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X15695 is selective and orally active estrogen receptor (ERα) degrader. X15695 is an aryl hydrocarbon receptor (AHR) ligand. X15695 enables AHR to form a complex with the ERα, promoting its proteasomal degradation. X15695 inhibits the breast cancer cells proliferation, promotes cell cycle block and induces apoptosis. X15695 can be used for the study of breast cancer .
NF449 octasodium is a highly potent P2X1receptor antagonist, with IC50s of 0.28, 0.69, and 120 nM for rP2X1,rP2X1+5,P2X2+3, respectively. NF449 octasodium is a Gsα-selective G Protein antagonist. NF449 octasodium suppresses the rate of GTP[γS] binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks the coupling of β-adrenergic receptors to Gs .
Tauro-α-muricholic acid (T-α-MCA) sodium is a FXR (Farnesoid Xreceptor) antagonist (IC50=28μM). Tauro-α-muricholic acid sodium is also a endogenous metabolite that can be found in cecal .
Iristectorigenin B (Iristectrigenin B) is a liver Xreceptor (LXR) modulator. Iristectrigenin B stimulates the transcriptional activity of both LXR-α and LXR-β .
α,β-Methylene-ATP trisodium is an agonist of P2X1 and P2X3receptors and can cross the blood-brain barrier. α,β-Methylene-ATP trisodium can trigger a reflex pressor response by activating P2Xreceptors in peripheral muscles and the central locus coeruleus (LC); this effect can be blocked by the P2X antagonist PPADS (HY-108960). α,β-Methylene-ATP trisodium also activates noradrenergic neurons in the central locus coeruleus, mediating antinociceptive effects; this effect can be attenuated by the locus coeruleus damaging agent DSP-4 (HY-103210/HY-121602). α,β-Methylene-ATP trisodium can be used to study the pathological mechanisms of neuropathic pain, cardiovascular reflex regulation, and antinociceptive effects of the central nervous system .
NF449 is a highly potent P2X1receptor antagonist, with IC50s of 0.28, 0.69, and 120 nM for rP2X1,rP2X1+5,P2X2+3, respectively. NF449 is a Gsα-selective G Protein antagonist. NF449 suppresses the rate of GTP[γS] binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks the coupling of β-adrenergic receptors to Gs .
Adimolol (free base) (MEN 935 (free base)) is an antagonist of β- and α-adrenolytic receptor. Adimolol (free base) shows Kis of 5.2 x 10 -7, 1.3 x 10 -5 mol/L at α1 and α2 drenoceptors, respectively. Adimolol (free base) can be used for antihypertensive study .
α,β-Methylene-ATP is an agonist of P2X1 and P2X3receptors and can cross the blood-brain barrier. α,β-Methylene-ATP can trigger a reflex pressor response by activating P2Xreceptors in peripheral muscles and the central locus coeruleus (LC); this effect can be blocked by the P2X antagonist PPADS (HY-108960). α,β-Methylene-ATP also activates noradrenergic neurons in the central locus coeruleus, mediating antinociceptive effects; this effect can be attenuated by the locus coeruleus damaging agent DSP-4 (HY-103210/HY-121602). α,β-Methylene-ATP can be used to study the pathological mechanisms of neuropathic pain, cardiovascular reflex regulation, and antinociceptive effects of the central nervous system .
α,β-Methylene-ATP dilithium is an agonist of P2X1 and P2X3receptors and can cross the blood-brain barrier. α,β-Methylene-ATP dilithium can trigger a reflex pressor response by activating P2Xreceptors in peripheral muscles and the central locus coeruleus (LC); this effect can be blocked by the P2X antagonist PPADS (HY-108960). α,β-Methylene-ATP dilithium also activates noradrenergic neurons in the central locus coeruleus, mediating antinociceptive effects; this effect can be attenuated by the locus coeruleus damaging agent DSP-4 (HY-103210/HY-121602). α,β-Methylene-ATP dilithium can be used to study the pathological mechanisms of neuropathic pain, cardiovascular reflex regulation, and antinociceptive effects of the central nervous system .
