BIO-5192

Research use only, not for human use.

A potent, highly selective inhibitor of integrin α4β1 (VLA-4) with Kd of <10 pM, IC50 of 1.8 nM.

A potent, highly selective inhibitor of integrin α4β1 (VLA-4) with Kd of <10 pM, IC50 of 1.8 nM; displays selectively over a range of other integrins (IC50 are 138, 1053, > 500 and > 10,000 nM for α9β1, α2β1, α4β7 and αIIbβ3, respectively); mobilizes hematopoietic stem and progenitor cells (HSPCs) alone or combined with plerixafor (AMD3100).Multiple Sclerosis Discontinued.

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The combination of BIO5192 (1 mg/kg; i.v.) and Plerixafor (5 mg/kg; s.c.) exert an additive effect on progenitor mobilization.BIO5192 (30 mg/kg; s.c; bid; during days 5 through 14) delays paralysis associated with EAE (experimental autoimmune encephalomyelitis).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. Animal Model:C57BL/6J x 129Sv/J F1 mice Dosage:1 mg/kg (with Plerixafor: 5 mg/kg) Administration:I.v.Result:Exerted an additive effect on progenitor mobilization.Animal Model:Healthy female Lewis rats weighing 150g Dosage:30 mg/kg Administration:S.c; bid; during days 5 through 14 Result:Showed a 3-day delay in onset of disease.

BIO5192

Cell Cycle/DNA Damage

Integrin

Integrin

Inflammation/Immunology

Multiple Sclerosis

327613-57-0

817.78

C38H46Cl2N6O8S

>98% (HPLC)

In Vitro:?DMSO : 12.5 mg/mL (15.29 mM)

Cc1ccccc1NC(=O)Nc2ccc(cc2)CC(=O)N(C)[C@@H](CC(C)C)C(=O)NCC[C@@H](C(=O)O)NC(=O)[C@@H]3CCCN3S(=O)(=O)c4cc(cc(c4)Cl)Cl

(2S)-2-[[[(2S)-1-[(3,5-Dichlorophenyl)sulfonyl]-2-pyrrolidinyl]carbonyl]amino]-4-[[(2S)-4-methyl-2-[methyl[2-[4-[[[(2-methylphenyl)amino]carbonyl]amino]phenyl]acetyl]amino]-1-oxopentyl]amino]butanoic acid

(-20℃)

With Ice Pack

≥ 2 years