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安全信息

SML2497

Sigma-Aldrich

BIO 1211 trifluoroacetate salt

≥97% (HPLC)

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别名:
2-MPUPA-LDVP trifluoroacetate, 4-(N′-(2-Methylphenyl)urea)-phenylacetyl-LDVP trifluoroacetate, BIO-1211 trifluoroacetate, BIO1211 trifluoroacetate, N-[2-[4-[[[(2-Methylphenyl)amino]carbonyl]amino]phenyl]acetyl]-L-leucyl-L-α-aspartyl-L-valyl-L-proline trifluoroacetate, N-[[4-[[[(2-Methylphenyl)amino]carbonyl]amino]-phenyl]acetyl]-LDVP trifluoroacetate, N-[[4-[[[(2-Methylphenyl)amino]carbonyl]amino]-phenyl]acetyl]-Leu-Asp-Val-Pro trifluoroacetate, N-[[4-[[[(2-Methylphenyl)amino]carbonyl]amino]-phenyl]acetyl]-fibronectin CS-1 fragment (1980-1983) trifluoroacetate
经验公式（希尔记法）:
C36H48N6O9 · xC2HF3O2
CAS号:
187735-94-0
分子量:
708.80 (free base basis)
MDL编号:
MFCD02259692

检测方案

≥97% (HPLC)

形式

film
lyophilized powder

储存条件

desiccated

颜色

white to beige

运输

wet ice

储存温度

−20°C

InChI

1S/C36H48N6O9/c1-20(2)17-26(38-29(43)18-23-12-14-24(15-13-23)37-36(51)40-25-10-7-6-9-22(25)5)32(46)39-27(19-30(44)45)33(47)41-31(21(3)4)34(48)42-16-8-11-28(42)35(49)50/h6-7,9-10,12-15,20-21,26-28,31H,8,11,16-19H2,1-5H3,(H,38,43)(H,39,46)(H,41,47)(H,44,45)(H,49,50)(H2,37,40,51)/t26-,27-,28-,31-/m0/s1

InChI key

NVVGCQABIHSJSQ-KFZSMJGVSA-N

生化/生理作用

BIO 1211 is a selective, tight-binding α4β1 (VLA-4, very late antigen-4; koff = 1.4 x 10-4/s, KD = 70 pM) integrin antagonist (VCAM-Ig Jurkat surface binding IC50 = 1 nM; integrin-mediated cell adhesion IC50 = 4 nM/α4β1, 2 μM/α4β7, >100 μM/α1β1, α5β1, α6β1, αLβ2, αIIBβ3) based on the Leu-Asp-Val (LDV) sequence from the alternatively spliced connecting segment-1 (CS-1) of fibronectin (aa 1980-1983). In addition to probing α4β1-mediated cellular responses, BIO 1211 is also widely used in animal disease models in vivo, including MS (5-10 mg/kg; murine EAE) and asthma (1-10 mg/kg via intranasal or nebulizer to mice, rats, sheep; 3 mg/sheep iv.).

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

常规特殊物品

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Olli-Pekka Pulkka et al.
Journal of cellular and molecular medicine, 22(4), 2220-2230 (2018-01-30)
The molecular mechanisms for the dissemination and metastasis of gastrointestinal stromal tumours (GIST) are incompletely understood. The purpose of the study was to investigate the clinical relevance of integrin alpha 4 (ITGA4) expression in GIST. GIST transcriptomes were first compared
B V Karanam et al.
Xenobiotica; the fate of foreign compounds in biological systems, 37(5), 487-502 (2007-05-25)
BIO1211 is a small peptidyl potent antagonist of the activated form of alpha4beta1 integrin. The effect of enalapril on the in vitro and in vivo cleavage of BIO1211 was investigated. In heparinized blood, plasma and rat liver, lung and intestinal
W M Abraham et al.
American journal of respiratory and critical care medicine, 162(2 Pt 1), 603-611 (2000-08-10)
The leukocyte integrin very late antigen-4 (alpha(4)beta(1), CD49d/CD29) is an adhesion receptor that plays an important role in allergic inflammation and contributes to antigen-induced late responses (LAR) and airway hyperresponsiveness (AHR). In this study, we show that single doses of
Gloria C Koo et al.
American journal of respiratory and critical care medicine, 167(10), 1400-1409 (2003-02-06)
A nonpeptidyl small molecule antagonist, compound A, to nonactivated very late antigen-4 (VLA4) was examined in lung inflammation induced by a single dose of ovalbumin challenge. Compound A presented a good pharmacokinetic property, when given intratracheally, and the blood cells
Nourollah Ramroodi et al.
Immunological investigations, 44(7), 694-712 (2015-10-06)
Some functional limitations and economic burden of therapeutic antibodies indicated that introducing of alternative therapeutic compounds with same or different mechanism of action could be worthwhile. In this regard small-molecule antagonists can have a wide range of impacts, so in
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