A-304121 | CAS 360551-71-9

A-304121

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Cat #: V3086 CAS #: 360551-71-9 Purity ≥ 98%

Description: A-304121, a piperazine amide, is a potent H3R antagonist. A-304121 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-304121 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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Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	359.47
Molecular Formula	C20H29N3O3
CAS No.	360551-71-9
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	A-304121; A 304121

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	2.7819 mL	13.9094 mL	27.8187 mL	55.6375 mL
5mM	0.5564 mL	2.7819 mL	5.5637 mL	11.1275 mL
10mM	0.2782 mL	1.3909 mL	2.7819 mL	5.5637 mL
20mM	0.1391 mL	0.6955 mL	1.3909 mL	2.7819 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.