TFCA is a liver Xreceptorα (LXRα) antagonist. TFCA inhibits ligand-activated LXRα coactivation and transcriptional expression of the downstream target genes involved in fatty acid synthesis. TFCA attenuates ligand-induced lipogenesis and fatty liver by selectively inhibiting LXRα in the liver .
Fluorobexarotene (compound 20) is a potent retinoid-X-receptor (RXR) agonist, with a Ki value of 12 nM and an EC50 value of 43 nM for RXRαreceptor. Fluorobexarotene possesses an apparent RXR binding affinity that is 75% greater than Bexarotene .
Tauro-α-muricholic acid-d4-1 (sodium) is deuterium labeled Tauro-α-muricholic acid (sodium). Tauro-α-muricholic acid (T-α-MCA) sodium is a FXR (Farnesoid Xreceptor) antagonist (IC50=28μM). Tauro-α-muricholic acid sodium is also a endogenous metabolite that can be found in cecal .
Tauro-alpha-muricholic acid (T-alpha-MCA) is a bile acid that belongs to a class of compounds that are synthesized in the liver and play an important role in the digestive process. Tauro-α-muricholic acid activates Farni Xreceptors (FXR) which are involved in the regulation of bile acid synthesis, metabolism and transport. Tauro-alpha-muricholic acid can be used in the study of metabolic syndrome and cardiovascular disease .
Benzophenone-2 (2,2',4,4'-Tetrahydroxybenzophenone) is an endocrine disruptor targeting pregnane Xreceptor (PXR) and estrogen receptorα (ERα). Benzophenone-2 regulates cytochrome P450 3A (CYP3A) expression by activating PXR. Benzophenone-2 is promising for research of UV filters .
UVI 3003 is a highly selective antagonist of retinoid Xreceptor (RXR), and inhibits xenopus and human RXRα in Cos7 cells, with IC50s of 0.22 and 0.24 μM, respectively.
LG-100064 is a retinoid-X-receptor (RXR) agonist, with EC50s of 330 nM, 200 nM, and 260 nM for RXRα, RXRβ and RXRγ; LG-100064 can be used in the research of cancer.
Ferolin is the agonist for farnesoid Xreceptor (FXR) with an EC50 of 0.56 µM. Ferolin inhibits the expression of inflammatory genes (such as iNOS, IL-1β and TNFα) upon the FXR activation .
LXR (Liver Xreceptor) agonist 1 is potent LXR agonist with AC50s of 1.5 nM and 12 nM for LXR-α and LXR-β, respectively. LXR agonist 1 has the potential for the research of atherosclerosis .
Human CXCL12 mRNA encodes the human C-X-C motif chemokine ligand 12 (CXCL12) protein, a stromal cell-derived alpha chemokine member of the intercrine family. CXCL12 functions as the ligand for the G-protein coupled receptor, chemokine (C-X-C motif) receptor 4, and plays a role in many diverse cellular functions, including embryogenesis, immune surveillance, inflammation response, tissue homeostasis, and tumor growth and metastasis.
MS437 is a potent TSH receptor (TSHR) stimulator with an EC50 value of 13x10 -8 M. MS437 shows potent activation of Gsα, Gαq and Gα12 and up-regulation of thyroglobulin (Tg), sodium iodine symporter (NIS) and TSHR gene expressions .
Bigelovin, a sesquiterpene lactone isolated from Inula hupehensis, is a selective retinoid Xreceptorα agonist. Bigelovin suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation .
SR9238 (Standard) is the analytical standard of SR9238. This product is intended for research and analytical applications. SR9238 is a synthetic liver Xreceptor (LXR) inverse agonist with IC50s of 214 nM and 43 nM for LXRα and LXRβ, respectively.
