BIO 1211 |
| Catalog No.GC17560 |
BIO 1211 est un inhibiteur α4β1 (VLA-4) hautement sélectif et actif par voie orale, avec des valeurs IC50 de 4 nM et 2 μM pour α4β1 et α4β7, respectivement.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 187735-94-0
Sample solution is provided at 25 µL, 10mM.
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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.
| 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 |
| Solubility | 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 32 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
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