LPL Receptor Inhibitor

Poloxamer 407 (F127) is a nonionic surfactant that is 100% active and relatively non-toxic to cells at low concentrations, and frequently used with dye AM esters such as Indo-1 AM, Fura-2 AM, Calcein AM, Fluo-3 AM, Fluo-4 AM, Quest Fluo-8 AM and Quest Rhod-4 AM, etc. to improve their water solubility. Poloxamer 407 is also a lipoprotein lipase inhibitor.

Obicetrapib (TA-8995; DEZ-001) potassium is an orally active cholesteryl ester transfer protein (CETP) inhibitor. Obicetrapib potassium potently reduces atherogenic lipoproteins (such as LDL-C, ApoB, Lp (a)) and increases HDL-C. Obicetrapib potassium can be used for the research of dyslipidemia and atherosclerotic cardiovascular disease (ASCVD).

SLB1122168 free base is a Spinster Homolog 2 (Spns2) inhibitor. SLB1122168 free base inhibits Spns2-mediated sphingosine-1-phosphate (S1P) release with an IC₅₀ of 94 nM. SLB1122168 free base induces lymphopenia in circulating lymphocytes in mice and rats.

AM095 (free acid) is a potent LPA1 receptor antagonist with IC₅₀ values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 respectively.

Ceranib-2 is a potent and nonlipid ceramidase inhibitor that inhibits cellular ceramidase activity with an IC₅₀ of 28 μM in SKOV3 cells. Ceranib-2 induces the accumulation of multiple ceramide species, decreases levels of sphingosine and sphingosine-1-phosphate (S1P), and induces cell apoptosis. Anticancer activity.

SLF1081851 is a Spns2 inhibitor, inhibits S1P release (IC₅₀=1.93 μM). SLF1081851 plays a key role in development and immune system.

BMS-986020 (AM152) sodium is a high-affinity lysophosphatidic acid receptor 1 (LPA1) antagonist. BMS-986020 sodium inhibits bile acid and phospholipid transporters with IC₅₀s of 4.8 μM, 6.2 μM, and 7.5 μM for BSEP, MRP4, and MDR3, respectively. BMS-986020 sodium has the potential for the treatment of idiopathic pulmonary fibrosis (IPF).

LPA2 antagonist 1 is a LPA2 antagonist with an IC₅₀ of 17 nM.

SLF80821178 is a potent and orally active inhibitor of Sphingosine-1-Phosphate Transporter (Spns2). SLF80821178 inhibits S1P release with an IC₅₀ of 51 nM in HeLa cells and a T_1/2 of 2.4 h in mouse.

2-Acetyl-5-tetrahydroxybutyl imidazole is a potent sphingosine-1-phosphate (S1P) lyase inhibitor in vivo.

S1PR1 modulator 1 is a selective S1PR1 inhibitor, with a pIC₅₀ of 7.6, with >40- and >80-fold selectivity, over the other S1PR isoforms S1PR2/3/4.

LX2931 is an inhibitor of Sphingosine 1-Phosphate Lyase (S1PL). LX2931 works by increasing levels of S1P inside and outside the cell. The decrease in S1PL activity leads to a significant increase in S1P content in tissues, especially in lymphoid tissues which may lead to a restricted exodus of lymphocytes from secondary immune tissues, resulting in lymphocytopenic and immunosuppressive effects in the peripheral circulation. LX2931 can be used in research for the study of autoimmune diseases, especially rheumatoid arthritis.

Sonepcizumab (LT 1009) is a fully human anti-S1P monoclonal antibody. Sonepcizumab has the potential for the research of metastatic renal cell carcinoma (mRCC).

SLB1122168 formic is a Spinster Homolog 2 (Spns2) inhibitor. SLB1122168 formic inhibits Spns2-mediated sphingosine-1-phosphate (S1P) release with an IC₅₀ of 94 nM. SLB1122168 formic induces lymphopenia in circulating lymphocytes in mice and rats.

SACLAC, a Ceramide analog, is a potent and covalent acid ceramidase (ASAH1; AC) inhibitor with a K_i of 97.1 nM. SACLAC effectively blocks AC activity and induces a decrease in sphingosine 1-phosphate (S1P) and total ceramide levels. SACLAC reduces the levels of splicing factor SF3B1 and alternative Mcl-1 mRNA splicing, increases pro-apoptotic Mcl-1S levels to induce apoptosis in acute myeloid leukemia (AML) cells. SACLAC reduces the leukemic burden in human AML xenograft mouse models.

A6770 is an orally active, potent sphingosine 1-phosphate (S1P) lyase (S1PL) inhibitor. A6770 is phosphorylated and the phosphorylated form directly inhibits S1P lyased.A6770, a potential key metabolite of THI, induces a [³H]dhS1P increase.

S1PR2 Human Pre-designed siRNA Set A contains three designed siRNAs for S1PR2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

S1PR1 Human Pre-designed siRNA Set A contains three designed siRNAs for S1PR1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

S1PL-IN-31 (compound ) is an oral active sphingosine-1-phosphate (S1P) lyase inhibitor with the IC₅₀ of 210 nM. S1PL-IN-31 is Smoothened receptor antagonist with the IC₅₀ of 440 nM. S1PL-IN-31 can be used for study of experimental autoimmune encephalomyelitis.

SLB1122168 is a Spinster Homolog 2 (Spns2) inhibitor. SLB1122168 inhibits Spns2-mediated sphingosine-1-phosphate (S1P) release with an IC₅₀ of 94 nM. SLB1122168 induces lymphopenia in circulating lymphocytes in mice and rats.