25-Hydroxytachysterol3 is the metabolite of Vitamin D3 (HY-15398). 25-Hydroxytachysterol3 inhibits the proliferation of epidermal keratinocytes and dermal fibroblasts, stimulates the expression of differentiation- and antioxidant-related genes in keratinocytes. 25-Hydroxytachysterol3 activates vitamin D receptor (VDR) and aryl hydrocarbon receptor (AhR), liver Xreceptorα/β (LXR α/β) and peroxisome proliferator-activated receptor γ (PPARγ), stimulates the expression of CYP24A1 .
GW3965 (hydrochloride) (Standard) is the analytical standard of GW3965 (hydrochloride). This product is intended for research and analytical applications. GW3965 hydrochloride is a potent and selective liver Xreceptor (LXR) agonist with EC50s of 190 nM and 30 nM for hLXRα and hLXRβ, respectively .
16-Dehydropregnenolone acetate (16-DPA), a sterols compound, is an orally active 17α-hydroxylase and 5α-reductase inhibitor. 16-Dehydropregnenolone is also a potent bile acid receptor (BAR)/farnesoid Xreceptor (FXR) antagonist. 16-Dehydropregnenolone hypolipidemic and anticancer effects. 16-Dehydropregnenolone acetate (16-DPA) is the drug intermediate that can be used for synthesis of Dexamethasone (HY-14648) and related other steroidal pharmacophores .
LXRβ agonist-2 is a highly potent and β-selective liver Xreceptor(LXRβ) agonist with EC50 of 7 nM, displays 28.5-fold selectivity over LXRα (EC50=200 nM) and used in the treatment of atherosclerosis .
16α-Hydroxy-11-keto prednisolone (compound M-X) is a metabolite of Budesonide (HY-13580). Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist. Budesonide is a widely used for study of asthma, rhinitis, and inflammatory bowel disease .
PFM046 is the antagonist for liver Xreceptor (LXR), that inhibits the activation of LXRα and LXRβ with IC50 of 2.04 μM and 1.58 μM. PFM046 inhibits the expression of SCD1 and FASN, upregulates the expression of ABCA1, and exhibits antitumor efficacy in mouse models .
7α,24(S)-Dihydroxycholesterol ((3β,7α,24S)-Cholest-5-ene-3,7,24-triol) serves as a ligand for liver Xreceptor (LXR), binding specifically to the ligand binding domains of both LXRα and LXRβ. This compound is synthetically produced from E-α,β-enone, utilizing Arsonium ylide and J-tert-butyldimethylsilyloxy-bisnor-5-cholenaldehyde as starting materials, followed by a series of transformations to yield 7α,24(S)-dihydroxycholesterol.
Bexarotene (LGD1069) is a high-affinity and selective retinoid Xreceptors (RXR) agonist with EC50s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC50 >10000 nM) . Bexarotene can be used for the research of cutaneous T-cell lymphoma.
KRH-3955 is a CXCR4 antagonist with good bioavailability and potent anti-HIV-1 activity. KRH-3955 can effectively inhibit the replication of X4 HIV-1, including clinical isolates from different donors. KRH-3955 also shows activity against recombinant X4 HIV-1 containing reverse transcriptase, protease and tyrosinase resistance mutations. KRH-3955 can inhibit the binding of SDF-1alpha to CXCR4 and calcium ion signaling through this receptor. KRH-3955 inhibits the binding of an antibody against CXCR4 to CXCR4, showing a potent antagonistic effect on CXCR4. KRH-3955 shows an oral bioavailability of 25.6% in rats and can inhibit the replication of X4 HIV-1 in vivo .
Bexarotene- 13C6 (LGD1069- 13C6) is 13C labeled Bexarotene. Bexarotene (LGD1069) is a high-affinity and selective retinoid Xreceptors (RXR) agonist with EC50s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC50 >10000 nM) . Bexarotene can be used for the research of cutaneous T-cell lymphoma.
Bexarotene (Standard) is the analytical standard of Bexarotene. This product is intended for research and analytical applications. Bexarotene (LGD1069) is a high-affinity and selective retinoid Xreceptors (RXR) agonist with EC50s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC50 >10000 nM) . Bexarotene can be used for the research of cutaneous T-cell lymphoma.
