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PROTAC ERα Degrader-1 comprises an ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Degrader-1 extracts from patent WO2017201449A1, compound P1. PROTAC ERα Degrader-1 is an estrogen receptor-alpha (ERα) degrader.
Ex26 (S1P1-IN-Ex26) is a potent and selective sphingosine 1-phosphate receptor 1(S1P1) antagonist (IC50=0.93 nM). Ex26 shows >3,000-fold selectivity for S1P1 over other Sphingosine 1-phosphate receptors. Ex26 can be used in experimental autoimmune encephalomyelitis reseach .
SAR247799 (S1P1 agonist 3) is an oral activity, selective G-protein-biased sphingosine-1 phosphate receptor-1 (S1P1 ) agonist, with EC50s rang from 12.6 to 493 nM in S1P1-overexpressing cells and HUVECs. SAR247799 can be used for the research of endothelial protection, including type-2 diabetes, metabolic syndrome .
Ozanimod (RPC-1063), a sphingosine 1-phosphate (S1P)receptor modulator that binds with high affinity selectively to S1P receptor subtypes 1 (S1P1) and 5 (S1P5). Ozanimod has modulate effect for hS1P1 and hS1P5receptor with EC50s of 1.03 nM and 8.6 nM, respectively. Ozanimod can be used for the research of relapsing multiple sclerosis (MS) .
Ozanimod (RPC-1063) hydrochloride, a sphingosine 1-phosphate (S1P)receptor modulator that binds with high affinity selectively to S1P receptor subtypes 1 (S1P1) and 5 (S1P5). Ozanimod hydrochloride has modulate effect for hS1P1 and hS1P5receptor with EC50s of 1.03 nM and 8.6 nM, respectively. Ozanimod hydrochloride can be used for the research of relapsing multiple sclerosis (MS) .
P1,P2-Diuridine-5’-diphosphate (Up2U) is a symmetrical dinucleoside polyphosphate containing two pyrimidine base moieties. P1,P2-Diuridine-5’-diphosphate is also an activator of purinergic P2Y receptor .
Amiselimod (MT-1303) is a modulator for sphingosine 1-phosphate receptor (S1P receptor). Amiselimod converses to its active metabolite (S)-amiselimod phosphate by sphingosine kinases (SPHKs), targets S1P1receptor, ameliorates the autoimmune disease without causing bradycardia .
S1p receptor agonist 2 (compound 1) is an agonist of S1P5 receptor, exhibits selectivity over the S1P1 and/or S1P3 receptors. S1p receptor agonist 2 can be used for endogenous SIP signaling system research, and alleviating or preventing CNS disorders research, such as neurodegenerative disorders .
Amiselimod hydrochloride is an orally active novel sphingosine 1-phosphate receptor-1 (S1P1) modulator, designed to reduce the bradycardia effects associated with fingolimod and other S1P receptor modulators. Amiselimod-P shows potent and high selectivity for S1P1 and S1P5 but with minimal agonist activity for S1P4 and no distinct agonist activity for S1P2 or S1P3. Amiselimod hydrochloride is promising for research of autoimmune diseases .
W123, a FTY720 analog, is a competitive sphingosine 1-phosphate type 1 (S1P1) receptor antagonist. W123 is measured by GTPγS activation, MAPK recruitment, cell migration, and ligand-induced receptor internalization .
Ozanimod (Standard) is the analytical standard of Ozanimod. This product is intended for research and analytical applications. Ozanimod (RPC-1063), a sphingosine 1-phosphate (S1P)receptor modulator that binds with high affinity selectively to S1P receptor subtypes 1 (S1P1) and 5 (S1P5). Ozanimod has modulate effect for hS1P1 and hS1P5receptor with EC50s of 1.03 nM and 8.6 nM, respectively. Ozanimod can be used for the research of relapsing multiple sclerosis (MS) .
BMS-960 is a potent and selective S1P1receptor agonist containing isoxazole, which can be used in the research of immune diseases and vascular diseases .
PZ-128 (P1pal-7), a cell-penetrating lipopeptide pepducin, is a first-in-class, specific and reversible protease-activated receptor-1 (PAR1) antagonist. PZ-128 targets the cytoplasmic surface of PAR1 and interrupts signaling to internally-located G (PAR1-G) proteins. PZ-128 has antiplatelet, anti-metastatic, anti-angiogenic and anticancer effects .
Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1)receptor with an IC50 value of 1.88 nM in CHO cells.
BMS-960 free base is a potent and selective S1P1receptor agonist containing isoxazole, which can be used in the research of immune diseases and vascular diseases .
Etrasimod arginine is an orally available S1Preceptor modulator that is a potent full agonist of the S1P1 receptor and has partial agonist activity at S1P4. Etrasimod arginine reduces inflammation in a CD4 +CD45RB high T cell-transferred mouse colitis model .
Cenerimod (ACT-334441) is a potent, selective and orally active S1P1receptor modulator, with an EC50 of 1 nM. Cenerimod shows more than 36 fold selctivity for hS1P1 over hS1P2, hS1P3, hS1P4, and hS1P5 receptor subtypes (EC50s=>10000, 228, 2134, and 36 nM, respectively). Cenerimod can attenuate murine experimental autoimmune encephalomyelitis (EAE) and murine sclerodermatous .
Agaridoxin (GDHB) is a blocker of catecholamine and adrenergic alpha-type receptors isolated from mushrooms. Agaridoxin activates adenylyl cyclase in rat hypothalamic membrane granules in the presence of guanosyl imide diphosphate (Gpp(NH)p) .
Icanbelimod (S1p receptor agonist 1) is a potent and orally active S1P receptor agonist, exhibits an activity of inducing S1P1 internalization (EC50=9.83 nM). Icanbelimod has the potential for the study of arthritis and EAE (experimental autoimmune encephalitis). Icanbelimod is extracted from patent WO2015039587A1, Compound 2.
VPC 23019, an aryl amide-containing Sphingosine 1-phosphate (S1P) analog, is a competitive antagonist at the S1P1 and S1P3 receptors (pKi= 7.86 and 5.93, respectively) and an agonist at the S1P4 and S1P5receptors (pEC50= 6.58 and 7.07, respectively) .
ASP-4058 is a next-generation, selective and oral bioactive agonist for Sphingosine 1-Phosphate receptors 1 and 5 (S1P1 and S1P5), ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile .
ASP-4058 hydrochloride is a next-generation, selective and orally active agonist for Sphingosine 1-Phosphate receptors 1 and 5 (S1P1 and S1P5), ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile .
ACT-209905 is a S1P1receptor agonist. ACT-209905 can inhibit glioblastoma (GBM) cell growth and migration. ACT-209905 also has immunomodulating activity, and can be used in research of autoimmune diseases .
Sphingosine-1-phosphate-d7 is the deuterium labeled Sphingosine-1-phosphate. Sphingosine-1-phosphate (S1P) is an agonist of S1P1-5 receptors and a ligand of GPR3, GPR6 and GPR12. Sphingosine-1-phosphate is an intracellular second messenger and mobilizes Ca2+ as an extracellular ligand for G protein-coupled receptors[1]. Sphingosine-1-phosphate is an important lipid mediator generated from Sphingomyelin (HY-113498) or other membrane phospholipids[2].
CS-0777-P, the phosphorylated form of CS-0777, acts as a potent and selective modulator of the S1P receptor-1 (S1P1). It exhibits approximately 320-fold higher agonist activity for human S1P1 compared to S1P3, with an EC50 of 1.1 nM. In pharmacological studies, CS-0777-P demonstrated significant effects in vitro as an S1P1 and S1P3 agonist, leading to lowered peripheral blood lymphocyte counts and suppressive effects on experimental autoimmune encephalomyelitis (EAE) in rats. Pharmacokinetic studies in rats revealed rapid lymphocyte count reductions following oral administration, making CS-0777 a promising candidate currently undergoing clinical trials for the treatment of multiple sclerosis (MS) .
SEW2871 is an orally active, potent, highly selective S1P1 (sphingosine-1-phosphate type 1 receptor) agonist, with an EC50 of 13.8 nM. SEW2871 activates ERK, Akt, and Rac signaling pathways and induces S1P1 internalization and recycling. SEW2871 reduces lymphocyte numbers in blood. SEW2871 can be used for the research of diabetes, Alzheimer’s disease, liver fibrosis, and inflammatory responses .
