TGF-β Receptor Activator

Sitaxsentan sodium (IPI 1040 sodium; TBC11251 sodium) is a potent, selective and orally active endothelin A receptor (ETA) antagonist with an IC₅₀ of 1.4 nM and a K_i of 0.43 nM. Sitaxsentan sodium exhibits an IC₅₀ for the ETB receptor of as high as 9800 nM. Sitaxsentan sodium is metabolized by CYP2C9 and CYP3A4, normalizes shunt-induced endothelial abnormalities, restores BMPR signaling, and suppresses pulmonary vascular remodeling and hemodynamic deterioration. Sitaxsentan sodium can be applied in the research of pulmonary arterial hypertension and portopulmonary hypertension.

SJ000291942 is an activator of the canonical bone morphogenetic proteins (BMP) signaling pathway. BMPs are members of the transforming growth factor beta (TGFβ) family of secreted signaling molecules.

Arecaidine is a GABA transport system inhibitor. Arecaidine inhibits the proliferation of oral mucosal fibroblasts, increases the secretion of IL-6, TGF-β and TNF-α in cells, downregulates the expression of PPAR-γ and PCK1 in cells, and upregulates the expression of TGF-β1. Arecaidine inhibits the uptake of γ-aminobutyric acid and β-alanine by the central nervous system of cats. Arecaidine inhibits hPAT1-mediated L-[³H]proline uptake in cells. Arecaidine can be used in research related to neurological diseases.

Isosaponarin is a flavone glycoside isolated from wasabi leaves. Isosaponarin is a P4HA2 enzymatic agonist. Isosaponarin increases collagen synthesis via up-regulated TGF-β type II receptor (TβR-II) and prolyl 4-hydroxylase (P4H) proteins production, promoting skin health and wound healing. Isosaponarin-rich plants exhibit strong antimicrobial, antioxidant, anti-hyaluronidase, antiplatelet, anti-atopic dermatitis, and anti-tumor effects.

Tiger17 is an effective wound healing agent. Tiger17 is able to induce the secretion of TGF-β1 and acts through the Smad signaling pathway, specifically promoting wound healing by increasing the phosphorylation of Smad2 and Smad3.

AMPK activator 12 (compound 21) is a potent AMPK activator and GDF15 inducer. AMPK activator 12 increases GDF15 protein levels in human hepatic cells.

Chromenone 1 is a potent osteogenic bone morphogenetic protein (BMP) potentiator. Chromenone 1 exhibits a unique mode of action as it induces a pronounced, kinase-independent, negative TGFβ feedback that enhances nuclear BMP-Smad signaling outputs.

Sitaxsentan (IPI 1040 sodium; TBC11251 sodium) is a potent, selective and orally active endothelin A receptor (ETA) antagonist with an IC₅₀ of 1.4 nM and a K_i of 0.43 nM. Sitaxsentan exhibits an IC₅₀ for the ETB receptor of as high as 9800 nM. Sitaxsentan is metabolized by CYP2C9 and CYP3A4, normalizes shunt-induced endothelial abnormalities, restores BMPR signaling, and suppresses pulmonary vascular remodeling and hemodynamic deterioration. Sitaxsentan can be applied in the research of pulmonary arterial hypertension and portopulmonary hypertension.

Endotrophin (Mus musculus) TFA is an adipokine, a cleavage fragment derived from Collagen VI, whose levels are elevated in adipose tissue and breast tumors of obese mice. Endotrophin (Mus musculus) TFA activates the TGF-β signaling pathway and reduces the expression of hormone-sensitive lipase. Endotrophin (Mus musculus) TFA induces adipogenesis, lipid accumulation, fibrosis, inflammation, angiogenesis, adipose tissue expansion, epithelial-mesenchymal transition, and insulin resistance; it also induces Cisplatin (HY-17394) resistance in cancer cells. Endotrophin (Mus musculus) TFA can be used in research related to metabolic diseases such as obesity and type 2 diabetes, as well as cancers such as breast cancer.

Endotrophin (Mus musculus) is an adipokine, a cleavage fragment derived from Collagen VI, whose levels are elevated in adipose tissue and breast tumors of obese mice. Endotrophin (Mus musculus) activates the TGF-β signaling pathway and reduces the expression of hormone-sensitive lipase. Endotrophin (Mus musculus) induces adipogenesis, lipid accumulation, fibrosis, inflammation, angiogenesis, adipose tissue expansion, epithelial-mesenchymal transition, and insulin resistance; it also induces Cisplatin (HY-17394) resistance in cancer cells. Endotrophin (Mus musculus) can be used in research related to metabolic diseases such as obesity and type 2 diabetes, as well as cancers such as breast cancer.