MHY 553 is a PPARα agonist that is effective when taken orally. MHY 553 helps alleviate liver fat accumulation by increasing fatty acid oxidation and reducing inflammation during the aging process. MHY 553 inhibits the accumulation of triglycerides induced by liver Xreceptor agonists in HepG2 cells. MHY 553 significantly suppresses the expression of inflammatory mRNA in aging rats .
7α-Hydroxy-4-cholesten-3-one is an intermediate in synthesis of bile acids from cholesterol. 7α-Hydroxy-4-cholesten-3-one is a pregnane Xreceptor (PXR) agonist. 7α-Hydroxy-cholest-4-en-3-one is a biomarker for bile acid loss, irritable bowel syndrome, and other diseases associated with defective bile acid biosynthesis. 7α-Hydroxy-cholest-4-en-3-one is the physiological substrate for CYP8B1 .
Bexarotene- 13C4 (LGD1069- 13C4) is the 13C-labeled Bexarotene (HY-14171). Bexarotene (LGD1069) is a high-affinity and selective retinoid Xreceptors (RXR) agonist with EC50s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC50 >10000 nM) . Bexarotene can be used for the research of cutaneous T-cell lymphoma.
E1231 is an orally active activator of Sirtuin 1 (SIRT1) (EC50=0.83 μM), to modulate cholesterol and lipid metabolism. E1231 interactes with SIRT1 (KD=9.61 μM) and deacetylated liver Xreceptor-alpha (LXRα), and increases ATP-binding cassette transporter A1 (ABCA1) expression. E1231 also reduces atherosclerotic plaque development in ApoE -/- mice model. E1231 can be used for research in cholesterol and lipid disorder-related diseases .
LG100268 (LG268) is a potent, selective and orally active retinoid Xreceptor (RXR) agonist with EC50 values of 4 nM, 3 nM, and 4 nM for RXR-α, RXR-β, and RXR-γ, respectively . LG100268 displays >1000-fold selectivity for RXR over RAR, the Ki values are 3.4 nM, 6.2 nM and 9.2 nM for RXR-α, RXR-β, and RXR-γ, respectively . LG100268 activates RXR homodimers to induce transcriptional activation. LG100268 can be used for the study of lung carcinogenesisy .
Ercalcitriol (1α,25-Dihydroxy Vitamin D2) is a vitamin D receptor (VDR) agonist with high binding affinity. After binding to VDR, Ercalcitriol forms a complex with retinoid Xreceptor (RXR) to regulate target gene transcription. For example, Ercalcitriol induces human gingival/oral epithelial cells to produce human cat antimicrobial peptide (hCAP-18/LL-37), which has antimicrobial activity against periodontal pathogens such as Porphyromonas gingivalis. Ercalcitriol enhances the innate immune defense of the oral mucosa by promoting the expression of antimicrobial peptides, and is mainly used in the study of periodontal diseases and immune-related oral diseases .
Mono (2-ethyl-5-hydroxyhexyl) terephthalate (MEHHTP), a hydroxyl metabolite of the phthalate alternative Di-2-ethylhexyl terephthalate (DEHTP), is a liver Xreceptorα (LXRα) agonist with a binding energy of -7.41 kcal/mol. Mono (2-ethyl-5-hydroxyhexyl) terephthalate upregulates LXRα downstream targets such as SREBP-1c and FASN and increases lipogenic enzyme activity in hepatocytes, and elevating triglyceride (TG) levels. Mono (2-ethyl-5-hydroxyhexyl) terephthalate is promising for research of nonalcoholic fatty liver disease (NAFLD) .
3,7,11,15-Tetramethyl-2-hexadecen-1-ol can be used to synthesize vitamin E and vitamin E's precursor vitamin K1. 3,7,11,15-Tetramethyl-2-hexadecen-1-ol regulates transcription in cells through the transcription factor PPAR-alpha and the retinoid Xreceptor (RXR)43 .