Sphingosine-1-phosphate (S1P) is an agonist of S1P1-5receptors and a ligand of GPR3, GPR6 and GPR12. Sphingosine-1-phosphate is an intracellular second messenger and mobilizes Ca 2+ as an extracellular ligand for G protein-coupled receptors . Sphingosine-1-phosphate is an important lipid mediator generated from Sphingomyelin (HY-113498) or other membrane phospholipids .
Siponimod (BAF-312) hemifumarate is a potent and selective sphingosine-1-phosphate (S1P)receptor modulator. Siponimod hemifumarate is selective for S1P1 and S1P5receptors over S1P2, S1P3, and S1P4 (EC50s of 0.39, 0.98, >10000, >1000, and 750 nM, respectively). Siponimod hemifumarate can be used for multiple sclerosis (MS) research .
CYM5442 hydrochloride is a potent, highly-selective and orally active sphingosine 1-phosphate (S1P1) receptor agonist with an EC50 of 1.35 nM. CYM5442 hydrochloride is inactive against S1P2, S1P3, S1P4, and S1P5. CYM5442 hydrochloride activates S1P1-dependent p42/p44-MAPK phosphorylation. CYM5442 exerts retinal neuroprotection. CYM5442 hydrochloride can easily penetrate the central nervous system (CNS) .
CYM5442 is a potent, highly-selective and orally active sphingosine 1-phosphate (S1P1) receptor agonist with an EC50 of 1.35 nM. CYM5442 is inactive against S1P2, S1P3, S1P4, and S1P5. CYM5442 activates S1P1-dependent p42/p44-MAPK phosphorylation. CYM5442 exerts retinal neuroprotection. CYM5442 can easily penetrate the central nervous system (CNS) .
AUY 954 hydrochloride is a potent and selective sphingosine-1-phosphate (S1P(1)) receptor agonist, exhibiting significant immunomodulatory activity. AUY 954 hydrochloride induces a profound and reversible reduction of circulating lymphocytes upon oral administration. AUY 954 hydrochloride has demonstrated efficacy in prolonging cardiac allograft survival when used in combination with RAD001 in a stringent transplantation model. AUY 954 hydrochloride effectively prevents experimental autoimmune neuritis in rats, showcasing its therapeutic potential in autoimmune conditions.
BMS-986104 is a potent and selective S1P1receptor modulator. BMS-986104 is effective in a mouse EAE model, which is comparable to FTY720. Mechanistically, BMS-986104 exhibites excellent remyelinating effects on lysophosphatidylcholine (LPC)-induced demyelination in a three-dimensional brain cell culture assay.
CYM50260 is a potent and exquisitely selective sphingosine-1-phosphate 4 receptor (S1P4-R) agonist with an EC50 of 45 nM. CYM50260 displays no activity against S1P1-R, S1P2-R, S1P3-R and S1P5-R .
GSK2018682 is an agonist for S1P1 and S1P5 receptor with pEC50s of 7.7 and 7.2, respectively, and has no agonist activity towards human S1P2, S1P3, or S1P4. GSK2018682 is used in the research of multiple sclerosis.
GSK2018682 hydrochloride is an agonist for S1P1 and S1P5 receptor with pEC50s of 7.7 and 7.2, respectively, and has no agonist activity towards human S1P2, S1P3, or S1P4. GSK2018682 hydrochloride is used in the research of multiple sclerosis.
L-threo Lysosphingomyelin (d18:1) (L-threo-Sphingosylphosphorylcholine) is an endogenous bioactive sphingolipid. L-threo Lysosphingomyelin (d18:1) is a potent S1P receptor agonist with EC50s of 19.3, 131.8, and 313.3 nM for hS1P1, hS1P3, and hS1P2, respectively .
GSK 1842799 hydrochloride is a selective S1P1receptor agonist with potent agonist activity and exceptional selectivity over S1P3. GSK 1842799 hydrochloride demonstrates good oral bioavailability and rapid conversion to its active phosphorylated form. GSK 1842799 hydrochloride significantly reduces blood lymphocyte counts in vivo following oral administration. GSK 1842799 hydrochloride has shown efficacy comparable to FTY720 in the mouse EAE model of multiple sclerosis.
Siponimod (BAF-312) is an orally active and selective sphingosine-1-phosphate (S1P) receptor modulator. Siponimod is selective for S1P1 and S1P5 over S1P2, S1P3, and S1P4, with EC50s of 0.4, 0.98, >10000, >1000, and 750 nM, respectively. Siponimod can be used for multiple sclerosis (MS) research - .
