Cipralisant maleate
Based on 1 Customer Validation
Cipralisant (GT-2331) (maleate) is an orally active, low-toxicity, potent, selective, high affinity histamine H3 receptor full 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 (maleate) has the potential for attention-deficit hyperactivity disorder research. Cipralisant (maleate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
For research use only. We do not sell to patients.
- Purity: 99.84%
- CAS No.: 223420-20-0
- Formula: C18H24N2O4
- Molecular Weight:332.39
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
All Histamine Receptor Isoforms
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Biological Activity
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H3 receptor 9.9 (pKi) |
rat H3 receptor 0.47 nM (Ki) |
Cipralisant (maleate) behaves as a full agonist on adenylyl cyclase inhibition. Cipralisant (maleate) (HEK cells) potently inhibits forskolin-induced cAMP accumulation, showing that Cipralisant (maleate) works as a potent full histamine H3 receptor agonist. Cipralisant (maleate) increases the basal [35S]GTPγS binding activities in membranes from HEK cells expressing the rat histamine H3 receptor (EC50, 5.6 nM)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cipralisant (maleate) (10 mg/kg; p.o.) completely blocks R-α-methylhistamine-induced drinking[3].
Cipralisant (maleate) promotes wakefulness in the rat. Cipralisant (maleate) potently and significantly improves performance in the repeated acquisition model, in line with its high affinity for the rat H3 receptor and good CNS penetration. Cipralisant (maleate) does not appear to be as efficacious as 3 mg/kg ciproxifan at its maximally effective dose [2]. Cipralisant (maleate) behaves as a partial agonist in a rat brain synaptosome model[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male SHR pups (35–50 g)[2]
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Dosage:0.3~30 mg/kg
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Administration:S.c.
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Result:Significantly enhanced performance of the SHR pups in a dose-related manner at 1 mg/kg.
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Animal Model:Male Sprague-Dawley rats[3]
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Dosage:10 and 30 mg/kg
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Administration:P.o.
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Result:Achieved greater brain exposure and water intake was monitored for 60 min after administration.
Chemical Information
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CAS No. 223420-20-0
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Appearance Solid
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Molecular Weight 332.39
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Formula C18H24N2O4
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Color White to off-white
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SMILES
O=C(O)/C=C\C(O)=O.CC(C)(C)CCC#C[C@H]1[C@H](C2=CN=CN2)C1
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Synonyms
GT-2331 maleate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : ≥ 100 mg/mL (300.85 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Raddatz R, et al. Histamine H3 antagonists for treatment of cognitive deficits in CNS diseases. Curr Top Med Chem. 2010;10(2):153-169. [Content Brief]
[2]. Fox GB, et al. Effects of histamine H(3) receptor ligands GT-2331 and ciproxifan in a repeated acquisition avoidance response in the spontaneously hypertensive rat pup. Behav Brain Res. 2002;131(1-2):151-161. [Content Brief]
[3]. Ito S, et al. Detailed pharmacological characterization of GT-2331 for the rat histamine H3 receptor. Eur J Pharmacol. 2006;529(1-3):40-46. [Content Brief]
[4]. Tedford CE, et al. High antagonist potency of GT-2227 and GT-2331, new histamine H3 receptor antagonists, in two functional models. Eur J Pharmacol. 1998;351(3):307-311. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 3.0085 mL | 15.0426 mL | 30.0851 mL | 75.2128 mL |
| 5 mM | 0.6017 mL | 3.0085 mL | 6.0170 mL | 15.0426 mL | |
| 10 mM | 0.3009 mL | 1.5043 mL | 3.0085 mL | 7.5213 mL | |
| 15 mM | 0.2006 mL | 1.0028 mL | 2.0057 mL | 5.0142 mL | |
| 20 mM | 0.1504 mL | 0.7521 mL | 1.5043 mL | 3.7606 mL | |
| 25 mM | 0.1203 mL | 0.6017 mL | 1.2034 mL | 3.0085 mL | |
| 30 mM | 0.1003 mL | 0.5014 mL | 1.0028 mL | 2.5071 mL | |
| 40 mM | 0.0752 mL | 0.3761 mL | 0.7521 mL | 1.8803 mL | |
| 50 mM | 0.0602 mL | 0.3009 mL | 0.6017 mL | 1.5043 mL | |
| 60 mM | 0.0501 mL | 0.2507 mL | 0.5014 mL | 1.2535 mL | |
| 80 mM | 0.0376 mL | 0.1880 mL | 0.3761 mL | 0.9402 mL | |
| 100 mM | 0.0301 mL | 0.1504 mL | 0.3009 mL | 0.7521 mL |
Cipralisant maleate Related Classifications
HY-106993A Related Classifications
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