Ionizable Lipid Products

Ravidasvir, also known as PPI-668 and ASC16, is a second-generation, orally active, potent and selective HCV NS5A protein inhibitor.

THZ531 is a covalent inhibitor of both CDK12 and CDK13 with IC50s of 158 nM and 69 nM, respectively.

Lazertinib is a potent, highly mutant-selective, blood-brain barrier permeable, orally available and irreversible third-generation EGFR tyrosine kinase inhibitor, and can be used in the research of non-small cell lung cancer.

Raltitrexed is an antimetabolite drug used in chemotherapy, acting by inhibiting thymidylate synthase.

HAMNO is a novel protein interaction inhibitor of replication protein A (RPA).

Fevipiprant(QAW039) is a selective, potent, reversible competitive CRTh2 antagonist with an in vitro dissociation constant KD value of 1.1nM at the CRTh2 receptor and an IC50 value of 0.44 nM for inhibition of PGD2-induced eosinophil shape change in human whole blood.IC50:0.44 nM(PGD2-induced eosinophil shape change)Kd value:1.1nM(CRTh2 receptor)[1]In vitro: CRTh2-mediated shape change in eosinophils was used to profile QAW039 in whole blood and represents a physiologically relevant environment. The comparable IC50 values for QAW039 in the whole blood and isolated shape-change assays are consistent with its lower plasma-protein binding and its relatively slow dissociation kinetics that drive its increased potency .QAW039 is highly potent in whole-blood systems, with the IC50 value obtained consistent with the affinity values calculated from radioligand experiments. In a further disease-relevant cellular context, the potency of QAW039 in the isolated Th2 cell cytokine inhibition assay is consistent with its CRTh2 receptor affinity, and, as with eosinophil assay readouts, this represents an improved potency compared with QAV680[2].

ABT-639 is a novel, peripherally acting, selective T-type Ca2+ channel blocker.

PF-04995274 is a potent, high-affinity, orally active and partial serotonin 4 receptor (5-HT4R) agonist. PF-04995274 has an EC50 range of 0.26-0.47 nM for human 5-HT4A/4B/4D/4E (Ki range of 0.15-0.46 nM), and has an EC50 range of 0.59-0.65 nM for rat 5-HT4S/4L/4E (Ki of 0.30 nM for rat 5-HT4S). PF-04995274 is brain penetrant and can be used to treat for cognitive disorders associated with Alzheimer＇s disease[1][2][3].

RMC-9805 is a first-in-class, mutant-selective, covalent and orally bioavailable KRAS-G12D(ON) inhibitor. RMC-9805 exhibits direct anti-tumor effects and indirectly transformed the TME through inhibition of cancer cell-intrinsic KRAS-G12D oncogenic signaling.

SMAP (DT-061, DT061) is an orally bioavailable small molecule activator of PP2A, inhibits KRAS-driven tumor growth; acts by binding to the PP2A Aα scaffold subunit to drive conformational changes in PP2A; inhibits the growth of KRAS-mutant lung cancers in mouse xenografts and transgenic models.

Ricolinostat (ACY-1215) is a potent and selective HDAC6 inhibitor, with an IC50 of 5 nM. ACY-1215 also inhibits HDAC1, HDAC2, and HDAC3 with IC50s of 58, 48, and 51 nM, respectively.

Xanthine amine congener (XAC) is a non-selective adenosine receptor antagonist with Kb values of 83, 25, and 15 nM for rat PC12 cells, human platelets that endogenously express adenosine A2A receptors, and rat fat cells that endogenously express A1 recept

Losmapimod is a selective, potent, and orally active p38 MAPK inhibitor with pKis of 8.1 and 7.6 for p38α and p38β, respectively.

MMP-3 inhibitor is a peptide inhibitor of matrix metalloproteinase-3 (MMP-3) with a Ki value of 95 nM.

CGP71683 hydrochloride is a competitive neuropeptide Y5 receptor antagonist with a Ki of 1.3 nM, and shows no obvious activity at Y1 receptor (Ki, >4000 nM) and Y2 receptor (Ki, 200 nM) in cell membranes.

Baloxavir marboxil is a prodrug of S-033447. S-033447 is a small molecule inhibitor of the cap-dependent endonuclease of influenza A and B viruses.

UU-T02 is a novel potent, selective small-molecule inhibitor of β-catenin/Tcf4 interaction with Ki of 1.36 uM; displays 63-fold and 175-fold selectivity over β-catenin/E-cadherin and β-catenin/APC interactions, respectively.

Balaglitazone is a selective partial PPARγ agonist with an EC50 of 1.351 μM for human PPARγ.

APD668 is a potent GPR119 agonist with EC50 of 2.7 nM and 33 nM for hGPR119 and ratGPR119 respectively.Chronic treatment withAPD668 showed for the first time that blood glucose and glycated hemoglobin (HbA1c) levels could be significantly reduced in Zucker Diabetic Fatty (ZDF) rats over several weeks of dosing. APD668 was the ?rst compound with thismechanism of action to be progressed into clinical development for the treatment of diabetes.

Bafetinib is a Lyn and Bcr-Abl tyrosine kinase inhibitor with potential antineoplastic activity.