IMMH001, also called SYL930, is an orally active, potent and selective S1P1 (sphingosine-1-phosphate receptor 1) agonist. IMMH001 decreased levels of both chemokines and proinflammatory cytokines, including IL-1β, IL-5, IL-18, IP10, CCL3, and CCL5. IMMH001 can be used for rheumatoid arthritis (RA) research .
Fingolimod (hydrochloride) (Standard) is the analytical standard of Fingolimod (hydrochloride). This product is intended for research and analytical applications. Fingolimod hydrochloride (FTY720), an analog of sphingosine, is a potent sphingosine 1-phosphate (S1P) receptors modulator. Fingolimod hydrochloride is phosphorylated by sphingosine kinases, particularly by SK2, and then binds S1PR1, 3, 4, and 5. Fingolimod hydrochloride induces the internalization of S1P1, and consequently, inhibits S1P activity. Fingolimod hydrochloride also is a pak1 activator .
CYM50308 (ML248) is a potent, selective and high affinity sphingosine-1-phosphate receptor 4 (S1P4-R) agonist with an EC50 of 56 nM. CYM50308 displays 37-fold more selective for S1P4-R than S1P5-R. CYM50308 has no activity at S1P1-R, S1P2-R and S1P3-R subtypes at concentrations up to 25 μM .
A-971432 is a potent, selective and orally active sphingosine-1-phosphate (S1P) receptor 5 agonist with IC50s of .362, >10, 0.006 µM for S1P1, S1P3, S1P5 respectively. A-971432 protects blood–brain barrier (BBB) homeostasis. A-971432 reverses age-related cognitive decline. A-971432 has the potential for the research of alzheimer’s disease or multiple sclerosis .
Siponimod-d11 is deuterium labeled Siponimod (HY-12355). Siponimod is an orally active and selective sphingosine-1-phosphate (S1P) receptor modulator. Siponimod is selective for S1P1 and S1P5 over S1P2, S1P3, and S1P4, with EC50s of 0.4, 0.98, >10000, >1000, and 750 nM, respectively. Siponimod can be used for multiple sclerosis (MS) research .
Siponimod (Standard) is the analytical standard of Siponimod. This product is intended for research and analytical applications. Siponimod (BAF-312) is an orally active and selective sphingosine-1-phosphate (S1P) receptor modulator. Siponimod is selective for S1P1 and S1P5 over S1P2, S1P3, and S1P4, with EC50s of 0.4, 0.98, >10000, >1000, and 750 nM, respectively. Siponimod can be used for multiple sclerosis (MS) research - .
PZ-128 (P1pal-7), a cell-penetrating lipopeptide pepducin, is a first-in-class, specific and reversible protease-activated receptor-1 (PAR1) antagonist. PZ-128 targets the cytoplasmic surface of PAR1 and interrupts signaling to internally-located G (PAR1-G) proteins. PZ-128 has antiplatelet, anti-metastatic, anti-angiogenic and anticancer effects .
Substance P(1-4) is a potent neurokinin receptors (NK-R) antagonist. Substance P(1-4) has regulation of normal hematopoiesis and inhibits endogenous erythroid colony (EEC) formation .
Sphingosine-1-phosphate (S1P) is an agonist of S1P1-5receptors and a ligand of GPR3, GPR6 and GPR12. Sphingosine-1-phosphate is an intracellular second messenger and mobilizes Ca 2+ as an extracellular ligand for G protein-coupled receptors . Sphingosine-1-phosphate is an important lipid mediator generated from Sphingomyelin (HY-113498) or other membrane phospholipids .
CL-P1/COLEC12 is a multifunctional scavenger receptor that effectively defends against microorganisms and promotes their binding and phagocytosis, covering Gram-positive and Gram-negative bacteria and yeast. In addition, it mediates the recognition, internalization, and degradation of oxidatively modified low-density lipoprotein (oxLDL) by vascular endothelial cells. CL-P1/COLEC12 Protein, Rat (sf9, His) is the recombinant rat-derived CL-P1/COLEC12 protein, expressed by Sf9 insect cells , with N-His labeled tag. The total length of CL-P1/COLEC12 Protein, Rat (sf9, His) is 642 a.a., with molecular weight of ~90 KDa.
