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Cipralisant is a selective histamine H3 receptor antagonist in vivo, and an agonist in vitro (pKi: 9.9 for histamine H3 receptor; Ki: 0.47 nM for rat histamine H3 receptor). It has the potential for the treatment of attention-deficit hyperactivity disorder.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $1,970 | 8-10 weeks | |
50 mg | $2,580 | 8-10 weeks | |
100 mg | $3,400 | 8-10 weeks |
Description | Cipralisant is a selective histamine H3 receptor antagonist in vivo, and an agonist in vitro (pKi: 9.9 for histamine H3 receptor; Ki: 0.47 nM for rat histamine H3 receptor). It has the potential for the treatment of attention-deficit hyperactivity disorde |
Targets&IC50 | H3 receptor:(pki)9.9 , H3 receptor (rat):(ki)0.47 nM |
In vitro | Cipralisant acts as a full agonist at the recombinant rat histamine H3 receptor in vitro and potently inhibits forskolin-induced cAMP accumulation (EC50: 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]. |
In vivo | Cipralisant (10 mg/kg, p.o.) blocks R-α-methylhistamine (a histamine H3 receptor agonist)-induced water intake in rats [2]. |
Alias | GT-2331 |
Molecular Weight | 216.32 |
Formula | C14H20N2 |
Cas No. | 213027-19-1 |
Relative Density. | 1.03g/cm3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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