Description
BI-1230 is potent and digit nanomolar inhibitor of HCV NS3 protease and of viral replication. BI-1230 is also highly selective against other serine/cysteine proteases. BI-1230 shows good Pharmacokinetic(PK) activity.
Product information
CAS Number: 849022-32-8
Molecular Weight: 816.96
Formula: C42H52N6O9S
Chemical Name: (1S,4R,6R,14S,18R)-14-{[(cyclopentyloxy)carbonyl]amino}-18-({7-methoxy-8-methyl-2-[2-(2-methylpropanamido)-1,3-thiazol-4-yl]quinolin-4-yl}oxy)-2,15-dioxo-3,16-diazatricyclo[14.3.0.0⁴,⁶]nonadec-7-ene-4-carboxylic acid
Smiles: CC1C(=CC=C2C=1N=C(C=C2O[C@H]1CN2[C@@H](C1)C(=O)N[C@@]1(C[C@@H]1C=CCCCCC[C@H](NC(=O)OC1CCCC1)C2=O)C(O)=O)C1=CSC(NC(=O)C(C)C)=N1)OC |c:27|
InChiKey: YQCVJBZPFAJZFJ-SYMKIPRJSA-N
InChi: InChI=1S/C42H52N6O9S/c1-23(2)36(49)46-40-44-31(22-58-40)30-19-34(28-16-17-33(55-4)24(3)35(28)43-30)56-27-18-32-37(50)47-42(39(52)53)20-25(42)12-8-6-5-7-9-15-29(38(51)48(32)21-27)45-41(54)57-26-13-10-11-14-26/h8,12,16-17,19,22-23,25-27,29,32H,5-7,9-11,13-15,18,20-21H2,1-4H3,(H,45,54)(H,47,50)(H,52,53)(H,44,46,49)/b12-8-/t25-,27+,29-,32-,42+/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
BI-1230 (60 min incubation) exhibits an IC50 value of 6.7 nM in a Enzymatic assay. BI-1230 (72 hours) shows EC50 values of 4.6 nM and <1.8 nM in a Cell-based HCVPV RNA replication Luciferase reporter assay, genotype background 1a and 1b, in Huh7 cells.
In Vivo:
BI-1230 (intravenous injection; 2 mg/kg) shows good PK activity in rat: CL: 15 ml/min/kg, Mean residence time after iv dose: 2.3 hours, Vss: 2.05 L/kg. BI-1230 (oral administation; 5 mg/kg) shows good PK activity in rat: T1/2: 2.1 hours; Tmax: 1.8 nM; Cmax: 405 nM; AUC0-inf: 2550 nM*h; F: 42%.
Products are for research use only. Not for human use.
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