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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.84%
- CAS 番号: 223420-20-0
- 分子式: C18H24N2O4
- 分子量:332.39
-
保管条件: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]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
Histamine Receptor アイソフォーム固有の製品をすべて表示
More
生物活性
|
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.
-
Animal Model:Male SHR pups (35–50 g)[2]
-
Dosage:0.3~30 mg/kg
-
Administration:S.c.
-
Result:Significantly enhanced performance of the SHR pups in a dose-related manner at 1 mg/kg.
-
Animal Model:Male Sprague-Dawley rats[3]
-
Dosage:10 and 30 mg/kg
-
Administration:P.o.
-
Result:Achieved greater brain exposure and water intake was monitored for 60 min after administration.
化学情報
-
CAS 番号 223420-20-0
-
性状 Solid
-
分子量 332.39
-
分子式 C18H24N2O4
-
Color White to off-white
-
SMILES
O=C(O)/C=C\C(O)=O.CC(C)(C)CCC#C[C@H]1[C@H](C2=CN=CN2)C1
-
別名
GT-2331 maleate
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
-
データシート (276 KB)
-
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)
-
取扱説明書 (2659 KB)
参考文献
[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 |
|---|---|---|---|---|---|
| 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 関連分類
HY-106993A 関連分類
Powered by Bioz