2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor
  4. Wy 49051

Wy 49051 is a potent, orally active H1 receptor antagonist, with IC50 of 44 nM.

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

Wy 49051 Chemical Structure

Wy 49051 Chemical Structure

CAS No. : 113418-56-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 3148 In-stock
Solution
10 mM * 1 mL in DMSO USD 3148 In-stock
Solid
1 mg USD 587 In-stock
5 mg   Get quote  
10 mg   Get quote  

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Wy 49051 Related Antibodies

Top Publications Citing Use of Products

View All Histamine Receptor Isoform Specific Products:

View All Isoforms
H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Wy 49051 is a potent, orally active H1 receptor antagonist, with IC50 of 44 nM.

IC50 & Target

IC50: 44 nM (H1 receptor)[1]
In Vitro

Wy 49051 shows great inhibitory effect on H1, producing 92% inhibition of the histamine-induced contraction of the guinea pig ileum at a concentration 100 nM. Wy 49051 is the most potent compound with 700 times the potency of astemazole, 470 times the potency of chlorpheniramine. Wy 49051 also has high affinity for α1 receptor with IC50 of 8 nM[1].

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

Wy 49051 Related Antibodies
In Vivo

Wy 49051 shows potent activity against histamine-induced lethality in the guinea pig, with ED50 of 1.91 mg/kg by po, 0.70 mg/kg by ip, and 0.01 mg/kg by iv. The duration of action of 24 is also favorable since there is no decrease in oral efficacy up to 18 h posttreatment[1].

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

487.59

Formula

C28H33N5O3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(N1C)N(C)C2=C(N(CCCN3CCC(OC(C4=CC=CC=C4)C5=CC=CC=C5)CC3)C=N2)C1=O
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 : 50 mg/mL (102.55 mM; ultrasonic and warming and heat to 60°C; 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 2.0509 mL 10.2545 mL 20.5090 mL
5 mM 0.4102 mL 2.0509 mL 4.1018 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
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Volume
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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: ≥ 5 mg/mL (10.25 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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% Corn Oil

    Solubility: ≥ 5 mg/mL (10.25 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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 2.0509 mL 10.2545 mL 20.5090 mL 51.2726 mL
5 mM 0.4102 mL 2.0509 mL 4.1018 mL 10.2545 mL
10 mM 0.2051 mL 1.0255 mL 2.0509 mL 5.1273 mL
15 mM 0.1367 mL 0.6836 mL 1.3673 mL 3.4182 mL
20 mM 0.1025 mL 0.5127 mL 1.0255 mL 2.5636 mL
25 mM 0.0820 mL 0.4102 mL 0.8204 mL 2.0509 mL
30 mM 0.0684 mL 0.3418 mL 0.6836 mL 1.7091 mL
40 mM 0.0513 mL 0.2564 mL 0.5127 mL 1.2818 mL
50 mM 0.0410 mL 0.2051 mL 0.4102 mL 1.0255 mL
60 mM 0.0342 mL 0.1709 mL 0.3418 mL 0.8545 mL
80 mM 0.0256 mL 0.1282 mL 0.2564 mL 0.6409 mL
100 mM 0.0205 mL 0.1025 mL 0.2051 mL 0.5127 mL
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Wy 49051 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:

Wy 49051113418-56-7Wy49051Wy-49051Histamine ReceptorInhibitorinhibitorinhibit

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