2. Signaling Pathways
  3. Immunology/Inflammation
  4. Cyclophilin
  5. Cyclophilin D Isoform

Cyclophilin D

Cyclophilin D (CypD/PPIF) is a mitochondrial matrix peptidyl-prolyl cis-trans isomerase and a unique human cyclophilin isoform imported into the mitochondrial matrix[1]. Mechanistically, CypD facilitates mitochondrial permeability transition pore (mPTP) regulation, because Ppif−/− mitochondria lack CypD and require a higher Ca2+ load for pore opening[2]. Sustained CypD-dependent mPTP activation links Ca2+ overload and oxidative stress to mitochondrial swelling, membrane failure, and regulated necrotic cell death[2][3]. In disease models, CypD deficiency reduced ischemia/reperfusion-induced cardiac injury and decreased brain infarct size after focal cerebral ischemia[3][4]. CypD also controlled mitochondrial pore-dependent Ca2+ exchange, metabolic flexibility, and heart-failure susceptibility in mice[5]. Compared with related cyclophilins, CypD is distinguished by mitochondrial matrix localization rather than a general cytosolic or secretory cyclophilin role[1]. For experimental applications, small-molecule cyclophilin inhibitors blocked mPTP opening in liver mitochondria, mouse and human hepatocytes, and protected mice from hepatic ischemia/reperfusion injury[6]. Reviews of CypD inhibitors therefore position CypD as a practical target for mitochondria-related disease models and inhibitor-screening studies[7].

Cyclophilin D Related Products (9):

Cat. No. Product Name Effect Purity
  • HY-B0579
    Cyclosporin A
    		Inhibitor 99.94%
    Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC50 of 5 nM. Cyclosporin A also inhibits CD11a/CD18 adhesion.
  • HY-N0663
    Talatisamine
    		Activator 99.77%
    Talatisamine is an orally active cyclophilin D activator isolated from the roots of Aconitum carmichaeli Debx. Talatisamine exerts biological functions by activating cyclophilin D, inhibiting Ca2+-dependent opening of the mitochondrial permeability transition pore (mPTP) (IC50=78 μM), and blocking delayed rectifier K+ channels (IC50=146 μM). Talatisamine possesses both antioxidant and membrane-stabilizing properties, effectively inhibits lipid peroxidation and protects mitochondrial membrane function. Talatisamine exhibits multiple activities including antiarrhythmic, hypotensive, anti-inflammatory, anticancer and neuroprotective effects. Talatisamine finds applications in the research of ischemic diseases, rheumatoid arthritis, inflammation-related diseases and Alzheimer's disease.
  • HY-135644
    Rencofilstat
    Rencofilstat (CRV431) is an orally active pan-cyclophilin inhibitor with IC50 values of 2.5 nM, 3.1 nM, 2.8 nM, 7.3 nM for Cyp A, CypB, Cyp D and Cyp G, respectively. Rencofilstat reduces fibrosis and tumor growth in models of chronic liver disease. Rencofilstat can be used for the study of nonalcoholic steatohepatitis (NASH), hepatocellular carcinoma and viral hepatitis-induced liver disease.
  • HY-157088
    C105SR
    		Inhibitor 99.49%
    C105SR is a cyclophilin D (CypD) inhibitor targeting to peptidyl-prolylcis-trans isomerase (PPIase). C105SR inhibits mitochondrial permeability transition opening (mPTP) with an IC 50 of 5 nM. C105SR inhibits hypoxia and reoxygenation inudced hepatocyte apoptosis and increases the level of calcium retention capacity (CRC). C105SR exhibits hepaprotective effect in ischaemia-reperfusion injury (IRI) mouse model.
  • HY-151488
    CypD-IN-4
    		Inhibitor
    CypD-IN-4 is a potent and subtype-selective cyclophilin D (CypD) inhibitor. CypD-IN-4 has CypD affinity with an IC50 value of 0.057 μM. CypD-IN-4 can be used for the research of several diseases including oxidative stress, neurodegenerative disorders, liver diseases, aging, autophagy and diabetes.
  • HY-179417
    CypD-IN-7
    		Inhibitor
    CypD-IN-7 is a potent cyclophilin D (CypD/PPIF) inhibitor that inhibits CypD PPIase activity (Ki = 2.4 nM) and provides protection against mitochondrial permeability transition pore (MPTP) opening. CypD-IN-7 can be used for pancreatitis research.
  • HY-179416
    CypD-IN-6
    		Inhibitor
    CypD-IN-6 is a potent cyclophilin D (CypD/PPIF) inhibitor that inhibits CypD PPIase activity (Ki = 32 nM) and binds to CypD (Kd = 60 nM). CypD-IN-6 can be used for mitochondrial permeability transition pore (MPTP) related disease research such as ischemia-reperfusion injury and acute pancreatitis1.
  • HY-151487
    CypD-IN-3
    		Inhibitor
    CypD-IN-3 is a potent and subtype-selective cyclophilin D (CypD) inhibitor. CypD-IN-3 has CypD affinity with an IC50 value of 0.01 μM. CypD-IN-3 can be used for the research of several diseases including oxidative stress, neurodegenerative disorders, liver diseases, aging, autophagy and diabetes.
  • HY-151489
    CypE-IN-1
    		Inhibitor
    CypE-IN-1 is a potent and subtype-selective cyclophilin E (CypE) inhibitor. CypE-IN-1 has CypE affinity with IC50 and Ki values of 0.013 μM and 0.072 μM, respectively. CypE-IN-1 can be used for the research of several diseases including oxidative stress, neurodegenerative disorders, liver diseases, aging, autophagy and diabetes.