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BIO 1211
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BIO 1211图片
CAS NO:187735-94-0
包装:1mg
市场价:2489元

产品介绍
BIO 1211 是一种高选择性和口服活性的 α4β1 (VLA-4) 抑制剂,对 α4β1 和 α4β7 的 IC50 值分别为 4 nM 和 2 μM。
Cas No.187735-94-0
化学名(2S)-1-[(2S)-2-[[(2S)-3-carboxy-2-[[(2S)-4-methyl-2-[[2-[4-[(2-methylphenyl)carbamoylamino]phenyl]acetyl]amino]pentanoyl]amino]propanoyl]amino]-3-methylbutanoyl]pyrrolidine-2-carboxylic acid
Canonical SMILESCC1=CC=CC=C1NC(=O)NC2=CC=C(C=C2)CC(=O)NC(CC(C)C)C(=O)NC(CC(=O)O)C(=O)NC(C(C)C)C(=O)N3CCCC3C(=O)O
分子式C36H48N6O9
分子量708.8
溶解度Soluble to 2 mg/ml in 0.2M PBS
储存条件Store at -20°C, sealed storage, away from moisture and light
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

BIO 1211 is a selective and high affinity inhibitor of α4β1 with IC50 value of 0.004uM [1].
The leukocyte integrin α4β1 mediates leukocyte recruitment, activation, apoptosis inhibition and mediator release, it plays an important role in inflammatory responses [1].
BIO-1211 was about 200-fold selective for the activated form of α4β1 and it stimulated expression of ligand-induced epitopes on the integrin β1 subunit, consistent with occupancy of the receptor's ligand-binding site [1]. In Jurkat cells, KD values for BIO1211 binding ranged from 20–40 nM in the nonactivated state of the integrin to 100 pM in the activated state. Different KD values were controlled exclusively by differences in the dissociation rates of the integrin-BIO1211 complex [2].
Treatment allergic sheep with a 3-mg nebulized dose BIO-1211, BIO-1211 prevented nonspecific airway hyperresponsiveness to carbachol and inhibited early and late airway responses following antigen challenge [1].
References:
[1]. Lin Kc, Ateeq HS, Hsiung SH, et al. Selective, tight-binding inhibitors of integrin α4β1 that inhibit allergic airway responses. J Med Chem, 1999, 42(5): 920-934.
[2]. Chen LL, Whitty A, Lobb RR, et al. Multiple activation sites of integrin α4β1 detected through their different affinities for a small molecule ligand. J Biol Chem, 1999, 274(19): 13167-13175.