Mifobate (SR-202) is a potent and specific PPARγ antagonist. Mifobate (SR-202) selectively inhibits Thiazolidinedione (TZD)-induced PPARγ transcriptional activity (IC50=140 μM). Mifobate (SR-202) does not affect basal or ligand-stimulated transcriptional activity of PPARα, PPARβ, or the farnesoid Xreceptor (FXR). Mifobate (SR-202) shows antiobesity and antidiabetic effects .
7α-Hydroxy-4-cholesten-3-one-d7 is the deuterium labeled 7α-Hydroxy-4-cholesten-3-one. 7α-Hydroxy-4-cholesten-3-one is an intermediate in synthesis of bile acids from cholesterol. 7α-Hydroxy-4-cholesten-3-one is a pregnane Xreceptor (PXR) agonist. 7α-Hydroxy-cholest-4-en-3-one is a biomarker for bile acid loss, irritable bowel syndrome, and other diseases associated with defective bile acid biosynthesis. 7α-Hydroxy-cholest-4-en-3-one is the physiological substrate for CYP8B1 .
9(R)-HODE is a monohydroxy fatty acid and metabolite of linoleic acid. It is formed from linoleic acid by COX and lipoxygenase (LO).9(R)-HODE induces chemotaxis, increases the levels of chemokine (C-C motif) receptor 9 (CCR9) and chemokine (C-X-C motif) receptor 4 (CXCR4), and inhibits IL-6 release in primary human monocytes. It inhibits CD3α- and CD28-induced proliferation of isolated human peripheral blood lymphocytes when used at a concentration of 25 μg/mL.
7α-Hydroxy-4-cholesten-3-one (Standard) is the analytical standard of 7α-Hydroxy-4-cholesten-3-one. This product is intended for research and analytical applications. 7α-Hydroxy-4-cholesten-3-one is an intermediate in synthesis of bile acids from cholesterol. 7α-Hydroxy-4-cholesten-3-one is a pregnane Xreceptor (PXR) agonist. 7α-Hydroxy-cholest-4-en-3-one is a biomarker for bile acid loss, irritable bowel syndrome, and other diseases associated with defective bile acid biosynthesis. 7α-Hydroxy-cholest-4-en-3-one is the physiological substrate for CYP8B1 .
LG100268 (Standard) is the analytical standard of LG100268. This product is intended for research and analytical applications. LG100268 (LG268) is a potent, selective and orally active retinoid Xreceptor (RXR) agonist with EC50 values of 4 nM, 3 nM, and 4 nM for RXR-α, RXR-β, and RXR-γ, respectively . LG100268 displays >1000-fold selectivity for RXR over RAR, the Ki values are 3.4 nM, 6.2 nM and 9.2 nM for RXR-α, RXR-β, and RXR-γ, respectively . LG100268 activates RXR homodimers to induce transcriptional activation. LG100268 can be used for the study of lung carcinogenesisy .
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) .
Mifobate (Standard) is the analytical standard of Mifobate. This product is intended for research and analytical applications. Mifobate (SR-202) is a potent and specific PPARγ antagonist. Mifobate (SR-202) selectively inhibits Thiazolidinedione (TZD)-induced PPARγ transcriptional activity (IC50=140 μM). Mifobate (SR-202) does not affect basal or ligand-stimulated transcriptional activity of PPARα, PPARβ, or the farnesoid Xreceptor (FXR). Mifobate (SR-202) shows antiobesity and antidiabetic effects .
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) .
Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import . Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19 .
Kaempferol-7-O-rhamnoside is a PD-1/PD-L1 inhibitor and farnesoid Xreceptor (FXR) agonist. Kaempferol-7-O-rhamnoside demonstrates cardioprotective potential targeting the AMPKα1 signaling pathway. Kaempferol-7-O-rhamnoside significantly upregulates the mRNA expression of AMPKα1 in H9c2 cardiomyocytes. Kaempferol-7-O-rhamnoside reverses APAP-induced reduction of glutathione (GSH) content and increase of ROS production in L02 cells. Kaempferol-7-O-rhamnoside has the potential for heart failure .
