Revefenacin free base · Synonyms: TD-4208 | GSK1160724
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. Not for human or veterinary use.
Revefenacin structure
CAS No.: 864750-70-9
Pack sizes & pricing
| Size | Price | SKU | Stock | |
|---|---|---|---|---|
| 50 mg | USD 340.00 | BP-02090-50mg | In stock | Get quote |
| 100 mg | USD 545.00 | BP-02090-100mg | In stock | Get quote |
| 250 mg | USD 1,090.00 | BP-02090-250mg | In stock | Get quote |
| 500 mg | USD 1,740.00 | BP-02090-500mg | In stock | Get quote |
| 1 g | USD 2,785.00 | BP-02090-1g | In stock | Get quote |
| 2 g | USD 4,460.00 | BP-02090-2g | In stock | Get quote |
| 3 g | Inquire | BP-02090-3g | In stock | Inquire |
Need another size or custom synthesis? Request a quote.
Description
Revefenacin (TD-4208; GSK1160724) is a potent mAChR antagonist; has a high affinity on M3 receptor with a Ki of 0.18 nM.
Biological activity
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. 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.
Identifiers
- SMILES
-
CN(CCN1CCC(CC1)OC(=O)NC1=CC=CC=C1C1=CC=CC=C1)C(=O)C1=CC=C(CN2CCC(CC2)C(N)=O)C=C1 - InChIKey
-
FYDWDCIFZSGNBU-UHFFFAOYSA-N
Specifications
- MW (average)
- 597.7470
- Formula
- C35H43N5O4
- CAS No.
- 864750-70-9
- Physical state
- Solid
- Color
- white to off-white
- Shipping
- Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
- Storage
- Powder -20℃ 2 years; In solvent -20℃ 1 month;
Solubility
Soluble in DMSO