AP1903


CAS No. : 195514-63-7

AP1903,195514-63-7
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I002495
Synonyms:AP1903; Rimiducid;
Molecular Formula:C78H98N4O20
Molecular Weight:1411.63
Target:Homodimerizers
IC50:0.1 nM (EC50, HT1080)
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Appearance:Semisolid (wax like)
Purity: > 98%
Cat No:I002495
Cas No:195514-63-7
Product-Name:AP1903
IUPAC Name:[(1R)-3-(3,4-dimethoxyphenyl)-1-[3-[2-[2-[[2-[3-[(1R)-3-(3,4-dimethoxyphenyl)-1-[(2S)-1-[(2S)-2-(3,4,5-trimethoxyphenyl)butanoyl]piperidine-2-carbonyl]oxypropyl]phenoxy]acetyl]amino]ethylamino]-2-oxoethoxy]phenyl]propyl] (2S)-1-[(2S)-2-(3,4,5-trimethoxyphenyl)butanoyl]piperidine-2-carboxylate
InChI:InChI=1S/C78H98N4O20/c1-13-57(53-43-67(93-7)73(97-11)68(44-53)94-8)75(85)81-37-17-15-25-59(81)77(87)101-61(31-27-49-29-33-63(89-3)65(39-49)91-5)51-21-19-23-55(41-51)99-47-71(83)79-35-36-80-72(84)48-100-56-24-20-22-52(42-56)62(32-28-50-30-34-64(90-4)66(40-
InChIKey:GQLCLPLEEOUJQC-WFMNNBDOSA-N
SMILES:O=C(NCCNC(COC1=CC([C@H](OC([C@H]2CCCCN2C([C@H](C3=CC(OC)=C(OC)C(OC)=C3)CC)=O)=O)CCC4=CC=C(OC)C(OC)=C4)=CC=C1)=O)COC5=CC([C@H](OC([C@H]6CCCCN6C([C@@H](CC)C7=CC(OC)=C(OC)C(OC)=C7)=O)=O)CCC8=CC=C(OC)C(OC)=C8)=CC=C5.

Rimiducid is a lipid-permeable tacrolimus analogue with homodimerizing activity. Dimerizer drug AP1903(cas 195514-63-7) homodimerizes an analogue of human protein FKBP12 (Fv) which contains a single acid substitution (Phe36Val) so that AP1903 binds to wild-type FKBP12 with 1000-fold lower affinity. This agent is used to homodimerize the Fv-containing drug-binding domains of genetically engineered receptors such as the iCD40 receptor of the autologous dendritic cell vaccine BP-GMAX-CD1, resulting in receptor activation.

1:J Clin Pharmacol. 2001 Aug;41(8):870-9. Intravenous safety and pharmacokinetics of a novel dimerizer drug, AP1903, in healthy volunteers.Iuliucci JD,Oliver SD,Morley S,Ward C,Ward J,Dalgarno D,Clackson T,Berger HJ, PMID: 11504275
Abstract: AP1903 is a novel gene-targeted drug that is being developed for use in drug-regulated cell therapies. An intravenous, single-blind, placebo- and saline-controlled, ascending-dose study was performed to evaluate the safety, tolerability, and pharmacokinetics of AP1903. Twenty-eight normal healthy male volunteers were randomized into five dosage groups of AP1903 (0.01, 0.05, 0.1, 0.5, and 1 mg/kg). Within each group, 4 volunteers received a single dose of AP1903, 1 volunteer received an equal volume of placebo, and 1 received an equal volume of normal saline. The only exception was in the 0.5 mg/kg group, in which 4 volunteers were dosed: 3 received AP1903 and 1 received normal saline. All dosages were administered as intravenous infusions over 2 hours. Clinical safety parameters were monitored, and serial blood and urine samples were collected for analysis of AP1903. No drug-related adverse events were observed at any of the dose levels with the possible exception of facial flushing in 1 volunteer at the 1.0 mg/kg dose level. AP1903 plasma levels were directly proportional to the administered dose, with mean Cmax values ranging from approximately 10 to 1,275 ng/mL over the 0.01 to 1.0 mg/kg dose range. Following the infusion period, blood concentrations revealed a rapid distribution phase, with plasma levels being reduced to approximately 18%, 7%, and 1% of the maximal concentration at 0.5, 2, and 10 hours postdose, respectively. AP1903 was shown to be safe and well tolerated at all dose levels and demonstrated a favorable pharmacokinetic profile at doses well above the anticipated therapeutic dose.
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