ChemicalBook > CAS DataBase List > AP20187

AP20187

Product Name
AP20187
CAS No.
195514-80-8
Chemical Name
AP20187
Synonyms
AP20187;B/B Homodimerizer;AP20187 (AP-20187;AP20187;AP-20187;AP 20187;inhibit,AP 20187,AP20187,FKBP,FK506-binding protein,Inhibitor,AP-20187;(1S,1'S)-(((2,2'-((2-((dimethylamino)methyl)propane-1,3-diyl)bis(azanediyl))bis(acetyl))bis(oxy))bis(3,1-phenylene))bis(3-(3,4-dimethoxyphenyl)propane-1,1-diyl) (2S,2'S)-bis(1-(2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate);2-Piperidinecarboxylic acid, 1-[(2S)-1-oxo-2-(3,4,5-trimethoxyphenyl)butyl]-, 2,2'-[[2-[( dimethylamino)methyl]-1,3-propanediyl]bis[imino(2-oxo-2,1-ethanediyl)oxy-3,1-phen ylene[(1R)-3-(3,4-dimethoxyphenyl)propylidene]]] ester, (2S,2'S)-;(1S,1'S)-(((2,2'-((2-((dimethylamino)methyl)propane-1,3-diyl)bis(azanediyl))bis(acetyl))bis(oxy))bis(3,1-phenylene))bis(3-(3,4-dimethoxyphenyl)propane-1,1-diyl) (2S,2'S)-bis(1-(2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate);(1R,1'R)-(((((2-((dimethylamino)methyl)propane-1,3-diyl)bis(azanediyl))bis(2-oxoethane-2,1-diyl))bis(oxy))bis(3,1-phenylene))bis(3-(3,4-dimethoxyphenyl)propane-1,1-diyl) (2S,2'S)-bis(1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate);(S,2S,2'S)-(1R,1'R)-(((((2-((dimethylamino)methyl)propane-1,3-diyl)bis(azanediyl))bis(2-oxoethane-2,1-diyl))bis(oxy))bis(3,1-phenylene))bis(3-(3,4-dimethoxyphenyl)propane-1,1-diyl) bis(1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate)
CBNumber
CB92677067
Molecular Formula
C82H107N5O20
Formula Weight
1482.75
MOL File
195514-80-8.mol
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AP20187 Property

Boiling point:
1333.5±65.0 °C(Predicted)
Density 
1.192±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C,protect from light
solubility 
≥74.14 mg/mL in DMSO; ≥100 mg/mL in EtOH
form 
A solid
pka
13.97±0.46(Predicted)
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Tocris
Product number
6297
Product name
AP20187
Purity
≥98%(HPLC)
Packaging
5
Price
$335
Updated
2021/12/16
ChemScene
Product number
CS-1953
Product name
AP20187
Purity
99.80%
Packaging
1mg
Price
$360
Updated
2021/12/16
ApexBio Technology
Product number
B1274
Product name
AP20187
Packaging
1mg
Price
$275
Updated
2021/12/16
ApexBio Technology
Product number
B1274
Product name
AP20187
Packaging
5mg
Price
$733
Updated
2021/12/16
ChemScene
Product number
CS-1953
Product name
AP20187
Purity
99.80%
Packaging
5mg
Price
$960
Updated
2021/12/16
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AP20187 Chemical Properties,Usage,Production

Definition

ChEBI: AP20187 is a tertiary amino compound that is 2-(aminomethyl)-N,N-dimethylpropane-1,3-diamine in which the primary ammino groups have each been acylated by condensation with the carboxy group of 2-{3-[(1R)-3-(3,4-dimethoxyphenyl)-1-hydroxypropyl]phenoxy}acetic acid, the hydroxy groups of which have been esterified by condensation with the carboxy group of L-pipecolic acid, the nitrogen of which has been acylated by condensation with (2S)-2-(3,4,5-trimethoxyphenyl)butyric acid. It is a synthetic, cell-permeable ligand that can be used to induce homodimerization of fusion proteins containing the DmrB domain. It has a role as a ligand. It is a N-acylpiperidine, a carboxylic ester, an aromatic ether and a tertiary amino compound.

Biological Activity

ap20187 is a small dimerizer drug [1].to solve the graft-versus-host disease, the in vivo behavior of the transplanted cells should be controlled. ap20187 is used in the conditional system as a chemical inducer of dimerization (cid). another component is a fusion protein. the cids have advantages in gene therapy, it offers the possibility of achieving selection without the toxic effects. in vivo studies show that ap20187 can produces a notable expansion of transduced red cells, platelets, and to a lesser extent, granulocytes [1].ap20187 is also reported to be used in an ap20187–lfv2ire system. in this system, ap20187 administration causes the activation of lfv2ire and results in increased uptake of both hepatic glycogen content and muscular glucose [2].

in vitro

When LNCaP cells are treated with AP20187 (B/B Homodimerizer) (100 nM), ro-iCaspase-9 levels are significantly reduced, and the smaller processed active caspase-9 becomes apparent.

