Ionizable Lipid Products

Pramlintide is a polypeptide analogue of human amylin. Pramlintide, an antidiabetic agent, is antineoplastic in colorectal cancer.

CX-5461 is a potent and oral rRNA synthesis inhibitor. It inhibits RNA polymerase I-driven transcription of rRNA with IC50s of 142, 113, and 54 nM in HCT-116, A375, and MIA PaCa-2 cells, respectively.

Cenupatide is an urokinase plasminogen activator receptor (uPAR) inhibitor for treating disorders associated altered cell migration, such as cancer.

Belvarafenib is a potent and pan RAF (Rapidly Accelerated Fibrosarcoma) inhibitor, with IC50s of 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv600E and C-RAF respectively.

TNO155 is a potent selective and orally active allosteric inhibitor of wild-type SHP2 (IC50=0.011 µM). TNO155 has the potential for the study of RTK-dependent malignancies, especially advanced solid tumors[1].

Eluxadoline is an orally active mixed μ opioid receptor (μOR) agonist δ opioid receptor (δOR) antagonist. in vitro: Eluxadoline is a locally active, mixed ?-opioid receptor (?OR) agonist and δ-opioid receptor (δOR) antagonist being developed for the treatment of IBS-d (diarrhea-predominant irritable bowel syndrome).Eluxadoline, an orally active mixed μ opioid receptor (μOR) agonist δ opioid receptor (δOR) antagonist developed for the treatment of diarrhea-predominant irritable bowel syndrome, normalizes gastrointestinal (GI) transit and defecation under conditions of novel environment stress or post-inflammatory altered GI function. in vivo: Coadministration of a single 200 mg dose of eluxadoline with cyclosporine, and probenecid increased eluxadoline systemic exposure [AUC(0-inf) ] by 4.4- and 1.4-fold, respectively, whereas peak exposure (Cmax) increased 6.2-fold and 1.3-fold, respectively. Cyclosporine had little effect on renal clearance (CLren) of eluxadoline whereas probenecid reduced CLren by nearly 50%.

Orteronel (racemic) is a mixture of S-Orteronel and R-Orteronel isomers. Orteronel, aslo known as TAK-700, is an orally bioavailable non-steroidal androgen synthesis inhibitor of steroid 17alpha-monooxygenase (17,20 lyase) with potential antiandrogen activity. TAK-700 binds to and inhibits the steroid 17alpha-monooxygenase in both the testes and adrenal glands, thereby inhibiting androgen production. This may decrease androgen-dependent growth signaling and may inhibit cell proliferation of androgen-dependent tumor cells.

PF-05221304 is an orally bioavailable, liver-directed and dual ACC1 (and ACC2) inhibitor with IC50s of 7.5 nM for rat ACC1, 8.2 nM for rat ACC2, 12.4 nM for human ACC1 and 8.7 nM for human ACC2. PF-05221304 is a substrate for organic anion transport polypeptides. PF-05221304 directly improves a variety of non-alcoholic fatty liver (NAFL) and non-alcoholic steatohepatitis (NASH) pathogenic factors.

MK-0557 is a highly selective, orally available neuropeptide Y5 receptor antagonist with a Ki of 1.6 nM.

GSK481 can inhibit RIP1 WT S166 phosphorylation in human vs mouse plasmids overexpressed in HEK293T cellsGSK'481 have approximately equivalent RIP1 FP potencies against human andcynomolgus monkey RIP1 but was >100-fold less potent against nonprimate RIP1

Butoconazole nitrate is an anti-fungal agent.Target: Antifungalbutoconazole 1-BSR is an effective and safe alternative to longer-term therapy with miconazole nitrate (seven days) for vulvovaginal candidiasis [1]. A sustained-release (SR) bioadhesive vaginal cream (2% butoconazole nitrate) has incorporated VagiSite technology, a topical drug delivery system that allows SR of the drug [2].

Tioconazole is an antifungal medication of the imidazole class used to treat infections caused by a fungus or yeast. It is marketed under the brand names Trosyd and Gyno-Trosyd (Pfizer). Tioconazole ointments serve to treat women's vaginal yeast infections. Tioconazole topical (skin) preparations are also available for ringworm, jock itch, athlete's foot, and tinea versicolor or "sun fungus".

Pracinostat is a potent histone deacetylase (HDAC) inhibitor, with IC50s of 40-140 nM, used for cancer research.

NSC23005 sodium is a novel and effective p18 inhibitor (ED50=5.21 nM) in promoting Hematopoietic stem cells (HSCs) expansion in both murine and human models.

O-304 is a small molecule AMPK activator.

AP1867 is a synthetic FKBP12F36V-directed ligand.

PrNMI is a peripherally restricted cannabinoid 1 receptor (CB1R) agonist, significantly alleviates spontaneous pain behaviors in the animals.

Hydroxy Dynasore (Dyngo-4a), a structural analog of Dynasore (HY-15304), is an potency improved, low cytotoxicity and non‐specific binding dynamin inhibitor with IC50 values of 0.38 μM and 2.3 μM for brain dynamin I and recombinant rat dynamin II, respectively. Hydroxy Dynasore inhibits dynamin‐dependent endocytosis of transferrin with an IC50 of 5.7 μM in vitro.

UNC 669 is a potent antagonist of L3MBTL1(IC50=4.2 uM) and L3MBTL3(IC50=3.1 uM).IC50 value: 4.2 uM/3.1 uM (L3MBTL1/L3MBTL3) [1]Target: L3MBTL1/L3MBTL3

DC661 is a potent palmitoyl-protein thioesterase 1 (PPT1) inhibitor, inhibits autophagy, and acts as an anti-lysosomal agent. Anti-cancer activity[1].