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

Cipralisant  (Synonyms: GT-2331)

Art. -Nr.: HY-106993 Reinheit: 99.26% ee.: 100%
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Cipralisant (GT-2331) 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 has the potential for attention-deficit hyperactivity disorder research. Cipralisant is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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Cipralisant

Cipralisant Chemische Struktur

CAS. Nr. : 213027-19-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Other Forms of Cipralisant:

Cipralisant Related Antibodies

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Alle Histamine Receptor Isoform-spezifische Produkte anzeigen:

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H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

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Beschreibung

Cipralisant (GT-2331) 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 has the potential for attention-deficit hyperactivity disorder research[1][2][3][4]. Cipralisant 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 behaves as a full agonist on adenylyl cyclase inhibition. Cipralisant (HEK cells) potently inhibits forskolin-induced cAMP accumulation, showing that Cipralisant works as a potent full histamine H3 receptor agonist. Cipralisant 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 Related Antibodies
In Vivo

Cipralisant (0.3~30 mg/kg; s.c.) enhances acquisition over five trials, reaching significance at 1 mg/kg[2].
Cipralisant (10 mg/kg; p.o.) completely blocks R-α-methylhistamine-induced drinking[3].
Cipralisant promotes wakefulness in the rat. Cipralisant 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 does not appear to be as efficacious as 3 mg/kg ciproxifan at its maximally effective dose [2]. Cipralisant 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.
Molekulargewicht

216.32

Formel

C14H20N2
CAS. Nr.
Appearance

Solid

Color

White to off-white

SMILES

CC(C)(C)CCC#C[C@H]1[C@H](C2=CN=CN2)C1
Versand

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

DMSO : 200 mg/mL (924.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
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.

  • Molaritätsrechner

  • Verdünnungsrechner

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

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

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 4.6228 mL 23.1139 mL 46.2278 mL 115.5695 mL
5 mM 0.9246 mL 4.6228 mL 9.2456 mL 23.1139 mL
10 mM 0.4623 mL 2.3114 mL 4.6228 mL 11.5570 mL
15 mM 0.3082 mL 1.5409 mL 3.0819 mL 7.7046 mL
20 mM 0.2311 mL 1.1557 mL 2.3114 mL 5.7785 mL
25 mM 0.1849 mL 0.9246 mL 1.8491 mL 4.6228 mL
30 mM 0.1541 mL 0.7705 mL 1.5409 mL 3.8523 mL
40 mM 0.1156 mL 0.5778 mL 1.1557 mL 2.8892 mL
50 mM 0.0925 mL 0.4623 mL 0.9246 mL 2.3114 mL
60 mM 0.0770 mL 0.3852 mL 0.7705 mL 1.9262 mL
80 mM 0.0578 mL 0.2889 mL 0.5778 mL 1.4446 mL
100 mM 0.0462 mL 0.2311 mL 0.4623 mL 1.1557 mL
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Cipralisant 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:

Cipralisant213027-19-1GT-2331GT2331GT 2331Histamine Receptororallyactivelow-toxicitypotentselectiveaffinityattention-deficithyperactivityInhibitorinhibitorinhibit

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