AZ876 is a selective, orally active agonist of liver Xreceptor (LXRα/β) (Ki=0.007 μM [LXRα, human], 0.011 μM [LXRβ, human]. AZ876 induces the expression of target genes such as ABCA1 and ABCG1, promotes reverse cholesterol transport (RCT) and regulates lipid metabolism and anti-inflammatory effects. AZ876 increases cardiac polyunsaturated fatty acid levels, reduces myocardial fibrosis, and reduces lesion area and monocyte adhesion in atherosclerosis models. AZ876 can be used in cardiovascular disease research, such as preventing and treating β-adrenergic-induced cardiac diastolic dysfunction and inhibiting the progression of atherosclerosis .
AZ876 (Standard) is the analytical standard of AZ876. This product is intended for research and analytical applications. AZ876 is a selective, orally active agonist of liver Xreceptor (LXRα/β) (Ki=0.007 μM [LXRα, human], 0.011 μM [LXRβ, human]. AZ876 induces the expression of target genes such as ABCA1 and ABCG1, promotes reverse cholesterol transport (RCT) and regulates lipid metabolism and anti-inflammatory effects. AZ876 increases cardiac polyunsaturated fatty acid levels, reduces myocardial fibrosis, and reduces lesion area and monocyte adhesion in atherosclerosis models. AZ876 can be used in cardiovascular disease research, such as preventing and treating β-adrenergic-induced cardiac diastolic dysfunction and inhibiting the progression of atherosclerosis .
Alogabat is a positive allosteric modulator (PAM) and agonist (Ki <100 nM) of the GABAAα5 receptor, targeting the α5β3γ2 subunit with a Ki of 8.7 nM. Alogabat increases the expression level of α5β3γ2 in oocytes (1.97-fold). GABAA has been implicated in cognitive impairment associated with central nervous system (CNS) disorders, brain cancer (including brain tumors such as medulloblastoma), and can be used in the study of mild cognitive impairment (MCI), amnestic MCI (aMCI), age-associated memory impairment (AAMI), age-related cognitive decline (ARCD), dementia, Alzheimer's disease (AD), prodromal AD, post-traumatic stress disorder (PTSD), schizophrenia, bipolar disorder, amyotrophic lateral sclerosis (ALS), cognitive impairment associated with cancer treatment, mental retardation, Parkinson's disease (PD), autism spectrum disorder, fragile X, Rett syndrome, obsessive-compulsive behavior, and substance addiction .
Fast green FCF free acid is a dye that is acid-resistant. Fast Green FCF free acid inhibits α-synuclein aggregation, as well as Aβ, P2X4receptor and TLR4/Myd88/NF-κB. Fast Green FCF free acid is widely used as a staining agent like quantitative stain for histones at alkaline pH after acid extraction of DNA, and as a protein stain in electrophoresis. Fast Green FCF free acid improves cognitive impairment, depression, relieves pain allergies, and promotes reproductive function .
Fast Green FCF is a sea green triarylmethane food dye, with absorption maximum ranging from 622 to 626 nm. Fast Green FCF inhibits α-synuclein aggregation, as well as Aβ and P2X4receptor, and TLR4/Myd88/NF-κB. Fast Green FCF is widely used as a staining agent like quantitative stain for histones at alkaline pH after acid extraction of DNA, and as a protein stain in electrophoresis. Fast Green FCF improves cognitive impairment, depression, relieves pain allergies, and promotes reproductive function .
Z-3578 is a small-molecule antagonist targeting MrgX2 (Mas-related G protein-coupled receptorX2) with significant anti-pseudoallergic activity and a KD value of 729 nM. Z-3578 effectively inhibits mast cell degranulation induced by substance P (SP) and C48/80, suppressing the release of β-hexosaminidase with IC50 values of 4.90 µM and 6.18 µM, respectively. It also markedly reduces the release of histamine and TNF-α, along with intracellular calcium flux. In a murine pseudoallergy model, Z-3578 significantly alleviates paw swelling and dye extravasation and lowers serum histamine levels, indicating potent in vivo anti-allergic effects. Z-3578 holds promise as a lead compound for the treatment of allergic diseases, especially pseudoallergic reactions .
