| Size | Price | Stock | Qty |
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| 1mg |
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| Targets |
Cipralisant targets the histamine H3 receptor, a G protein-coupled receptor that modulates the release of histamine and other neurotransmitters in the central nervous system. It acts as a high-affinity ligand with a pKi of 9.9 and a Ki of 0.47 nM. The compound displays functional selectivity, acting as a full antagonist in vivo and an agonist in vitro. This protean behavior makes it a valuable tool for studying H3 receptor pharmacology.
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| ln Vitro |
Cipralisant is a complete agonist for adenylyl cyclase inhibition. Cipralisant (HEK cells) suppresses forskolin-induced cAMP accumulation, showing that it is a strong complete histamine H3 receptor agonist. Cipralisant enhances basal [35S]GTPγS binding activity (EC50, 5.6 nM) in HEK cells expressing rat histamine H3 receptors [3].
In vitro, Cipralisant acts as a potent full agonist at the histamine H3 receptor. In HEK cells, it potently inhibits forskolin-induced cAMP accumulation, demonstrating its agonist activity. It exhibits high affinity and selectivity for the H3 receptor, with a Ki of 0.47 nM for the rat H3 receptor. Its in vitro agonist profile contrasts with its in vivo antagonist activity, highlighting its protean nature. |
| ln Vivo |
In five trials, cipraisant (0.3 to 30 mg/kg; subcutaneous injection) improved collection; at 1 mg/kg, it became significant [2]. Alcohol consumption produced by R-alpha-methylhistamine is totally blocked by Cipralisant (10 mg/kg; oral) [3]. In rats, cipralisant increases wakefulness. Cipralisant's strong affinity for rat H3 receptors and strong CNS penetration are consistent with its ability to effectively and dramatically increase performance in repeated acquisition models. Cipralisant seems to be less efficacious than 3 mg/kg ciproxifene at the maximal effective dose [2]. In a rat brain synaptosome model, cipralisant functions as a partial agonist [3].
In vivo, Cipralisant acts as an orally active, low-toxicity, potent, and selective histamine H3 receptor full antagonist. It potently and significantly improves performance in the repeated acquisition model, consistent with its high affinity for the H3 receptor. This suggests potential for treating cognitive disorders. Its oral activity and low toxicity profile make it a promising candidate for further development in ADHD and other central nervous system disorders. |
| Enzyme Assay |
For in vitro enzyme/receptor binding assays, Cipralisant can be evaluated using radioligand binding studies with membranes expressing the histamine H3 receptor. Competition binding experiments using a labeled H3 receptor ligand, such as [3H]-Nalpha-methylhistamine, can determine the compound's affinity (Ki) for the receptor. Functional assays, such as measuring inhibition of forskolin-induced cAMP accumulation in HEK cells expressing the H3 receptor, can assess agonist or antagonist activity. Dose-response curves are generated to determine EC₅0 or IC₅0 values.
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| Cell Assay |
For in vitro cellular experiments, Cipralisant is typically tested in cell lines expressing the histamine H3 receptor, such as HEK293 cells stably transfected with the receptor. Cells are cultured in appropriate media and treated with various concentrations of the compound. Receptor activation is measured by assessing inhibition of forskolin-induced cAMP accumulation. The compound's effects on downstream signaling pathways and receptor internalization can be further investigated.
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| Animal Protocol |
Animal/Disease Models: Male SHR puppies (35–50 g) [2]
Doses: 0.3~30 mg/kg Route of Administration: subcutaneous injection Experimental Results: At the dose of 1 mg/kg, the performance of SHR puppies was Dramatically enhanced and was consistent with Dose related. Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat [3] Doses: 10 and 30 mg/kg Route of Administration: Oral Experimental Results: Greater brain exposure was achieved, monitor water intake for 60 minutes after dosing. For in vivo animal experiments, Cipralisant can be administered to rodents via oral gavage, taking advantage of its oral bioavailability. The compound's effects on cognition and behavior can be evaluated in models of attention and learning, such as the repeated acquisition model. Typical doses may range from 0.1 to 10 mg/kg. Performance in cognitive tasks, locomotor activity, and other behavioral parameters are assessed. Pharmacodynamic markers, such as histamine levels, can also be measured. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Cipralisant include oral activity and low toxicity, supporting its use in oral administration studies. As a small molecule with a molecular weight of 216.32, it is likely to have good oral bioavailability and tissue distribution, including brain penetration. Detailed parameters such as Cₘₐₓ, Tₘₐₓ, AUC, half-life, and clearance would need to be determined through comprehensive PK studies. The compound's metabolism and excretion pathways remain to be fully characterized.
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| Toxicity/Toxicokinetics |
Toxicological data for Cipralisant indicate it has low toxicity. As an H3 receptor ligand, its toxicity would depend on the importance of H3 receptor signaling for normal neurological function. Comprehensive toxicology studies including acute and repeated-dose toxicity, genotoxicity, and cardiotoxicity assessments would be needed for further development. Appropriate safety precautions should be taken when handling this compound.
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| References |
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| Additional Infomation |
Cipralisant is a research compound used to study histamine H3 receptor biology. No clinical trials or regulatory approvals have been reported for this compound as a therapeutic agent. It is available from various chemical suppliers for research purposes only. The compound has potential for ADHD research. It is also a click chemistry reagent, containing an alkyne group.
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| Molecular Formula |
C14H20N2
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| Molecular Weight |
216.322
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| Exact Mass |
216.163
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| CAS # |
213027-19-1
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| Related CAS # |
Cipralisant maleate;223420-20-0;Cipralisant (enantiomer);223420-11-9
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| PubChem CID |
6450823
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| Appearance |
White to off-white solid powder
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| Density |
1.03g/cm3
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| Boiling Point |
386.7ºC at 760 mmHg
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| Flash Point |
188.5ºC
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| Vapour Pressure |
7.72E-06mmHg at 25°C
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| Index of Refraction |
1.536
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| LogP |
3.342
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
16
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| Complexity |
302
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC(C)(C)CCC#C[C@@H]1C[C@H]1C2=CN=CN2
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| InChi Key |
CVKJAXCQPFOAIN-VXGBXAGGSA-N
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| InChi Code |
InChI=1S/C14H20N2/c1-14(2,3)7-5-4-6-11-8-12(11)13-9-15-10-16-13/h9-12H,5,7-8H2,1-3H3,(H,15,16)/t11-,12-/m1/s1
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| Chemical Name |
5-[(1R,2R)-2-(5,5-dimethylhex-1-ynyl)cyclopropyl]-1H-imidazole
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~200 mg/mL (~924.56 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(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.
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