[CAS NO. 195514-80-8]  AP20187

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PRODUCTS SPECIFICATIONS [195514-80-8]

Catalog
HY-13992
Brand
MCE
CAS
195514-80-8

DESCRIPTION [195514-80-8]

Overview

MDL-
Molecular Weight1482.75
Molecular FormulaC82H107N5O20
SMILESCOC1=C(OC)C=C(CC[C@H](C2=CC=CC(OCC(NCC(CN(C)C)CNC(COC3=CC=CC([C@H](OC([C@H]4N(C([C@@H](CC)C5=CC(OC)=C(OC)C(OC)=C5)=O)CCCC4)=O)CCC6=CC(OC)=C(OC)C=C6)=C3)=O)=O)=C2)OC([C@@H]7CCCCN7C([C@H](C8=CC(OC)=C(OC)C(OC)=C8)CC)=O)=O)C=C1

For research use only. We do not sell to patients.


Summary

AP20187 (B/B Homodimerizer) is a cell-permeable ligand used to dimerize FK506-binding protein ( FKBP ) fusion proteins and initiate biological signaling cascades and gene expression or disrupt protein-protein interactions.


IC50 & Target

FKBP homodimerizer [1]


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 [2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


In Vivo

Real-time PCR analysis shows that AP20187 (B/B Homodimerizer) (0.5 mg/kg, 2 mg/kg, or 5 mg/kg) treatment significantly increases the levels of CHOP mRNA in the CNS of 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 [2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

Ethanol : 150 mg/mL ( 101.16 mM ; Need ultrasonic)

DMSO : ≥ 57 mg/mL ( 38.44 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.6744 mL 3.3721 mL 6.7442 mL
5 mM 0.1349 mL 0.6744 mL 1.3488 mL
10 mM 0.0674 mL 0.3372 mL 0.6744 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% EtOH >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: 6 mg/mL (4.05 mM); Clear solution; Need ultrasonic

  • 2.

    Add each solvent one by one: 10% EtOH >> 90% (20% SBE-β-CD in saline)

    Solubility: 6 mg/mL (4.05 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.5 mg/mL (1.69 mM); Clear solution

  • 4.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.5 mg/mL (1.69 mM); Clear solution

  • 5.

    Add each solvent one by one: 4% ethanol >> 10% PEG-400 >> 2% Tween-80 >> 84%water.

    Solubility: 2.4 mg/mL (1.62 mM); Clear solution; Need ultrasonic

* All of the co-solvents are available by MCE.


Synonyms

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-phenylene[(1R)-3-(3,4-dimethoxyphenyl)propylidene]]] ester, (2S,2′S)-
2-Piperidinecarboxylic acid, 1-[1-oxo-2-(3,4,5-trimethoxyphenyl)butyl]-, [2-[(dimethylamino)methyl]-1,3-propanediyl]bis[imino(2-oxo-2,1-ethanediyl)oxy-3,1-phenylene[3-(3,4-dimethoxyphenyl)propylidene]] ester, [2S-[1(R*),2R*[S*[S*[1(R*),2R*]]]]]-
2-Piperidinecarboxylic acid, 1-[(2S)-1-oxo-2-(3,4,5-trimethoxyphenyl)butyl]-, [2-[(dimethylamino)methyl]-1,3-propanediyl]bis[imino(2-oxo-2,1-ethanediyl)oxy-3,1-phenylene[(1R)-3-(3,4-dimethoxyphenyl)propylidene]] ester, (2S,2′S)-
2,2′-[[2-[(Dimethylamino)methyl]-1,3-propanediyl]bis[imino(2-oxo-2,1-ethanediyl)oxy-3,1-phenylene[(1R)-3-(3,4-dimethoxyphenyl)propylidene]]] bis[1-[(2S)-1-oxo-2-(3,4,5-trimethoxyphenyl)butyl]-2-piperidinecarboxylate]
AP 20187