Wy 49051

Cat. No.: HY-101830 Purity: 98.70%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

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	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 3148	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 587	In-stock	Estimated Time of Arrival: December 31
5 mg		Get quote
10 mg		Get quote

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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.

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.

113418-56-7

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
10 mM	0.2051 mL	1.0255 mL	2.0509 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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)

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

Purity: 98.70%

Select Batch:

Data Sheet (273 KB) SDS (251 KB)

COA (250 KB) HNMR (147 KB) RP-HPLC (170 KB) LCMS (380 KB)

Handling Instructions (2659 KB)

References

[1]. Abou-Gharbia M, et al. New antihistamines: substituted piperazine and piperidine derivatives as novel H1-antagonists. J Med Chem. 1995 Sep 29;38(20):4026-32. [Content Brief]

Complete Stock Solution Preparation Table

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

Wy 49051 Related Classifications

Inflammation/Immunology Endocrinology

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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