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

Enerisant is a potent, highly selective, competitive and orally active histamine H3 receptor antagonist/inverse agonist with IC50s of 2.89 nM and 14.5 nM against human and rat histamine H3 receptors, respectively.

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

Enerisant Chemical Structure

Enerisant Chemical Structure

CAS No. : 1152747-82-4

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 242 In-stock
Solution
10 mM * 1 mL in DMSO USD 242 In-stock
Solid
1 mg USD 125 In-stock
5 mg USD 276 In-stock
10 mg USD 442 In-stock
25 mg USD 929 In-stock
50 mg USD 1487 In-stock
100 mg USD 2380 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Enerisant:

Enerisant Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Enerisant is a potent, highly selective, competitive and orally active histamine H3 receptor antagonist/inverse agonist with IC50s of 2.89 nM and 14.5 nM against human and rat histamine H3 receptors, respectively[1].

IC50 & Target

IC50: 2.89 nM (human histamine H3 receptor), 14.5 nM (rat histamine H3 receptor)
Ki: 1.65 nM (human histamine H3 receptor), 7.87 nM (rat histamine H3 receptor)[1]
In Vivo

Enerisant hydrochloride (0.3-1 mg/kg; p.o.; once) attenuats the dipsogenia response in rats[1].
Enerisant hydrochloride (0.1-3 mg/kg; p.o.; once) results in the occupancy of the histamine H3 receptor in a dose-dependent manner in rats. A dose eliciting a half-maximal receptor occupancy is 0.78 mg/kg[1].
Enerisant hydrochloride (1 mg/kg; s.c.; once) increases the total extracellular histamine levels in the posterior hypothalamus in rats[1].
Enerisant hydrochloride (1 mg/kg; i.p.; once) increases the total extracellular dopamine and acetylcholine levels in the medial prefrontal cortex (mPFC) in rats[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male SD rats, R-α-methylhistamine-induced dipsogenia model[1]
Dosage: 0.1, 0.3 and 1 mg/kg
Administration: Oral, single dose
Result: Attenuated the dipsogenia response, reaching statistical significance at doses of 0.3 mg/kg and 1 mg/kg.
Clinical Trial
Molecular Weight

398.50

Formula

C22H30N4O3
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=CN(C2=CC=C(OCCCN3[C@H](C)CCC3)C=C2)N=C1)N4CCOCC4
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 (250.94 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 2.5094 mL 12.5471 mL 25.0941 mL
5 mM 0.5019 mL 2.5094 mL 5.0188 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.

  • Molarity Calculator

  • Dilution Calculator

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:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (6.27 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (6.27 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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 2.5094 mL 12.5471 mL 25.0941 mL 62.7353 mL
5 mM 0.5019 mL 2.5094 mL 5.0188 mL 12.5471 mL
10 mM 0.2509 mL 1.2547 mL 2.5094 mL 6.2735 mL
15 mM 0.1673 mL 0.8365 mL 1.6729 mL 4.1824 mL
20 mM 0.1255 mL 0.6274 mL 1.2547 mL 3.1368 mL
25 mM 0.1004 mL 0.5019 mL 1.0038 mL 2.5094 mL
30 mM 0.0836 mL 0.4182 mL 0.8365 mL 2.0912 mL
40 mM 0.0627 mL 0.3137 mL 0.6274 mL 1.5684 mL
50 mM 0.0502 mL 0.2509 mL 0.5019 mL 1.2547 mL
60 mM 0.0418 mL 0.2091 mL 0.4182 mL 1.0456 mL
80 mM 0.0314 mL 0.1568 mL 0.3137 mL 0.7842 mL
100 mM 0.0251 mL 0.1255 mL 0.2509 mL 0.6274 mL
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Enerisant 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:

Enerisant1152747-82-4TS-091TS091TS 091Histamine Receptororally activedipsogeniaposterior hypothalamusdopamineSD ratsInhibitorinhibitorinhibit

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