Fast Green FCF is a sea green triarylmethane food dye, with absorption maximum ranging from 622 to 626 nm. Fast Green FCF inhibits α-synuclein aggregation, as well as Aβ and P2X4receptor, and TLR4/Myd88/NF-κB. Fast Green FCF is widely used as a staining agent like quantitative stain for histones at alkaline pH after acid extraction of DNA, and as a protein stain in electrophoresis. Fast Green FCF improves cognitive impairment, depression, relieves pain allergies, and promotes reproductive function .
Fast green FCF free acid is a dye that is acid-resistant. Fast Green FCF free acid inhibits α-synuclein aggregation, as well as Aβ, P2X4receptor and TLR4/Myd88/NF-κB. Fast Green FCF free acid is widely used as a staining agent like quantitative stain for histones at alkaline pH after acid extraction of DNA, and as a protein stain in electrophoresis. Fast Green FCF free acid improves cognitive impairment, depression, relieves pain allergies, and promotes reproductive function .
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) .
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) .
Tauro-α-muricholic acid (T-α-MCA) sodium is a FXR (Farnesoid Xreceptor) antagonist (IC50=28μM). Tauro-α-muricholic acid sodium is also a endogenous metabolite that can be found in cecal .
Iristectorigenin B (Iristectrigenin B) is a liver Xreceptor (LXR) modulator. Iristectrigenin B stimulates the transcriptional activity of both LXR-α and LXR-β .
Bigelovin, a sesquiterpene lactone isolated from Inula hupehensis, is a selective retinoid Xreceptorα agonist. Bigelovin suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation .
7α-Hydroxy-4-cholesten-3-one is an intermediate in synthesis of bile acids from cholesterol. 7α-Hydroxy-4-cholesten-3-one is a pregnane Xreceptor (PXR) agonist. 7α-Hydroxy-cholest-4-en-3-one is a biomarker for bile acid loss, irritable bowel syndrome, and other diseases associated with defective bile acid biosynthesis. 7α-Hydroxy-cholest-4-en-3-one is the physiological substrate for CYP8B1 .
Ercalcitriol (1α,25-Dihydroxy Vitamin D2) is a vitamin D receptor (VDR) agonist with high binding affinity. After binding to VDR, Ercalcitriol forms a complex with retinoid Xreceptor (RXR) to regulate target gene transcription. For example, Ercalcitriol induces human gingival/oral epithelial cells to produce human cat antimicrobial peptide (hCAP-18/LL-37), which has antimicrobial activity against periodontal pathogens such as Porphyromonas gingivalis. Ercalcitriol enhances the innate immune defense of the oral mucosa by promoting the expression of antimicrobial peptides, and is mainly used in the study of periodontal diseases and immune-related oral diseases .
3,7,11,15-Tetramethyl-2-hexadecen-1-ol can be used to synthesize vitamin E and vitamin E's precursor vitamin K1. 3,7,11,15-Tetramethyl-2-hexadecen-1-ol regulates transcription in cells through the transcription factor PPAR-alpha and the retinoid Xreceptor (RXR)43 .
Tauro-alpha-muricholic acid (T-alpha-MCA) is a bile acid that belongs to a class of compounds that are synthesized in the liver and play an important role in the digestive process. Tauro-α-muricholic acid activates Farni Xreceptors (FXR) which are involved in the regulation of bile acid synthesis, metabolism and transport. Tauro-alpha-muricholic acid can be used in the study of metabolic syndrome and cardiovascular disease .
Ferolin is the agonist for farnesoid Xreceptor (FXR) with an EC50 of 0.56 µM. Ferolin inhibits the expression of inflammatory genes (such as iNOS, IL-1β and TNFα) upon the FXR activation .
