1. GPCR/G Protein
    Immunology/Inflammation
  2. Histamine Receptor

Cipralisant (Synonyms: GT-2331)

Cat. No.: HY-106993
Handling Instructions

Cipralisant is a potent and selective histamine H3 receptor antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor; Cipralisant has entered in clinical trials for the treatment of attention-deficit hyperactivity disorder.

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

Cipralisant Chemical Structure

Cipralisant Chemical Structure

CAS No. : 213027-19-1

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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

Cipralisant is a potent and selective histamine H3 receptor antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor; Cipralisant has entered in clinical trials for the treatment of attention-deficit hyperactivity disorder.

IC50 & Target

pKi: 9.9 (Histamine H3 receptor)[1]
Ki: 0.47 nM (Rat histamine H3 receptor)[2]

In Vitro

Cipralisant (GT-2331) is a potent histamine H3 receptor antagonist with a pKi of 9.9[1] and a Ki of 0.47 nM for rat histamine H3 receptor[2]. Cipralisant acts as a full agonist at the recombinant rat histamine H3 receptor in vitro, and potently inhibits forskolin-induced cAMP accumulation with an EC50 of 0.23 nM. Cipralisant increases the basal [35S]GTPγS binding activities in membranes from HEK cells expressing the rat histamine H3 receptor (EC50, 5.6 nM)[2].

In Vivo

Cipralisant (GT-2331) acts as an antagonist of histamine H3 receptor, and blocks R-α-methylhistamine (a histamine H3 receptor agonist)-induced water intake at 10 mg/kg via oral administration in rats[2].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.6228 mL 23.1139 mL 46.2278 mL
5 mM 0.9246 mL 4.6228 mL 9.2456 mL
10 mM 0.4623 mL 2.3114 mL 4.6228 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

216.32

Formula

C₁₄H₂₀N₂

CAS No.

213027-19-1

SMILES

CC(C)(C)CCC#C[[email protected]]1[[email protected]](C2=CN=CN2)C1

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Cipralisant
Cat. No.:
HY-106993
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Cipralisant

Cat. No.: HY-106993