{"product_id":"abcam-ab286948","title":"Abcam, ab286948, S1RA (E-52862)","description":"\u003cp\u003eSize: 1mg \/ 5mg\u003cbr\u003e\nMW 337.4 Da, Purity \u0026gt;98%. A highly selective sigma-1 receptor antagonist. It shows high affinity for sigma 1 receptors with Ki values of 17 nM and 23.5 nM for human and guinea pig sigma 1 receptors respectively but no significant affinity for the sigma 2 receptors with Ki values of 1000 nM and 9300 nM for guinea pig and rat sigma 2 receptors respectively. It shows moderate affinity (Ki = 328 nM) and antagonistic activity with low potency at the human 5-HT2B receptor. S1RA inhibits neuropathic pain in formalin-induced nociception and capsaicin-induced mechanical hypersensitivity in mice. Sigma receptor modulators may show activity against SARS-CoV-2 as sigma receptors interact with SARS-CoV-2 proteins Nsp6 and Orf9c.\u003cbr\u003e\nKey facts\u003cbr\u003e\nCAS number:878141-96-9,\u003cbr\u003e\nPurity:\u0026gt;98%,\u003cbr\u003e\nForm:SolidSee storage information,\u003cbr\u003e\nMolecular weight:337.4 Da,\u003cbr\u003e\nMolecular formula:C20H23N3O2,\u003cbr\u003e\nPubChem:44247568,\u003cbr\u003e\nNature:Synthetic,\u003cbr\u003e\nSolubility:~10 mg\/ml in DMF~1 mg\/ml in ethanol~15 mg\/ml in DMSO,\u003cbr\u003e\nBiochemical name:S1RA,\u003cbr\u003e\nBiological description:A highly selective sigma-1 receptor antagonist. It shows high affinity for sigma 1 receptors with Ki values of 17 nM and 23.5 nM for human and guinea pig sigma 1 receptors respectively but no significant affinity for the sigma 2 receptors with Ki values of 1000 nM and 9300 nM for guinea pig and rat sigma 2 receptors respectively. It shows moderate affinity (Ki = 328 nM) and antagonistic activity with low potency at the human 5-HT2B receptor. S1RA inhibits neuropathic pain in formalin-induced nociception and capsaicin-induced mechanical hypersensitivity in mice. Sigma receptor modulators may show activity against SARS-CoV-2 as sigma receptors interact with SARS-CoV-2 proteins Nsp6 and Orf9c.,\u003cbr\u003e\nCanonical smiles:CC1=CC(=NN1C2=CC3=CC=CC=C3C=C2)OCCN4CCOCC4,\u003cbr\u003e\nInChi:InChI=1S\/C20H23N3O2\/c1-16-14-20(25-13-10-22-8-11-24-12-9-22)21-23(16)19-7-6-17-4-2-3-5-18(17)15-19\/h2-7,14-15H,8-13H2,1H3,\u003cbr\u003e\nInChiKey:DGPGXHRHNRYVDH-UHFFFAOYSA-N,\u003cbr\u003e\nIUPAC Name:4-[2-(5-methyl-1-naphthalen-2-ylpyrazol-3-yl)oxyethyl]morpholine\u003c\/p\u003e\n\n\u003cp\u003eProduct details:\u003cbr\u003e\nThis product is manufactured by BioVision, an Abcam company and was previously called B3048 S1RA (E-52862). B3048-1 is the same size as the 1 mg size of ab286948.\u003c\/p\u003e\n\n\u003cp\u003eProperties and Storage Information:\u003cbr\u003e\nShipped at conditions-Blue Ice, Appropriate short-term storage conditions--20°C, Appropriate long-term storage conditions--20°C\u003c\/p\u003e\n\n\u003cp\u003eSupplementary Information:\u003cbr\u003e\nThis supplementary information is collated from multiple sources and compiled automatically.\u003cbr\u003e\nThe 5-HT-2B receptor and Sigma1-receptor are two important protein targets with distinct mechanical roles. The 5-HT-2B receptor also known as the serotonin receptor 2B is a G-protein-coupled receptor with an approximate molecular mass of 54 kDa. Sigma1-receptor alternatively sometimes called the sigma-1 receptor is a chaperone protein that acts on multiple subcellular locations with a mass of about 25 kDa. The 5-HT-2B receptor is often expressed in the heart lungs and gastrointestinal tract while the Sigma1-receptor shows expression in the central nervous system liver and kidneys.\u003cbr\u003e\nBiological function summary\u003cbr\u003e\nSerotonin receptor 2B influences cardiovascular function gastrointestinal movement and mood regulation through serotonin signaling. It forms a complex with G-proteins to transduce signals. The Sigma1-receptor plays a role in cellular stress response and maintenance of calcium signaling affecting neuroplasticity and cellular survival. It associates with various ion channels and receptors to modulate their functions.\u003cbr\u003e\nPathways\u003cbr\u003e\nSerotonin receptor 2B takes part in the serotonin signaling cascade which is important for mood disorders and vasoconstriction. It interacts closely with other serotonin receptors notably 5-HT-2A and 5-HT-2C in the same family. The Sigma1-receptor participates in neuroprotection pathways by modulating the activity of the ion channels and receptors related to calcium and potassium having impactful interactions with proteins like N-methyl-D-aspartate (NMDA) receptors.\u003cbr\u003e\nSerotonin receptor 2B is involved in heart valve disease and pulmonary hypertension conditions where improper serotonin signaling can result in pathogenic vascular remodeling. It can influence heart-related disorders through interactions with proteins like transforming growth factor-beta (TGF-beta). The Sigma1-receptor is linked to neurodegenerative disorders such as Alzheimer's disease and amyotrophic lateral sclerosis (ALS) where its modulation of neuronal survival pathways and calcium homeostasis shows a protective effect relating it with markers like amyloid precursor protein (APP) in Alzheimer's pathology.\u003c\/p\u003e","brand":"Abcam","offers":[{"title":"Default Title","offer_id":46847496126633,"sku":"ab286948","price":0.99,"currency_code":"USD","in_stock":true}],"url":"https:\/\/iright.com\/products\/abcam-ab286948","provider":"Iright","version":"1.0","type":"link"}