A cell-permeable inhibitor of caspase-1, caspase-4, and caspase-5.
Caspase-1 inhibitor-I is a cell-permeable inhibitor of caspase-1 (also known as ICE or Interleukin-1β Converting Enzyme), caspase-4, and caspase-5. The C-terminal sequence (YVAD-CHO) of this peptide is a highly specific, potent, and reversible inhibitor of caspase-1 (Ki = 1 nM). The N-terminal amino acid residues 1-16 correspond to the hydrophobic region of the signal peptide of the Kaposi fibroblast growth factor (K-FGF) and confer cell-permeability to the peptide.
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Thornberry, N.A., et al. 1992. Nature. 356: 768-774. PMID: 1574116
[2] Thornberry, N.A., et al. 1994. Biochemistry. 33: 3934-3940. PMID: 8142397
[3] Thornberry, N.A., 1994. Meth. Enzymol. 244: 615-631. PMID: 7845238
[4] Lin, Y.Z., et al. 1995. J. Biol. Chem. 270: 14255-14258. PMID: 7782278
分子式 C97H160N20O24 |
分子量 1990.4 |
CAS号 201608-12-0 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO Soluble |
Water <1 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT02287818 | Gout | Drug: Placebo|Drug: AC-201|Drug: Febuxostat | TWi Biotechnology, Inc. | Phase 2 | 2014-12-01 | 2016-06-28 |
NCT02293811 | Crohn Disease-Associated Colorectal Adenocarcinoma | Other: Analysis | Centre Hospitalier Universitaire de Nice | 2014-12-01 | 2014-11-14 | |
NCT02090101 | Metastatic Colorectal Cancer | Drug: ANAKINRA | Centre Georges Francois Leclerc | Phase 2 | 2014-06-01 | 2016-04-22 |
NCT01538342 | Psoriasis|Atopic Dermatitis | Other: 3 Biopsies|Other: 2 biopsies|Other: biopsy | Centre Hospitalier Universitaire de Nice | 2012-07-01 | 2016-04-22 | |
NCT02656056 | Obesity | Other: Food: (Q-Can Plus fermented soybean beverage) | Yale University|BESO Biological Research, Inc. | Phase 1 | 2016-01-01 | 2017-02-17 |
NCT00137111 | Lymphoblastic Leukemia, Acute | Drug: Prednisone, Dexamethasone, Vincristine, Daunorubicin|Drug: Doxorubicin, L-asparaginase, PEG-L-asparaginase, Erwinia asparaginase|Drug: Methotrexate, Cyclophosphamide, Cytarabine, Etoposide|Drug: Mercaptopurine, Imatinib|Procedure: chemotherapy, intrathecal chemotherapy|Procedure: steroid therapy, hematopoietic stem cell transplantation | St. Jude Children's Research Hospital|National Cancer Institute (NCI) | Phase 3 | 2000-06-01 | 2016-06-01 |
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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