生物活性

• 描述CM-4620 is a CRAC (calcium-release activated calcium-channel) inhibitor with IC50 values of 119, 895 nM for Orai1/STIM1 and Orai2/STIM1 channels, respectively. Treatment with CM-4620 blocked SOCE in mouse pancreatic acinar cells in a dose-dependent manner, with IC50 value of 0.7μM, indicating that it may block the cell's ability to reload its ER with Calcium for successive rounds of signaling. Also CCK-induced Ca²⁺ entry in mouse pancreatic acinar cells could blocked by CM-4620. Release of multiple cytokines, like IFNgamma, IL-4, IL-6, IL-1beta, IL-6, IL-10, TNF-alpha, IL-2 and IL-17, were potently inhibited by CM-4620. Intraperitoneal injection with CM-4620 at dose ranging in 2-20mg/kg produced significant and dose-dependent reductions in caerulein-induced pathology in the mouse pancreas.

• 动物研究
  剂量	Rat: 5 mg/kg - 20 mg/kg[1] (i.v.) Mice: 20 mg/kg[1] (i.p.)
  给药途径	i.v., i.p.

• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT03709342	Acute Pancreatitis	Phase 2	Not yet recruiting	April 2019	United States, Michigan ... more >> Henry Ford Hospital Not yet recruiting Detroit, Michigan, United States, 48202 Contact: Joseph Miller, MD    313-916-5419    jmiller6@hfhs.org    Contact: Kathleen Wilson, RN    313-916-9551    kwilso10@hfhs.org Collapse <<
  NCT03401190	Acute Pancreatitis ... more >> Systemic Inflammatory Response Syndrome Collapse <<	Phase 2	Recruiting	March 2019	United States, Michigan ... more >> Detroit Receiving Hospital (Wayne State) Recruiting Detroit, Michigan, United States, 48201 Contact: John Wilburn, MD    313-745-4347    jwilburn@med.wayne.edu    Contact: Thomas Mazzocco, RN    313-745-4347    tmazzocco@wayne.edu    Henry Ford Hospital Recruiting Detroit, Michigan, United States, 48202 Contact: Joseph Miller, MD    313-916-5419    jmiller6@hfhs.org    Contact: Shannen Berry, RN    313-916-8551    sberry9@hfhs.org    Sinai-Grace Hospital (Wayne State) Recruiting Detroit, Michigan, United States, 48235 Contact: John Wilburn, MD    313-966-1829    jwilburn@med.wayne.edu    Contact: Thomas Mazzocco, RN    313-966-1829    tmazzocco@wayne.edu    United States, Minnesota Hennepin County Medical Center Recruiting Minneapolis, Minnesota, United States, 55415 Contact: Matthew Prekker, MD       matthew.prekker@hcmed.org    Contact: Audrey Hendrickson, MPH    612-873-9528    audrey.hendrickson@hcmed.org    Regions Hospital Recruiting Saint Paul, Minnesota, United States, 55101 Contact: Charles Bruen, MD       charles.a.bruen@healthpartners.com    Contact: Alexia Terwillinger    651-254-5315    alexia.j.terwillinger@healthpartners.com    United States, Missouri Washington University Recruiting Saint Louis, Missouri, United States, 63110 Contact: Philip Chan, MD       chanp@wustl.edu    Contact: Delea Payne-Gates    314-305-1054    dpayne@wustl.edu    United States, Ohio MetroHealth (Case Western) Recruiting Cleveland, Ohio, United States, 44109 Contact: Jon Schrock, MD       jschrock@metrohealth.org    Contact: Catherine Gilman, RN    216-957-6488    cgilman@metrohealth.org    Riverside Methodist Recruiting Columbus, Ohio, United States, 43214 Contact: Caleb Mackey, MD       cmackey@remdavis.com    Contact: Jennifer Botte, RN    614-487-2560    jbotte@remdavis.com    United States, Texas Ben Taub (Baylor College of Medicine) Recruiting Houston, Texas, United States, 77030 Contact: Frank Peacock, MD    713-873-7042       Contact: Kelly Keene, RN    713-873-7042    Kelly.Keene@bcm.edu Collapse <<