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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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Molecular Weight (MW) | 453.54 |
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Molecular Formula | C25H31N3O5 |
CAS No. | 360551-59-3 |
Storage | -20℃ for 3 years in powder form |
-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: |
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Solvent volume to be added | Mass (the weight of a compound) | |||
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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 |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (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.