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BIO 1211

カタログ番号GC17560

BIO 1211 は、α4β1 および α4β7 に対してそれぞれ 4 nM および 2 μM の IC50 値を持つ、高度に選択的で経口的に活性な α4β1 (VLA-4) 阻害剤です。

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BIO 1211 化学構造

Cas No.: 187735-94-0

サイズ 価格 在庫数 個数
1mg
$244.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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.

Chemical Properties

Cas No. 187735-94-0 SDF
Chemical Name (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 SMILES CC1=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
Formula C36H48N6O9 M.Wt 708.8
溶解度 Soluble to 2 mg/ml in 0.2M PBS Storage Store at -20°C, sealed storage, away from moisture and light
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.4108 mL 7.0542 mL 14.1084 mL
5 mM 0.2822 mL 1.4108 mL 2.8217 mL
10 mM 0.1411 mL 0.7054 mL 1.4108 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 32 reference(s) in Google Scholar.)

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