| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
BIO-5192 targets integrin α4β1 (VLA-4), a cell surface receptor that mediates cell-cell and cell-extracellular matrix interactions. VLA-4 is involved in various physiological and pathological processes, including lymphocyte homing, inflammation, and cancer metastasis. BIO-5192 is a potent and selective inhibitor of α4β1, with a Kd of <10 pM and an IC50 of 1.8 nM. By binding to α4β1, BIO-5192 blocks the interaction between VLA-4 and its ligands, such as VCAM-1 and fibronectin, thereby inhibiting cell adhesion and migration.
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| ln Vitro |
In vitro, BIO-5192 is a highly potent inhibitor of integrin α4β1 with a Kd of <10 pM and an IC50 of 1.8 nM. It displays significant selectivity for α4β1 over a range of other integrins. BIO-5192 causes a 30-fold increase in the mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels. This activity makes it a valuable tool for studying stem cell mobilization and integrin biology.
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| ln Vivo |
The combination of BIO5192 (1 mg/kg; intravenously) and Plerixafor (5 mg/kg; subcutaneously) produces additive effects on progenitor cell mobilization [1]. BIO5192 (30 mg/kg; subcutaneous; bid; days 5 to 14) delays paralysis associated with EAE (experimental autoimmune encephalomyelitis) [2]. BIO5192 (1 mg/kg, intravenously) showed a terminal half-life of 1.1 hours. The half-lives of BIO5192 (3, 10 and 30 mg/kg; subcutaneous) are 1.7, 2.7 and 4.7 hours, respectively. Plasma curves showed an approximately 2.5-fold increase in AUC for the subcutaneous route, from 5,460 h*ng/ml at the 3 mg/kg dose to 14,175 h*ng/ml at the 30 mg/kg dose [1].
In vivo, BIO-5192 has been shown to increase the mobilization of hematopoietic stem and progenitor cells (HSPCs) in murine models. The compound's ability to block VLA-4-mediated adhesion facilitates the release of stem cells from the bone marrow into the circulation. This suggests potential applications in stem cell transplantation and mobilization therapies. However, specific in vivo protocols and results are not extensively detailed in standard product descriptions. BIO-5192 is primarily a research tool for studying integrin function. |
| Enzyme Assay |
In vitro receptor binding assays for BIO-5192 measure its affinity for integrin α4β1. Binding assays are performed using purified α4β1 protein or cells expressing α4β1 and a labeled ligand (e.g., VCAM-1 or fibronectin). BIO-5192 is added at increasing concentrations to compete with the labeled ligand. The Kd and IC50 are determined from binding curves. Selectivity is assessed by testing the compound against a panel of other integrins, including α9β1, α2β1, α4β7, and αIIbβ3.
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| Cell Assay |
In vitro cell-based assays for BIO-5192 are used to study its effects on integrin-mediated cell adhesion and migration. Cells expressing α4β1 (e.g., lymphocytes or hematopoietic stem cells) are treated with BIO-5192, and their adhesion to immobilized VCAM-1 or fibronectin is measured. Cell migration assays, such as transwell migration assays, can also be performed. The compound's ability to inhibit cell adhesion and migration is assessed. These assays confirm the functional activity of BIO-5192 as an integrin inhibitor.
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| Animal Protocol |
Animal/Disease Models: C57BL/6J x 129Sv/J F1 mice [1]
Doses: 1 mg/kg (with plerixafor: 5 mg/kg) Route of Administration: intravenous (iv) (iv)injection Experimental Results: Additive effect on progenitor cell mobilization. Animal/Disease Models: Healthy female Lewis rats, body weight 150g [2] Doses: 30 mg/kg Route of Administration: Sc; Bid; Days 5 to 14 Experimental Results: demonstrated a 3-day delay in disease onset. In vivo animal experiments for BIO-5192 have been conducted in murine models to study stem cell mobilization. In a typical study, BIO-5192 is administered subcutaneously to mice at doses of 3, 10, and 30 mg/kg. The number of hematopoietic stem and progenitor cells (HSPCs) in the peripheral blood is measured at various time points. The compound causes a 30-fold increase in HSPC mobilization over basal levels. These studies confirm the in vivo activity of BIO-5192 in mobilizing stem cells. |
| ADME/Pharmacokinetics |
BIO-5192 has a molecular weight of 817.78 g/mol and a molecular formula of C38H46Cl2N6O8S. It has a density of 1.4±0.1 g/cm3. The compound is a solid with a purity of ≥98% by HPLC. It is soluble in DMSO and other organic solvents. For storage, it is recommended to keep the powder at -20°C. Pharmacokinetic studies show that BIO-5192 has a terminal half-life of 1.1 hours. Subcutaneous administration at 3, 10, and 30 mg/kg results in half-lives of 1.7, 2.7, and 4.7 hours, respectively.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for BIO-5192 is not provided in standard product descriptions. As a research compound, its toxicity profile has not been extensively characterized. In vivo studies have used BIO-5192 at doses up to 30 mg/kg in mice without reported overt toxicity. However, comprehensive toxicological studies have not been reported. As with all research chemicals, standard laboratory safety precautions should be followed when handling BIO-5192. Its use is limited to research applications.
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| References |
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| Additional Infomation |
BIO-5192 is a research compound and is not approved for any clinical or therapeutic use. It is a potent, highly selective inhibitor of integrin α4β1 (VLA-4) with a Kd of <10 pM and an IC50 of 1.8 nM. BIO-5192 displays selectivity for α4β1 over a range of other integrins. It causes a 30-fold increase in the mobilization of murine hematopoietic stem and progenitors (HSPCs). The compound is a valuable research tool for studying integrin-mediated cell adhesion, migration, and stem cell mobilization.
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| Exact Mass |
816.247
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| CAS # |
327613-57-0
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| Related CAS # |
BIO5192 hydrate
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| PubChem CID |
10350459
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.625
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| LogP |
5.1
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
16
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| Heavy Atom Count |
55
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| Complexity |
1430
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| Defined Atom Stereocenter Count |
3
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| SMILES |
CC1=CC=CC=C1NC(=O)NC2=CC=C(C=C2)CC(=O)N(C)C(CC(C)C)C(=O)NCCC(C(=O)O)NC(=O)C3CCCN3S(=O)(=O)C4=CC(=CC(=C4)Cl)Cl
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| InChi Key |
MNQBPRHHZPXCKZ-ZDCRTTOTSA-N
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| InChi Code |
1S/C38H46Cl2N6O8S/c1-23(2)18-33(45(4)34(47)19-25-11-13-28(14-12-25)42-38(52)44-30-9-6-5-8-24(30)3)35(48)41-16-15-31(37(50)51)43-36(49)32-10-7-17-46(32)55(53,54)29-21-26(39)20-27(40)22-29/h5-6,8-9,11-14,20-23,31-33H,7,10,15-19H2,1-4H3,(H,41,48)(H,43,49)(H,50,51)(H2,42,44,52)/t31-,32-,33-/m0/s1
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| Chemical Name |
Butanoic acid,
1-((3,5-dichlorophenyl)sulfonyl)-L-prolyl-N4-(N-methyl-N-((4-((((2-methylphenyl)amino)carbonyl)amino)phenyl)acetyl)-L-leucyl)-2,4-diamino-,
(2S)-
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| Synonyms |
BIO-5192 AMD-15057BIO5192 AMD15057BIO 5192 AMD 15057
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~12.5 mg/mL (~15.29 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (1.53 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (1.53 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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