BIO5192
Based on 2 publication(s) in Google Scholar
BIO5192 is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels.
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- Pureza: 99.96%
- No. CAS: 327613-57-0
- Fòrmula: C38H46Cl2N6O8S
- Peso molecular:817.78
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) BIO5192
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Actividad biológica
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α4β1 1.8 nM (IC50) |
α9β1 138 nM (IC50) |
α2β1 1053 nM (IC50) |
α4β7 >500 nM (IC50) |
BIO5192 (30 mg/kg; s.c; bid; during days 5 through 14) delays paralysis associated with EAE (experimental autoimmune encephalomyelitis)[2].
BIO5192 (1 mg/kg, i.v.) shows the terminal half-life is 1.1 hours. BIO5192 (3, 10, and 30 mg/kg; s.c.) shows half-lives of 1.7, 2.7, and 4.7 hours, respectively. The blood plasma curves show that the AUC for the s.c. route of administration increased about 2.5-fold from 5,460 h*ng/ml for the 3 mg/kg dose to 14,175 h*ng/ml for the 30 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J x 129Sv/J F1 mice[1]
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Dosage:1 mg/kg (with Plerixafor: 5 mg/kg)
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Administration:I.v.
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Result:Exerted an additive effect on progenitor mobilization.
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Animal Model:Healthy female Lewis rats weighing 150g[2]
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Dosage:30 mg/kg
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Administration:S.c; bid; during days 5 through 14
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Result:Showed a 3-day delay in onset of disease.
Chemical Information
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No. CAS 327613-57-0
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Appearance Solid
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Peso molecular 817.78
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Fòrmula C38H46Cl2N6O8S
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Color White to off-white
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SMILES
O=[S](N(CCC1)[C@@H]1C(N[C@H](C(O)=O)CCNC([C@H](CC(C)C)N(C)C(CC(C=C2)=CC=C2NC(NC(C=CC=C3)=C3C)=O)=O)=O)=O)(C4=CC(Cl)=CC(Cl)=C4)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Blood Adv
VLA-4 agonist promotes engraftment and immune reconstitution of allogeneic hematopoietic stem cells. [Abstract]2026 May 12;10(9):3103-3117. PMID: 41758999 -
Immun Ageing
Vascular Cell Adhesion Molecule-1 (VCAM-1) contributes to macular fibrosis in neovascular age-related macular degeneration through modulating macrophage functions. [Abstract]2023 Nov 20;20(1):65. PMID: 37985993
Solvente y solubilidad
DMSO : 100 mg/mL (122.28 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.06 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Ramirez P, et al. BIO5192, a small molecule inhibitor of VLA-4, mobilizes hematopoietic stem and progenitor cells. Blood. 2009;114(7):1340‐1343. [Content Brief]
[2]. Leone DR, et al. An assessment of the mechanistic differences between two integrin alpha 4 beta 1 inhibitors, the monoclonal antibody TA-2 and the small molecule BIO5192, in rat experimental autoimmune encephalomyelitis. J Pharmacol Exp Ther. 2003;305(3): [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.2228 mL | 6.1141 mL | 12.2282 mL | 30.5706 mL |
| 5 mM | 0.2446 mL | 1.2228 mL | 2.4456 mL | 6.1141 mL | |
| 10 mM | 0.1223 mL | 0.6114 mL | 1.2228 mL | 3.0571 mL | |
| 15 mM | 0.0815 mL | 0.4076 mL | 0.8152 mL | 2.0380 mL | |
| 20 mM | 0.0611 mL | 0.3057 mL | 0.6114 mL | 1.5285 mL | |
| 25 mM | 0.0489 mL | 0.2446 mL | 0.4891 mL | 1.2228 mL | |
| 30 mM | 0.0408 mL | 0.2038 mL | 0.4076 mL | 1.0190 mL | |
| 40 mM | 0.0306 mL | 0.1529 mL | 0.3057 mL | 0.7643 mL | |
| 50 mM | 0.0245 mL | 0.1223 mL | 0.2446 mL | 0.6114 mL | |
| 60 mM | 0.0204 mL | 0.1019 mL | 0.2038 mL | 0.5095 mL | |
| 80 mM | 0.0153 mL | 0.0764 mL | 0.1529 mL | 0.3821 mL | |
| 100 mM | 0.0122 mL | 0.0611 mL | 0.1223 mL | 0.3057 mL |
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