Revefenacin (Synonyms: TD-4208; GSK1160724)

Name: Revefenacin
Brand: MedChemExpress
SKU: HY-15851
Rating: 4.5 (1 reviews)

Cat. No.: HY-15851 Purity: 99.23%: FAQs
Data Sheet SDS COA Handling Instructions

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Revefenacin (TD-4208; GSK1160724) is a potent mAChR antagonist; has a high affinity on M3 receptor with a K_i of 0.18 nM.

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

Revefenacin Chemical Structure

CAS No. : 864750-70-9

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 132	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 132	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 100	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 180	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 320	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 480	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 680	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Biological Activity
Protocol
Purity & Documentation
References
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Description

Revefenacin (TD-4208; GSK1160724) is a potent mAChR antagonist; has a high affinity on M3 receptor with a K_i of 0.18 nM.

IC₅₀ & Target

Ki: 0.42 nM (M1), 0.32 nM (M2), 0.18 nM (M3), 0.56 nM (M4), 6.7 nM (M5)^[1]

In Vitro

The K_is of revefenacin are 0.42, 0.32, 0.18, 0.56, and 6.7 nM at human M1, M2, M3, M4 and M5 receptors, respectively. In a functional assay, revefenacin is shown to be a functional antagonist with inhibition constants similar to binding K_i's. Revefenacin also inhibits agonist-induced contraction of guinea pig isolated tracheal ring preparation with an affinity of 0.1 nM, similar to the measured M3 biding K_i^[1].

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

In Vivo

In anesthetized dogs, revefenacin, along with tiotropium and glycopyrronium, produce sustained inhibition of acetylcholine-induced bronchoconstriction for up to 24 hours. In anesthetized rats, inhaled revefenacin exhibits dose-dependent 24-hour bronchoprotection against methacholine-induced bronchoconstriction. The estimated 24-hour potency is 45.0 µg/mL and the bronchoprotective potencies are maintained after 7 days of once-daily dosing^[2].

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

Clinical Trial

Molecular Weight

597.75

Formula

C₃₅H₄₃N₅O₄

CAS No.

864750-70-9

Appearance

Solid

Color

White to off-white

SMILES

O=C(OC1CCN(CCN(C(C2=CC=C(CN3CCC(C(N)=O)CC3)C=C2)=O)C)CC1)NC4=CC=CC=C4C5=CC=CC=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (167.29 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	1.6729 mL	8.3647 mL	16.7294 mL
5 mM	0.3346 mL	1.6729 mL	3.3459 mL
10 mM	0.1673 mL	0.8365 mL	1.6729 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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

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 (4.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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 (4.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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: 99.23%

Select Batch:

Data Sheet (271 KB) SDS (0 KB)

COA (244 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. Steinfeld T, et al. In vitro characterization of TD-4208, a lung-selective and long-acting muscarinic antagonist bronchodilator (Abstract). Am J Respir Crit Care Med 179:A4553.

[2]. Pulido-Rios MT, et al. In vivo pharmacological characterization of TD-4208, a novel lung-selective inhaled muscarinic antagonist with sustained bronchoprotective effect in experimental animal models. J Pharmacol Exp Ther. 2013 Aug;346(2):241-50. [Content Brief]

Animal Administration
^[2]

Rats: To determine the bronchoprotective and antisialagogue potency after a single dose, rats are exposed by inhalation to a nebulized solution of revefenacin (3–3000 µg/mL), tiotropium (0.3–300 µg/mL), glycopyrronium (1–1000 µg/mL), or vehicle (sterile water). Bronchoprotective activity is assessed 24 hours postdose. For the antisialagogue effect, inhibition of Pilo is assessed 1, 6, or 12 hours after inhalation of an efficacious dose of test compound to determine the time point at which peak effect occurred. All subsequent doses are measured at this time point^[2].

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

References

[1]. Steinfeld T, et al. In vitro characterization of TD-4208, a lung-selective and long-acting muscarinic antagonist bronchodilator (Abstract). Am J Respir Crit Care Med 179:A4553.

[2]. Pulido-Rios MT, et al. In vivo pharmacological characterization of TD-4208, a novel lung-selective inhaled muscarinic antagonist with sustained bronchoprotective effect in experimental animal models. J Pharmacol Exp Ther. 2013 Aug;346(2):241-50. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.6729 mL	8.3647 mL	16.7294 mL	41.8235 mL
	5 mM	0.3346 mL	1.6729 mL	3.3459 mL	8.3647 mL
	10 mM	0.1673 mL	0.8365 mL	1.6729 mL	4.1824 mL
	15 mM	0.1115 mL	0.5576 mL	1.1153 mL	2.7882 mL
	20 mM	0.0836 mL	0.4182 mL	0.8365 mL	2.0912 mL
	25 mM	0.0669 mL	0.3346 mL	0.6692 mL	1.6729 mL
	30 mM	0.0558 mL	0.2788 mL	0.5576 mL	1.3941 mL
	40 mM	0.0418 mL	0.2091 mL	0.4182 mL	1.0456 mL
	50 mM	0.0335 mL	0.1673 mL	0.3346 mL	0.8365 mL
	60 mM	0.0279 mL	0.1394 mL	0.2788 mL	0.6971 mL
	80 mM	0.0209 mL	0.1046 mL	0.2091 mL	0.5228 mL
	100 mM	0.0167 mL	0.0836 mL	0.1673 mL	0.4182 mL

Revefenacin 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:

Revefenacin864750-70-9TD-4208 GSK1160724TD4208TD 4208GSK1160724GSK 1160724GSK-1160724mAChRMuscarinic acetylcholine receptorInhibitorinhibitorinhibit

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Revefenacin (Synonyms: TD-4208; GSK1160724)

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Complete Stock Solution Preparation Table

Revefenacin Related Classifications

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