BIO 5192
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
BIO5192是整合蛋白α4β1的小分子抑制剂，IC50值为1.8 ± 0.7 nM [1]。
整合蛋白α4β1在炎症过程中至关重要。在炎症过程中，α4β1调节淋巴细胞迁移进入发炎组织[1]。
在使用表达α4β7、α9β1、α2β1和αIIbβ3的细胞实验中，BIO5192对α4β1表现出高选择性。BIO5192对α4β1的亲和性比与α4β1共享许多配体的α4β7高250至1000倍。BIO5192与α2β1和αIIbβ3的结合不紧密。在含有1 mM Mn2+的缓冲液中，可以观察到BIO5192与α9β1显著但低水平的结合（KD = 140 nM）[1]。
BIO5192治疗24小时后，淋巴细胞数目上升约1.5倍。使用BIO5192治疗后，有给予TA-2时将近一半的细胞释放到循环系统中。数据表明，24小时时BIO5192仍然与100％的α4β1受体结合，48小时的结合率为50％。大鼠中，与对照组相比，30 mg/kg剂量的BIO5192皮下给药，每日一次，将疾病EAE发病时间延迟1-2天，每日两次，将疾病EAE发病时间延迟3天。BIO5192治疗组中EAE的发病延迟与BIO5192结合长期占据α4β1，直至BIO5192在血液中检测不到的发现相一致[1]。
参考文献：
[1]. Leone DR, Giza K, Gill A, et al. An assessment of the mechanistic differences between two integrin α4β1 inhibitors, the monoclonal antibody TA-2 and the small molecule BIO5192, in rat experimental autoimmune encephalomyelitis[J]. Journal of Pharmacology and Experimental Therapeutics, 2003, 305(3): 1150-1162.
| Physical Appearance | White solid |
| Storage | Store at -20°C |
| M.Wt | 817.78 |
| Cas No. | 327613-57-0 |
| Formula | C38H46Cl2N6O8S |
| Solubility | <81.78mg/ml in DMSO; <40.89mg/ml in 1eq. NaOH |
| Chemical Name | (S)-2-((S)-1-((3,5-dichlorophenyl)sulfonyl)pyrrolidine-2-carboxamido)-4-((S)-4-methyl-2-(N-methyl-2-(4-(3-(o-tolyl)ureido)phenyl)acetamido)pentanamido)butanoic acid |
| SDF | Download SDF |
| Canonical SMILES | ClC1=CC(Cl)=CC(S(=O)(N2[C@H](C(N[C@H](C(O)=O)CCNC([C@H](CC(C)C)N(C)C(CC(C=C3)=CC=C3NC(NC4=CC=CC=C4C)=O)=O)=O)=O)CCC2)=O)=C1 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
化学结构
