2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor
  4. Cipralisant maleate

Cipralisant maleate  (Synonyms: GT-2331 maleate)

Cat. No.: HY-106993A Purity: 99.84%
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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.

For research use only. We do not sell to patients.

Cipralisant maleate Chemical Structure

Cipralisant maleate Chemical Structure

CAS No. : 223420-20-0

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Based on 1 publication(s) in Google Scholar

Other Forms of Cipralisant maleate:

Cipralisant maleate Related Antibodies

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Description

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[1][2][3][4]. 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.

IC50 & Target[3][4]

H3 receptor

9.9 (pKi)

rat H3 receptor

0.47 nM (Ki)

In Vitro

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 Related Antibodies
In Vivo

Cipralisant (maleate) (0.3~30 mg/kg; s.c.) enhances acquisition over five trials, reaching significance at 1 mg/kg[2].
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.
Molecular Weight

332.39

Formula

C18H24N2O4
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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
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Cipralisant maleate Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Cipralisant223420-20-0GT-2331GT2331GT 2331Histamine Receptororallyactivelow-toxicitypotentselectiveaffinityattention-deficithyperactivityInhibitorinhibitorinhibit

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