1. GPCR/G Protein
    Neuronal Signaling
  2. mAChR
  3. Revefenacin

Revefenacin (Synonyms: TD-4208; GSK1160724)

Cat. No.: HY-15851 Purity: 99.78%
Handling Instructions

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

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

Revefenacin Chemical Structure

Revefenacin Chemical Structure

CAS No. : 864750-70-9

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10 mM * 1  mL in DMSO USD 252 In-stock
Estimated Time of Arrival: December 31
2 mg USD 120 In-stock
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5 mg USD 192 In-stock
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10 mg USD 312 In-stock
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50 mg USD 1020 In-stock
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100 mg USD 1920 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Revefenacin (TD-4208; GSK1160724) is a potent mAChR antagonist; has a high affinity on M3 receptor with a Ki 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 Kis 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 Ki'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 Ki[1].

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].

Clinical Trial
Molecular Weight

597.75

Formula

C₃₅H₄₃N₅O₄

CAS No.

864750-70-9

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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 125 mg/mL (209.12 mM)

*"≥" means soluble, but saturation unknown.

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
*Please refer to the solubility information to select the appropriate solvent.
References
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
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Keywords:

RevefenacinTD-4208GSK1160724TD4208TD 4208GSK 1160724GSK-1160724mAChRMuscarinic acetylcholine receptorInhibitorinhibitorinhibit

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Product name:
Revefenacin
Cat. No.:
HY-15851
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