Ionizable Lipid Products

PD0325901 is a selective and cell permeable MEK inhibitor with an IC50 of 0.33 nM.

MLS 0263839 is a potent, specific inhibitor of the phosphatase PHOSPHO1 with IC50 of 0.14 uM, shows minimal cross-inhibition of TNAP and no inhibition of ENPP1 activity; suppresses vascular smooth muscle cell calcification in cimbined with MLS 0038949.

Ribociclib hydrochloride (LEE011 hydrochloride) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.

Pemetrexed disodium is a novel antifolate that inhibits the folatedependent enzymes thymidylate synthase, dihydrofolate reductase, and glycinamide ribonucleotide formyltransferase with Kis of 1.3, 7.2, and 65 nM, respectively.

Losartan (potassium) is an angiotensin II receptor type 1 (AT1) antagonist, competing with the binding of angiotensin II to AT1 with an IC50 of 20 nM.

p38-α MAPK-IN-1 is an inhibitor of MAPK14 (p38-α), with IC50 of 2300 nM in EFC displacement assay, and 5500 nM in HTRF assay.

Sildenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 5.22 nM.

C-178, a covalent inhibitor of STING, binds to Cys91, potently and selectively suppresses the STING responses elicited by distinct bona fide activators in mouse but not human. C-178 significantly reduces STING-, but not RIG-I- or TBK1-, mediated IFN-β reporter activity. C-178 blocks palmitoylation (PMA)-induced clustering of STING; inhibits the CMA-induced phosphorylation of TBK1 (downstream protein kinase of STING)[1].

AC-263093 (AC263093) is a potent, functionally selective neuropeptide FF receptor type 2 (NPFFR2) agonist with pKi of 6.9; shows equal affinity for NPFFR1 and NPFFR2, and functionally inactivated NPFFR1; attenuates morphine tolerance in vivo.

GLS1 inhibitor is an inhibitor of glutaminase 1

Protease-Activated Receptor-2, amide (SLIGKV-NH2) is a highly potent protease-activated receptor-2 (PAR2) activating peptide.

BVT948 is a protein tyrosine phosphatase (PTP) inhibitor which can also inhibit several cytochrome P450 (P450) isoforms and lysine methyltransferase SETD8.

MF-766 (MF766) is a highly potent and selective EP(4) antagonist with binding Ki of 0.23 nM, displays no significant affinity (>7000-fold selectivity) against other PG receptors (IC50>1500 nM); behaved as a full antagonist with an IC50 of 1.4 nM (shifted to 1.8 nM in the presence of 10% HS) in the functional assay; exhibits blockade of inhibition of TNFa-induced IP10 release by the specific EP4 agonist L-000902688 (IC50=9.5 nM); demonstrates potency and efficacy of in the rat AIA model measuring inhibition of paw swelling.

IXA6 is a novel small molecule compound of inducing IRE1 RNase activity.

ML372 is a small molecule SMN modulator that increases SMN protein in patient fibroblasts with EC50 of 37 nM; possesses good potency, pharmacokinetics, tolerance, and CNS penetration that are able to increase levels of SMN protein in several model cell lines; increase SMN protein levels in vivo, restore motor function, and prolong survival of SMNΔ7 SMA Mice; improves the righting reflex and extended survival of a severe mouse model of SMA.

PGN-9856 (PGN9856) is a novel potent, selective prostaglandin EP2 receptor agonist with pKi of > 8.3, shows higi selectivity over EP1 , EP3 , EP4 , DP, FP, IP and TP receptors; displays a potency (pEC50 >8.5) and a maximal response (increase in cAMP) comparable to that of the endogenous agonist PGE2 in cells over-expressing human recombinant EP2 receptors; exhibited tocolytic, anti-inflammatory, and long-acting ocular hypotensive properties consistent with its potent EP2 agonist properties.

IXA4 is the most selective for the IRE1–XBP1s signaling pathway.IXA4 selectively activate IRE1–XBP1s signaling and reduces secretion of APP through IRE1 activation.

A peptidic glucagon like peptide 2 (GLP-2) analogue for treatment of type2 diabetes.

Safinamide mesylate mesylate (FCE 26743 mesylate; EMD 1195686 mesylate) is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 µM)[1]. Safinamide mesylate also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide mesylate has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al[2][3].

ML-T531 is a potent, selective hERG potassium channel (Kv11.1) activator with EC50 of 3.13 uM; exhibits no potentiation for KCNQ1 and KCNE1, and no noticeable effects on other cardiac channels including Cav1.2, Kir2.1, Nav1.5, and Kv4.3; significantly potentiates hERG steady-state currents and tail currents in CHO cells at 10 uM, enhances voltage-dependent potassium current amplitudes in the presence of an Iks-specific inhibitor chromanol 293B; potentiates native potassium currents in iPSC-derived cardiomyocytes, shortens the APD90 of LQT1 cardiomyocytes with EC50 of 5.71 uM, normalizes the disease phenotype of cardiomycytes derived from a patient with LQT1.