小分子抑制剂

Small molecule inhibitor

Abatacept

货号:HY-108829
规格:
名称:Synonyms: CTLA4lg; BMS-188667

产品详情

生物活性

Abatacept (CTLA4lg) is a soluble fusion protein consisting of the extra-cellular domain of human CTLA4 and a fragment of the Fc portion of human IgG1 (hinge and CH2 and 3 domains)[1]. Abatacept is a selective T-cell co-stimulation modulator and a protein drug for the autoimmune diseases[2].

体内研究
(In Vivo)

Abatacept reduces paw edema, and the SC Multiple-dose group shows significantly greater (tobs = 2.50) paw edema reduction compared with the IV dose group[2].
Abatacept exhibits linear PK across the studied doses. The NCA clearance (CL) is 20.8 mL/day/kg, volume (Vss) is 146 mL/kg, and bioavailability (F) of the SC dose dosing is 57.7%[2].
Abatacept (oral; 10 mg/kg; every 2 days) reduces the proportion of activated T cells (CD44highCD62L–) and inhibits the up-regulation of ICOS and CD71 in homozygous DO11.10 RAG-2–/–BALB/c (H-2d/d) mice[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Lewis rats (6-9 weeks old) with weights of 150-175 g[2]
Dosage: 10 mg/kg (IV), 20 mg/kg (SC single-dose), 20 mg/kg (SC Multiple-dose) on day 21 with 10 mg/kg SC doses on days 23, 25, 27, and 29
Administration: IV or SC
Result: Reduced paw edema, and the SC Multiple-dose group showed significantly greater (tobs = 2.50) paw edema reduction compared with the IV dose group.
 
Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT00784459 Washington University School of Medicine|Bristol-Myers Squibb
Atopic Asthma
October 2008 Phase 2
NCT04449224 Hanyang University|Ministry of Health, Republic of Korea
Rheumatoid Arthritis
April 27, 2020  
NCT04593940 Daniel Benjamin|National Center for Advancing Translational Science (NCATS)|Biomedical Advanced Research and Development Authority|Duke University
Covid19
October 15, 2020 Phase 3
 
CAS 号
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献