A-317920 | CAS 360551-59-3

A-317920

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Cat #: V3092 CAS #: 360551-59-3 Purity ≥ 98%

Description: A-317920, a piperazine amide, is an inverse agonist radioligand for the H3R receptor. A-317920 potently antagonize native H3Rs by blocking histamine inhibition of potassium-evoked [3H]histamine release from rat brain cortical synaptosomes (pKb values = 8.6 and 9.3) and (R)-alpha-MeHA reversal of electric field-stimulated guinea pig ileum contractions (pA2 values = 7.1 and 8.3). A-317920 is also more efficacious inverse agonists in reversing basal guanosine 5'-O-(3-[35S]thio)triphosphate ([35S]GTP gamma S) binding at the human H3R (pEC50 values = 5.7 and 7.0) than are the imidazole antagonists. These novel and selective piperazine amides represent useful leads for the development of H3R antagonist therapeutic agents.

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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	453.54
Molecular Formula	C25H31N3O5
CAS No.	360551-59-3
Storage	-20℃ for 3 years in powder form
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: 10 mM
	Water: N/A
	Ethanol: N/A
Synonyms	A317920; A 317920

Protocol	In Vitro	In vitro activity: Kinase Assay: Cell Assay:

These protocols are for reference only. InvivoChem does not independently validate these methods.

Related Biological Data

A-304121 and A-317920 block (R)-α-MeHA reversal of forskolin-stimulated cAMP formation in a concentration-dependent manner in C6 cells stably expressing the full-length human (top panel) and rat (bottom panel) histamine H3LRs. J Pharmacol Exp Ther. 2003 Jun;305(3):887-96.

A-304121 and A-317920 block histamine reversal of potassium-stimulated [3H]histamine release in a concentration-dependent manner in rat brain cortical synaptosomes. J Pharmacol Exp Ther. 2003 Jun;305(3):887-96.

A-304121 and A-317920 decrease basal [35S]GTPγS binding in a concentration-dependent manner in membranes from HEK cells stably expressing the full-length human histamine H3LR. J Pharmacol Exp Ther. 2003 Jun;305(3):887-96.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	2.2049 mL	11.0244 mL	22.0488 mL	44.0975 mL
5mM	0.4410 mL	2.2049 mL	4.4098 mL	8.8195 mL
10mM	0.2205 mL	1.1024 mL	2.2049 mL	4.4098 mL
20mM	0.1102 mL	0.5512 mL	1.1024 mL	2.2049 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

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

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

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 add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.