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abatacept

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库存信息

关闭

库存信息

关闭
货号 (SKU) 包装规格 是否现货 价格 数量
rp173355-500μg 500μg 期货 Stock Image
rp173355-1mg 1mg 期货 Stock Image

基本描述

产品名称 abatacept

产品规格参数

CAS编号和信息 rp173355

靶标

Target ID 2744
名称 CD80
缩写名 SHP2
家族 Other immune checkpoint proteins
别名 KCa2.1
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 1 288 3q13.33 CD80 CD80 molecule
Mouse 1 306 16 26.86 cM Cd80 CD80 antigen
Rat 2 321 11q21 Cd80 Cd80 molecule
RefSeq Protein NP_005182 (Hs) , NP_033985 (Mm) , NP_037058 (Rn)
RefSeq Nucleotide NM_005191 (Hs) , NM_009855 (Mm) , NM_012926 (Rn)
Entrez Gene 941 (Hs) , 12519 (Mm) , 25408 (Rn)
UniProtKB P33681 (Hs) , Q00609 (Mm)
Ensembl Gene ENSG00000121594 (Hs) , ENSMUSG00000075122 (Mm) , ENSRNOG00000001527 (Rn)
OMIM 112203 (Hs)
Protein GI 4885123 (Hs) , 112983684 (Mm) , 29789034 (Rn)
DrugBank Target P33681 (Hs)
CATH/Gene3D 2.60.40.10 (N/A)
ChEMBL Target CHEMBL2364157 (Hs)
Target ID 2745
名称 CD86
缩写名 SHP2
家族 Other immune checkpoint proteins
别名 KCa2.1
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 1 329 3q13.33 CD86 CD86 molecule
Mouse 1 309 16 25.72 cM Cd86 CD86 antigen
Rat 2 313 11q22 Cd86 CD86 molecule
RefSeq Protein NP_787058 (Hs) , NP_062261 (Mm) , NP_064466 (Rn)
RefSeq Nucleotide NM_175862 (Hs) , NM_019388 (Mm) , NM_020081 (Rn)
Entrez Gene 942 (Hs) , 12524 (Mm) , 56822 (Rn)
UniProtKB P42081 (Hs) , P42082 (Mm)
Ensembl Gene ENSG00000114013 (Hs) , ENSMUSG00000022901 (Mm) , ENSRNOG00000038835 (Rn)
OMIM 601020 (Hs)
Protein GI 332634934 (Hs) , 161484599 (Mm) , 11464989 (Rn)
DrugBank Target P42081 (Hs)
CATH/Gene3D 2.60.40.10 (N/A)
ChEMBL Target CHEMBL2364156 (Hs)

关联配体

Ligand ID 6891
名称 abatacept
别名 RG-1046
类别 Peptide
学名 4-amino-N-(4,6-dimethylpyrimidin-2-yl)benzenesulfonamide
生物活性评价 In a cell based CD80/86 inhibition assay abatacept inhibits IL-2 release with an IC50 of 22.6 nM .
评价 Abatacept is a recombinant protein fusing the extracellular domain of human cytotoxic T-lymphocyte-associated antigen 4 (CTLA-4) to the modified Fc (hinge, CH2, and CH3 domains) portion of human immunoglobulin G1 (IgG1) . In essence, abatacept is a CTLA-4 mimetic, that enhances CTLA-4's inhibitory signal to T cells, thereby down-modulating T cell mediated inflammation.
配体家族 Immune checkpoint modulators
单字母多肽序列 MGVLLTQRTLLSLVLALLFPSMASMAMHVAQPAVVLASSRGIASFVCEYASPGKATEVRVTVLRQADSQVTEVCAATYMMGNELTFLDDSICTGTSSGNQVNLTIQGLRAMDTGLYICKVELMYPPPYYLGIGNGTQIYVIDPEPCPDSDQEPKSSDKTHTSPPSPAPELLGGSSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK
三字母多肽序列
翻译后修饰
化学修饰 The drug is a dimeric protein, consisting of two identical subunits linked by a disulphide bridge (between Cys146 on each subunit). The sequence shown above is for a single monomer. Intra-subunit disulphide bridges form between cysteines 47-118, 74-92, 197-217 and 303-401. There are glycosylation sites at Asn102, Asn134 and Asn233. This additional structural information is taken from the INN record for the drug.

参考文献

1. Linsley PS, Brady W, Urnes M, Grosmaire LS, Damle NK, Ledbetter JA.  (1991)  CTLA-4 is a second receptor for the B cell activation antigen B7..  J Exp Med,  174  (3):  (561-9).  [PMID:1714933]
2. Ludvigsson J.  (2016)  Therapies to Preserve β-Cell Function in Type 1 Diabetes..  Drugs,  76  (2):  (169-85).  [PMID:26645223]
3. Davis IC, Randell J, Davis SN.  (2015)  Immunotherapies currently in development for the treatment of type 1 diabetes..  Expert Opin Investig Drugs,  24  (10):  (1331-41).  [PMID:26364507]
4. Douthwaite J, Moisan J, Privezentzev C, Soskic B, Sabbah S, Cohen S, Collinson A, England E, Huntington C, Kemp B et al..  (2017)  A CD80-Biased CTLA4-Ig Fusion Protein with Superior In Vivo Efficacy by Simultaneous Engineering of Affinity, Selectivity, Stability, and FcRn Binding..  J Immunol,  198  (1):  (528-537).  [PMID:27881707]

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