1-Oleoyl lysophosphatidic acid sodium (GMP) is the GMP-grade form of 1-Oleoyl lysophosphatidic acid sodium (HY-107614). GMP-grade small molecules serve as auxiliary reagents in cell therapy. 1-Oleoyl lysophosphatidic acid sodium is a bioactive lipid signaling molecule. 1-Oleoyl lysophosphatidic acid sodium inhibits lysoPLD-catalyzed hydrolysis of lysophosphatidylcholine and FS-3. 1-Oleoyl lysophosphatidic acid sodium activates LPA₁ and LPA₂, thereby triggering calcium mobilization, NFATc1 translocation, Rho/ROCK activation, Smad2/3 phosphorylation and c-Fos expression. 1-Oleoyl lysophosphatidic acid sodium induces anxiety-like, depression-like and hypoactivity phenotypes, regulates osteoclast cytoskeleton and viability, reduces osteoclast bone resorptive activity, and drives mesenchymal stem cell differentiation into myofibroblast-like cells. 1-Oleoyl lysophosphatidic acid sodium stimulates the secretion of transforming growth factor-β1 and stromal cell-derived factor-1. 1-Oleoyl lysophosphatidic acid sodium is applicable to research related to anxiety, depression and ovarian cancer.

Phenamil is a compound that promotes bone repair and regulates stem cell differentiation. It can activate the bone morphogenetic protein signaling pathway to promote bone repair, but it also induces adipogenesis. A specific 3D scaffold strategy can improve its induced osteogenic differentiation and reduce adipogenesis.

YXX0248 is an orally active anti-hypoxic agent. YXX0248 upregulates mRNA expression of FGF21 and GDF15 via activation of the ISR/ATF4 transcriptional axis. YXX0248 exhibits low cytotoxicity. YXX0248 enhances hypoxic survival in mice. YXX0248 can be used for the research of acute mountain sickness and hypoxia-related diseases.

LG190155 is a nonsteroidal vitamin D receptor (VDR) agonist. LG190155 activates VDR in mesenchymal stem cells, thereby upregulating the BMP6-IL6 autocrine axis. Pretreatment of mesenchymal stem cells with LG190155 significantly enhances their ability to induce differentiation of acute myeloid leukemia cells, without inducing hypercalcemia. LG190155 is applicable to research related to acute myeloid leukemia (AML).

YXX0237 is an orally active anti-hypoxic agent. YXX0237 upregulates mRNA expression of FGF21 and GDF15 via activation of the ISR/ATF4 transcriptional axis. YXX0237 exhibits low cytotoxicity. YXX0237 enhances hypoxic survival in mice. YXX0237 can be used for the research of acute mountain sickness and hypoxia-related diseases.

Sitaxsentan-¹³C₆ (IPI 1040-¹³C₆) is ¹³C labeled Sitaxsentan (HY-76520). Sitaxsentan (IPI 1040 sodium; TBC11251 sodium) is a potent, selective and orally active endothelin A receptor (ETA) antagonist with an IC₅₀ of 1.4 nM and a K_i of 0.43 nM. Sitaxsentan exhibits an IC₅₀ for the ETB receptor of as high as 9800 nM. Sitaxsentan is metabolized by CYP2C9 and CYP3A4, normalizes shunt-induced endothelial abnormalities, restores BMPR signaling, and suppresses pulmonary vascular remodeling and hemodynamic deterioration. Sitaxsentan can be applied in the research of pulmonary arterial hypertension and portopulmonary hypertension.

Sitaxsentan (sodium) (Standard) is the analytical standard of Sitaxsentan sodium (IPI 1040 sodium; TBC11251 sodium) (HY-11103). This product is intended for research and analytical applications. Sitaxsentan sodium is a potent, selective and orally active endothelin A receptor (ETA) antagonist with an IC₅₀ of 1.4 nM and a K_i of 0.43 nM. Sitaxsentan sodium exhibits an IC₅₀ for the ETB receptor of as high as 9800 nM. Sitaxsentan sodium is metabolized by CYP2C9 and CYP3A4, normalizes shunt-induced endothelial abnormalities, restores BMPR signaling, and suppresses pulmonary vascular remodeling and hemodynamic deterioration. Sitaxsentan sodium can be applied in the research of pulmonary arterial hypertension and portopulmonary hypertension.

Ldalaptican pegol (AON-D21; NOX-D21) is a PEGylated mixed RNA/DNA L-aptamer that specifically binds to complement C5a. Ldalaptican pegol binds to C5a and the C5a moiety on uncleaved C5, thereby blocking C5a signaling. This inhibition suppresses downstream inflammatory responses, immune cell infiltration and chemotaxis, the release of pro-fibrotic factors, and abnormalities in lipid metabolism signaling pathways. Ldalaptican pegol can also alleviate allograft rejection. Ldalaptican pegol can be used in research on inflammatory muscle diseases, Duchenne muscular dystrophy (DMD), diabetes, renal fibrosis, and allograft organ transplant rejection.