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Chemical Structure| 357263-13-9 Chemical Structure| 357263-13-9

Structure of BMS-378806
CAS No.: 357263-13-9

Chemical Structure| 357263-13-9

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BMS-378806 selectively inhibits the binding of HIV-1 gp120 to the CD4 receptor with EC50 of 0.85-26.5 nM in virus.

Synonyms: BMS-806

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Product Details of BMS-378806

CAS No. :357263-13-9
Formula : C22H22N4O4
M.W : 406.43
SMILES Code : COC1=C2C(NC=C2C(C(N3CCN(C[C@H]3C)C(C4=CC=CC=C4)=O)=O)=O)=NC=C1
Synonyms :
BMS-806
MDL No. :MFCD09026945

Safety of BMS-378806

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
A549 cells 10 μM 1 hour Inhibited RSK4 activation, resulting in decreased cellular cIAP1 and cIAP2 expression PMC7199401
Canine Cf2Th thymocytes 1-300 nM 48 hours Test the inhibitory effects of BMS-806 and #155 on HIV-1 infection PMC371073
U87.CD4.CCR5 cells IC50 > 200 nM Evaluation of the inhibitory activity of BMS-378806 derivative 7 against HIV-1 PMC3673733
HeLa-CD4 50 nM 48 hours Determine the antiviral target of BMS-378806 PMC196918
293F cells 10 μM 1 hour To evaluate the effect of BMS-806 on monomeric gp120 binding, results showed BMS-806 mildly decreased the binding of CD4BS and CD4i antibodies. PMC7199401
Human 293T embryonic kidney cells 1-300 nM 48 hours Test the inhibitory effects of BMS-806 and #155 on HIV-1 infection PMC371073
IDCs 2.37 ± 0.46 nM (2h pulse), 0.35 ± 0.16 nM (24h pulse), 0.29 ± 0.21 nM (sustained exposure) 2h pulse, 24h pulse, sustained exposure Evaluate the inhibitory activity of DS003 against HIV-1 BaL infection in iDCs, results showed prolonged exposure significantly enhances inhibition PMC8416713
TZM-bl cells 1.09 ± 0.34 nM 48 hours Assess the ability of CRISPR-Cas9 to edit the CCR5 gene PMC8416713

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rats, dogs, and cynomolgus monkeys Rats, dogs, and cynomolgus monkeys Intravenous and oral 1 mg/kg i.v. and 5 mg/kg orally in rats; 0.67 mg/kg i.v. and 3.4 mg/kg orally in dogs and monkeys Single dose, plasma samples collected for 24 hours (8 hours in rats) Evaluate the pharmacokinetic properties of BMS-378806 PMC196918

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.46mL

0.49mL

0.25mL

12.30mL

2.46mL

1.23mL

24.60mL

4.92mL

2.46mL

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