Cipralisant (GT-2331) (Synonyms: GT-2331) |
| カタログ番号GC31269 |
Cipralisant (GT-2331) (GT-2331) は、経口活性、低毒性、強力、選択的、高親和性のヒスタミン H3 受容体のインビボ完全アンタゴニストであり、インビトロでのアゴニストであり、ヒスタミン H3 受容体の pKi は 9.9 であり、ラット ヒスタミン H3 受容体の Ki は 0.47 nM。
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Cas No.: 213027-19-1
Sample solution is provided at 25 µL, 10mM.
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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.
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].
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].
[1]. 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 Jun 26;351(3):307-11. [2]. Ito S, et al. Detailed pharmacological characterization of GT-2331 for the rat histamine H3 receptor. Eur J Pharmacol. 2006 Jan 4;529(1-3):40-6.
| Cas No. | 213027-19-1 | SDF | |
| 同義語 | GT-2331 | ||
| Canonical SMILES | CC(C)(C)CCC#C[C@H]1[C@H](C2=CN=CN2)C1 | ||
| Formula | C14H20N2 | M.Wt | 216.32 |
| 溶解度 | DMSO : 200 mg/mL (924.56 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 11 reference(s) in Google Scholar.)
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