< p>

in vivo

Real-time PCR analysis showed that AP20187 (B/B Homodimerizer) (0.5 mg/kg, 2 mg/kg, or 5 mg/kg) treatment significantly increased the levels of CHOP mRNA in the CNS of < i> PLP/Fv2E-PERK mice at PID12. AP20187 treatment significantly alleviates EAE-induced myelin damage in these mice. AP20187 (B/B Homodimerizer) treatment significantly reduces the number of degenerating axons and increases the density of axons in the demyelinating lesions in the lumbar spinal cord of PLP/Fv2E-PERK mice.

target

FKBP homodimerizer

storage

Store at -20°C

References

[1] neff t, blau ca. pharmacologically regulated cell therapy. blood. 2001 may 1;97(9):2535-40.
[2] cotugno g, formisano p, giacco f, colella p, beguinot f, auricchio a. ap20187-mediated activation of a chimeric insulin receptor results in insulin-like actions in skeletal muscle and liver of diabetic mice. hum gene ther. 2007 feb;18(2):106-17.

AP20187 Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from AP20187 manufacturers

Hubei Chuchang Biotech Co., Ltd.
Product
AP20187 195514-80-8
Price
US $0.00-0.00/MG
Min. Order
1MG
Purity
98
Supply Ability
100G
Release date
2024-04-17

195514-80-8, AP20187Related Search:


  • AP20187
  • AP20187;AP-20187;AP 20187
  • AP20187 (AP-20187
  • (1R,1'R)-(((((2-((dimethylamino)methyl)propane-1,3-diyl)bis(azanediyl))bis(2-oxoethane-2,1-diyl))bis(oxy))bis(3,1-phenylene))bis(3-(3,4-dimethoxyphenyl)propane-1,1-diyl) (2S,2'S)-bis(1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate)
  • B/B Homodimerizer
  • (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]methyl]-3-(dimethylamino)propyl]amino]-2-oxoethoxy]phenyl]propyl] (2S)-1-[(2S)-2-(3,4,5-trimethoxyphenyl)butanoyl]piperidine-2-carboxylate
  • (S,2S,2'S)-(1R,1'R)-(((((2-((dimethylamino)methyl)propane-1,3-diyl)bis(azanediyl))bis(2-oxoethane-2,1-diyl))bis(oxy))bis(3,1-phenylene))bis(3-(3,4-dimethoxyphenyl)propane-1,1-diyl) bis(1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate)
  • (1S,1'S)-(((2,2'-((2-((dimethylamino)methyl)propane-1,3-diyl)bis(azanediyl))bis(acetyl))bis(oxy))bis(3,1-phenylene))bis(3-(3,4-dimethoxyphenyl)propane-1,1-diyl) (2S,2'S)-bis(1-(2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate)
  • inhibit,AP 20187,AP20187,FKBP,FK506-binding protein,Inhibitor,AP-20187
  • 2-Piperidinecarboxylic acid, 1-[(2S)-1-oxo-2-(3,4,5-trimethoxyphenyl)butyl]-, 2,2'-[[2-[( dimethylamino)methyl]-1,3-propanediyl]bis[imino(2-oxo-2,1-ethanediyl)oxy-3,1-phen ylene[(1R)-3-(3,4-dimethoxyphenyl)propylidene]]] ester, (2S,2'S)-
  • (1S,1'S)-(((2,2'-((2-((dimethylamino)methyl)propane-1,3-diyl)bis(azanediyl))bis(acetyl))bis(oxy))bis(3,1-phenylene))bis(3-(3,4-dimethoxyphenyl)propane-1,1-diyl) (2S,2'S)-bis(1-(2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate)
  • (1R)-3-(3,4-dimethoxyphenyl)-1-{3-[({2-[(2-{3-[(1R)-3-(3,4-dimethoxyphenyl)-1-{1-[(2S)-2-(3,4,5-trimethoxyphenyl)butanoyl]piperidine-2-carbonyloxy}propyl]phenoxy}acetamido)methyl]-3-(dimethylamino)propyl}carbamoyl)methoxy]phenyl}propyl (2S)-1-[(2S)-2-(3,4,5-trimethoxyphenyl)butanoyl]piperidine-2-carboxylate
  • 195514-80-8
  • 195514-08-8
  • C82H107N5O20