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)
color: White to yellow

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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.

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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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AP20187 Suppliers

China 88 United States 10 Global 98

Haoyuan Chemexpress Co., Ltd.

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MedChemexpress LLC

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SPIRO PHARMA

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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