Ionizable Lipid Products

Encorafenib (LGX818) is a highly potent RAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E (EC50=4 nM).

Elamipretide is a cardiolipin peroxidase inhibitor and mitochondria-targeting peptide.

S-2765, which is specific to activated factor X (FXa), is a short peptide covalently bound to pNA (4-nitroaniline). When attacked by FXa, it releases a free pNA which could be detected by a spectrophotometer at 405 nm.S-2765 is mainly used in anti-FXa activity assay of heparin. S-2765 can be used in many applications, such as: 1:Anti-factor Xa activity to anti-factor IIa activity ratios of heparin and LMWHs. 2: Anti-factor Xa activities of heparin and LMWHs. 3: Activities of antithrombin and coagulation factors. 4: Anti-factor Xa activities of heparin and LMWHs in human plasma. 5: Production of kits for automated blood analyzers. 6: Evaluation of potential anticoagulants from chemical synthesis, bacterial fermentation and animal tissues.

ONO-7300243 is a novel, potent lysophosphatidic acid receptor 1 (LPA1) antagonist with IC50 of 0.16 μM.

Mdivi-1 is a selective dynamin-related protein 1 (Drp1) inhibitor.

1-Methoxy PMS is stable electron-transport mediator between NAD(P)H and tetrazolium dyes.1-Methoxy PMS can induce active oxygen formation.

GDC-0810 is an orally bioavailable selective estrogen receptor degrader (SERD) with IC50 of 0.7 nM.

UCPH-101 is an excitatory amino acid transporter subtype 1 (EAAT1) inhibitor with an IC50 of 0.66 μM.

Cyclic-di-GMP is a STING agonist and a ubiquitous second messenger that regulates biofilm formation, motility, and virulence in diverse bacterial species.

The amine-reactive 5-TAMRA, SE and its conjugates yield bright, pH-insensitive orange-red fluorescence (approximate excitation/emission maxima ~546/579) with good photostability.

PF-06835919, also known as MDK1846, is a potent ketohexokinase (KHK) inhibitor. PF-06835919 is reported in patent US 20170183328 A1, example 4. Increased fructose consumption and its subsequent metabolism have been implicated in hepatic steatosis, dyslipidemia, obesity, and insulin resistance in humans. Since ketohexokinase (KHK) is the principal enzyme responsible for fructose metabolism, identification of a selective KHK inhibitor may help to further elucidate the effect of KHK inhibition on these metabolic disorders.

BAY-293 is a potent SOS1 inhibitors that block RAS activation via disruption of the RAS-SOS1 interaction with an IC50 of 21 nM[1].

MK-3903 is a potent and selective AMP-activated protein kinase (AMPK) activator with an EC50 of 8 nM.

AF-353 is a novel, potent and orally bioavailable P2X3/P2X2/3 receptor antagonist, inhibits human and rat P2X3 (pIC50= 8.0).

BMY 7378 is a multi-targeted inhibitor of α2C-adrenoceptor and α1D-adrenoceptor with pKi of 6.54 and 8.2, respectively, and acts as a mixed agonist and antagonist for 5-HT1A receptor with pKi of 8.3.

Peficitinib is an oral JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.

Apilimod is a potent IL-12/IL-23 inhibitor, and strongly inhibits IL-12 with IC50s of 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs and SAC-treated monkey PBMCs, respectively.

GLPG1690 is a first-in-class autotaxin (ATX) inhibitor, with an IC50 of 131 nM and Ki of 15 nM.

Sertindole, a neuroleptic, is one of the newer antipsychotic medications available.In vitro studies showed that sertindole exerts a potent antagonism at serotonin 5-HT2A, 5-HT2C, dopamine D2, and αl adrenergic receptors. Sertindole offers an alternative treatment option for refractory patients given its good EPS profile, favorable metabolic profile, and comparable efficacy to risperidone. Due to cardiovascular safety concerns, sertindole is available as a second-line choice for patients intolerant to other antipsychotic agents [1]. Sertindole should prove to be a very useful addition to the therapeutic options available for the treatment of psychotic disorders [2]. Sertindole improves negative symptoms, and is also effective for the treatment of neuroleptic-resistant schizophrenia. Sertindole is generally well tolerated and is associated with a low rate of extrapyramidal symptoms (EPS). Thus, sertindole is a useful option in the treatment of patients with schizophrenia [3].

GRA Ex-25 is an inhibitor of glucagon receptor, with IC50 of 56 and 55 nM for rat and human glucagon receptors, respectively.