethyl dabrafenib (GSK2167542, Dabrafenib metabolite M8) is the desmethyl- metabolic byproduct of Dabrafenib, ameliorates developmental pathologies of Kabuki Syndrome in vivo.

SR-717 is a non-nucleotide STING agonist with EC50s of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 cGAS KO (cGAS KO) cell lines, respectively. SR-717 is a stable cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic. Antitumor activity[1].

Pitolisant hydrochloride is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM).

Talampanel is a potent and selective AMPA-receptor antagonist, is a potential new antiepileptic drug (AED).

PF-4618433 is a potent and selective PYK2 inhibitor, with an IC50 of 637 nM. PF-4618433 may be suitable for the research of osteoporosis, craniofacial and appendicular skeletal defects and for targeted bone regeneration[1][2].

ML277(CID53347902) is a novel, potent and selective K(v)7.1 (KCNQ1) potassium channel activator with EC50 of 270 nM.ML277 was shown to be highly selective against other KCNQ channels (>100-fold selectivity versus KCNQ2 and KCNQ4) as well as against the distantly related hERG potassium channel.