Prostaglandin F2 receptor inhibitor (PTGFRN) is a type I transmembrane Ig superfamily cell adhesion molecule. PTGFRN is overexpressed in glioblastoma and promotes cell growth and radiation resistance through the PI3K-AKT signaling pathway. PTGFRN is involved in adipocyte maturation, muscle regeneration, tumor angiogenesis, metastasis, inhibition of follicle-stimulating hormone and luteinizing hormone secretion, and plasmodium infection. FPRP/PTGFRN Protein, Cynomolgus (HEK293, His) is the recombinant cynomolgus-derived FPRP/PTGFRN protein, expressed by HEK293 , with C-His labeled tag. The total length of FPRP/PTGFRN Protein, Cynomolgus (HEK293, His) is 809 a.a., with molecular weight of 96-106 kDa.
The Klrb1a protein is critical for stimulating NK cell cytotoxicity and contributes to immune defense mechanisms.Klrb1a exists as a homodimer with disulfide bonds and complexly regulates NK cell activity.Klrb1a Protein, Mouse (HEK293, His) is the recombinant mouse-derived Klrb1a protein, expressed by HEK293 , with N-His labeled tag.
CD161 protein plays a crucial role in inhibiting NK cell toxicity by activating specific acid sphingomyelinase/SMPD1 and increasing ceramide levels. Activation stimulates AKT1/PKB and RPS6KA1/RSK1 kinases, enhancing anti-CD3-induced T cell proliferation. CD161 Protein, Human (HEK293, Fc) is the recombinant human-derived CD161 protein, expressed by HEK293 , with C-hFc labeled tag. The total length of CD161 Protein, Human (HEK293, Fc) is 159 a.a., with molecular weight of 55-70 kDa.
Collectin-12 is a family of Ca2+-dependent, C-type lectins that contain a collagenous domain and function as recognition molecules for molecular patterns found on pathogens (1 - 4). CL-P1/COLEC12 Protein, Rhesus Macaque (sf9, His) is the recombinant Rhesus Macaque-derived CL-P1/COLEC12 protein, expressed by Sf9 insect cells , with N-His labeled tag. The total length of CL-P1/COLEC12 Protein, Rhesus Macaque (sf9, His) is 642 a.a., with molecular weight of ~72.3 KDa.
FPRP/PTGFRN protein plays a key role in regulating prostaglandin F2-α (PGF2-α) signaling by inhibiting the binding of PGF2-α to its FP receptor. This inhibition reduces receptor number without changing the affinity constant, revealing subtle mechanisms. FPRP/PTGFRN Protein, Human (HEK293, His) is the recombinant human-derived FPRP/PTGFRN protein, expressed by HEK293 , with C-His labeled tag. The total length of FPRP/PTGFRN Protein, Human (HEK293, His) is 807 a.a., with molecular weight of 100-110 kDa.
The FPRP/PTGFRN Protein inhibits PGF2-alpha binding to its FP receptor, mainly by reducing receptor numbers.It interacts with CD9 and CD81, preventing myotube fusion in myoblasts during muscle regeneration.It also forms a complex with CD9, CD81, and IGSF8, potentially interacting with other tetraspanins like CD63, CD82, and CD151.These interactions highlight its regulatory role in prostaglandin signaling and muscle regeneration.FPRP/PTGFRN Protein, Mouse (HEK293, His) is the recombinant mouse-derived FPRP/PTGFRN protein, expressed by HEK293 , with C-His labeled tag.
Sphingosine-1-phosphate-d7 is the deuterium labeled Sphingosine-1-phosphate. Sphingosine-1-phosphate (S1P) is an agonist of S1P1-5 receptors and a ligand of GPR3, GPR6 and GPR12. Sphingosine-1-phosphate is an intracellular second messenger and mobilizes Ca2+ as an extracellular ligand for G protein-coupled receptors[1]. Sphingosine-1-phosphate is an important lipid mediator generated from Sphingomyelin (HY-113498) or other membrane phospholipids[2].
Siponimod-d11 is deuterium labeled Siponimod (HY-12355). Siponimod is an orally active and selective sphingosine-1-phosphate (S1P) receptor modulator. Siponimod is selective for S1P1 and S1P5 over S1P2, S1P3, and S1P4, with EC50s of 0.4, 0.98, >10000, >1000, and 750 nM, respectively. Siponimod can be used for multiple sclerosis (MS) research .
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