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AP20187

Name: AP20187
Brand: Selleck Chemicals
SKU: S8487
Rating: 5 (1 reviews)

Synonyms: B/B Homodimerizer

Catalog No.S8487 Purity: 99.98%

AP20187 (B/B Homodimerizer) is a chemical inducer of dimerization that activates FKBP-Casp8.

AP20187 Chemical Structure

CAS: 195514-80-8

Selleck's AP20187 has been cited by 1 publication

Purity & Quality Control

Batch: S848701 DMSO] 100 mg/mL] false] Ethanol] 100 mg/mL] false] Water] Insoluble] false Purity: 99.98%

99.98

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Biological Activity

Description

AP20187 (B/B Homodimerizer) is a chemical inducer of dimerization that activates FKBP-Casp8.

Targets

FKBP ^[1]	Casp8 ^[1]

In vitro
In vitro	In oligodendrocytes, AP20187 treatment increases the expression of PERK-responsive genes encoding CAATT enhancer binding protein homologous protein (CHOP) and growth arrest and DNA damage 34 (GADD34) in a dose-dependent manner. The activity of PERK signaling in oligodendrocytes can be temporally manipulated by the administration of AP20187.^[2]
Cell Research	Cell lines	Oligodendrocytes
	Concentrations	1 nM
	Incubation Time	4 h
	Method	After 3 d of differentiation, the cells are treated with 1 nM AP20187 or vehicle for 4 h and are then fixed with cold 4% paraformaldehyde in PBS. The cells are blocked with PBS containing 10% goat serum and 0.1% Triton X-100 and incubate overnight with the primary antibody diluted in blocking solution. Appropriate fluorochrome-labeled secondary antibodies are used for detection.

In Vivo
In vivo	AP20187 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. AP20187 is also sufficient to activate Fv2E-PERK in oligodendrocytes in the CNS of PLP/Fv2E-PERK mice.^[2]
Animal Research	Animal Models	PLP/Fv2E-PERK mice
	Dosages	0.5 mg/kg, 2 mg/kg, 5 mg/kg
	Administration	i.p.

References

Chemical lnformation & Solubility

Molecular Weight	1482.75	Formula	C₈₂H₁₀₇N₅O₂₀
CAS No.	195514-80-8	SDF	--
Smiles	CCC(C1=CC(=C(C(=C1)OC)OC)OC)C(=O)N2CCCCC2C(=O)OC(CCC3=CC(=C(C=C3)OC)OC)C4=CC(=CC=C4)OCC(=O)NCC(CNC(=O)COC5=CC=CC(=C5)C(CCC6=CC(=C(C=C6)OC)OC)OC(=O)C7CCCCN7C(=O)C(CC)C8=CC(=C(C(=C8)OC)OC)OC)CN(C)C
Storage (From the date of receipt)	3 years -20°C powder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (67.44 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.					In vivo Formulation Calculator
	Clear solution	5%Ethanol 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.0mg/ml (3.37mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified Ethanol stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.	In vivo Formulation Calculator
	5% DMSO 1 95% Corn oil	5.0mg/ml (3.37mM)
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.0mg/ml (3.37mM)

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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