7α-Hydroxy-4-cholesten-3-one (Standard) is the analytical standard of 7α-Hydroxy-4-cholesten-3-one. This product is intended for research and analytical applications. 7α-Hydroxy-4-cholesten-3-one is an intermediate in synthesis of bile acids from cholesterol. 7α-Hydroxy-4-cholesten-3-one is a pregnane Xreceptor (PXR) agonist. 7α-Hydroxy-cholest-4-en-3-one is a biomarker for bile acid loss, irritable bowel syndrome, and other diseases associated with defective bile acid biosynthesis. 7α-Hydroxy-cholest-4-en-3-one is the physiological substrate for CYP8B1 .
Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import . Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19 .
Kaempferol-7-O-rhamnoside is a PD-1/PD-L1 inhibitor and farnesoid Xreceptor (FXR) agonist. Kaempferol-7-O-rhamnoside demonstrates cardioprotective potential targeting the AMPKα1 signaling pathway. Kaempferol-7-O-rhamnoside significantly upregulates the mRNA expression of AMPKα1 in H9c2 cardiomyocytes. Kaempferol-7-O-rhamnoside reverses APAP-induced reduction of glutathione (GSH) content and increase of ROS production in L02 cells. Kaempferol-7-O-rhamnoside has the potential for heart failure .
LXR-α protein is a nuclear receptor that activates transcription by interacting with RXR. It regulates cholesterol uptake through MYLIP-dependent ubiquitination and is critical for cholesterol homeostasis. LXR-α Protein, Human is the recombinant human-derived LXR-α protein, expressed by E. coli , with tag free.
LXR-α protein is a nuclear receptor that activates transcription by interacting with RXR. It regulates cholesterol uptake through MYLIP-dependent ubiquitination and is critical for cholesterol homeostasis. LXR-α Protein, Human (His) is the recombinant human-derived LXR-α protein, expressed by E. coli , with N-6*His labeled tag.
7α-Hydroxy-4-cholesten-3-one-d7 is the deuterium labeled 7α-Hydroxy-4-cholesten-3-one. 7α-Hydroxy-4-cholesten-3-one is an intermediate in synthesis of bile acids from cholesterol. 7α-Hydroxy-4-cholesten-3-one is a pregnane Xreceptor (PXR) agonist. 7α-Hydroxy-cholest-4-en-3-one is a biomarker for bile acid loss, irritable bowel syndrome, and other diseases associated with defective bile acid biosynthesis. 7α-Hydroxy-cholest-4-en-3-one is the physiological substrate for CYP8B1 .
Tauro-α-muricholic acid-d4-1 (sodium) is deuterium labeled Tauro-α-muricholic acid (sodium). Tauro-α-muricholic acid (T-α-MCA) sodium is a FXR (Farnesoid Xreceptor) antagonist (IC50=28μM). Tauro-α-muricholic acid sodium is also a endogenous metabolite that can be found in cecal .
Bexarotene- 13C6 (LGD1069- 13C6) is 13C labeled Bexarotene. Bexarotene (LGD1069) is a high-affinity and selective retinoid Xreceptors (RXR) agonist with EC50s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC50 >10000 nM) . Bexarotene can be used for the research of cutaneous T-cell lymphoma.
Bexarotene- 13C4 (LGD1069- 13C4) is the 13C-labeled Bexarotene (HY-14171). Bexarotene (LGD1069) is a high-affinity and selective retinoid Xreceptors (RXR) agonist with EC50s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC50 >10000 nM) . Bexarotene can be used for the research of cutaneous T-cell lymphoma.
Human CXCL12 mRNA encodes the human C-X-C motif chemokine ligand 12 (CXCL12) protein, a stromal cell-derived alpha chemokine member of the intercrine family. CXCL12 functions as the ligand for the G-protein coupled receptor, chemokine (C-X-C motif) receptor 4, and plays a role in many diverse cellular functions, including embryogenesis, immune surveillance, inflammation response, tissue homeostasis, and tumor growth and metastasis.
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