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1mg |
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5mg |
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Other Sizes |
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ln Vitro |
Maleate, or cipralate, functions as a complete agonist to block adenylyl cyclase. The forskolin-induced cAMP buildup is potently inhibited by Cipralisant (maleate) in HEK cells, suggesting that Cipralisant (maleate) functions as a strong complete histamine H3 receptor agonist. The basal [35S]GTPγS binding activity (EC50, 5.6 nM) on the membrane of HEK cells expressing rat histamine H3 receptors is increased by Cipralisant (maleate) [3].
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ln Vivo |
In five trials, Cipralisant (maleate) (0.3 to 30 mg/kg; subcutaneous injection) improved collection; at 1 mg/kg, it became significant [2]. Oral Cipralisant (maleate) at a dose of 10 mg/kg totally prevents alcohol consumption induced by R-alpha-methylhistamine [3]. Maleate, or cipralate, increases waking in rats. Cipralisant (maleate), which has a high affinity for rat H3 receptors and strong CNS penetration, efficiently and significantly enhances performance in the repeated acquisition model. At the highest effective dosage, ciproxifene 3 mg/kg seems to be more effective than cipralisant (maleate) [2]. In a rat brain synaptosome model, diprolisant (maleate) functions as a partial agonist [3].
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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. |
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.
[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. [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. [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. |
Molecular Formula |
C14H20N2.C4H4O4
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Molecular Weight |
332.39416
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CAS # |
223420-20-0
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Related CAS # |
Cipralisant;213027-19-1;Cipralisant (enantiomer);223420-11-9
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SMILES |
C(O)(=O)/C=C/C(O)=O.CC(C)(C)CCC#CC1CC1C1NC=NC=1
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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 : ≥ 100 mg/mL (~300.85 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 | 3.0085 mL | 15.0426 mL | 30.0851 mL | |
5 mM | 0.6017 mL | 3.0085 mL | 6.0170 mL | |
10 mM | 0.3009 mL | 1.5043 mL | 3.0085 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.