| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
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Purity: ≥98%
BIO-5192 is a novel, potent α4β1 VLA-4 inhibitor with Kd<10 pM. It selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 hydrate results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels. BIO-5192 has been shown to increase mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels. An additive affect on HSPC mobilization (3-fold) was observed when plerixafor (AMD3100), a small molecule inhibitor of the CXCR-4/SDF-1 axis, was combined with BIO5192. HSPCs mobilized by BIO5192 or the combination of BIO5192 and plerixafor has been shown to mobilize long-term repopulating cells, which successfully engraft and expand in a multilineage fashion in secondary transplantation recipients.
| 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].
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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. |
| References |
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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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