Description
Key facts
CAS number:223499-30-7,
Purity:>98%,
Form:SolidSee storage information,
Molecular weight:421.3 Da,
Molecular formula:C15H9F6N5OS,
PubChem:2455,
Nature:Synthetic,
Solubility:Soluble in ethanol to 100 mMSoluble in DMSO to 100 mM,
Biochemical name:N-[4-[3,5-bis(trifluoromethyl)pyrazol-1-yl]phenyl]-4-methylthiadiazole-5-carboxamide,
Biological description:Store-operated Ca2+ entry blocker. Potent, selective CRAC channel inhibitor. Inhibits thapsigargin-induced sustained Ca2+ influx (IC50 = 100 nM). Suppresses cytokine production. Potent T-cell antiproliferative agent (IC50 = 12.7 nM). Shows immunomodulatory and anti-inflammatory effects in vivo. Orally active.,
Canonical smiles:CC1=C(SN=N1)C(=O)NC2=CC=C(C=C2)N3C(=CC(=N3)C(F)(F)F)C(F)(F)F,
InChi:InChI=1S/C15H9F6N5OS/c1-7-12(28-25-23-7)13(27)22-8-2-4-9(5-3-8)26-11(15(19,20)21)6-10(24-26)14(16,17)18/h2-6H,1H3,(H,22,27),
InChiKey:XPRZIORDEVHURQ-UHFFFAOYSA-N,
IUPAC Name:N-[4-[3,5-bis(trifluoromethyl)pyrazol-1-yl]phenyl]-4-methylthiadiazole-5-carboxamide
Properties and Storage Information:
Shipped at conditions-Ambient - Can Ship with Ice, Appropriate short-term storage conditions--20°C, Appropriate long-term storage conditions--20°C, Storage information-Store under desiccating conditions, The product can be stored for up to 12 months
Supplementary Information:
This supplementary information is collated from multiple sources and compiled automatically.
Orai1 also known as CRACM1 is an important protein that forms part of the calcium release-activated calcium (CRAC) channels. These channels are essential for calcium ion flow across cell membranes. Orai1 weighs about 33 kDa and plays an integral role in cellular calcium homeostasis. This protein is expressed ubiquitously but it is found in high levels in excitable cells like T-cells where calcium signaling is important for activation and function. The Orai1 channel structure includes six transmembrane segments and works specifically with calcium-specific pore formation.
Biological function summary
Orai1 is a critical component of the store-operated calcium entry (SOCE) mechanism which maintains cellular calcium levels after depletion. Orai1 partners with stromal interaction molecule 1 (STIM1) to form the functional CRAC channel complex. Upon calcium store depletion STIM1 senses this change and interacts with Orai1 triggering calcium influx. This process is important in activating various cellular responses and promoting the function of immune cells among others.
Pathways
Orai1 is a significant player in the calcium signaling pathway and the immune response pathway. Through its role in maintaining cellular calcium levels it influences the activation of various downstream signaling events including those involving calcineurin and nuclear factor of activated T-cells (NFAT). These interactions highlight the protein's importance in transcriptional regulation and immune cell activation highlighting its connection to proteins like STIM1 and NFAT.
Orai1 disruption relates to immune dysfunction and autoimmune diseases like severe combined immunodeficiency (SCID) and rheumatoid arthritis. Mutations in Orai1 lead to impaired CRAC channel function and compromised calcium homeostasis affecting immune cell function. Furthermore the aberrant expression or function of Orai1 and its partner STIM1 associates with these disorders providing potential targets for therapeutic CRAC channel inhibitors aimed to restore normal signaling and immune function.
