871814-52-7
Chemical Structure
Libvatrep
Synonym(s): SAF312; Vanilloid receptor antagonist 1
- CAS No.: 871814-52-7
- Formula:C18H15N3O2
- Molecular Weight:305.33
IUPAC Name: 4-(7-hydroxy-2-isopropyl-4-oxoquinazolin-3(4H)-yl)benzonitrile
InChIKey: JFPXRFIBKKSHGY-UHFFFAOYSA-N
SMILES: N#CC1=CC=C(N2C(C(C)C)=NC3=C(C=CC(O)=C3)C2=O)C=C1
Biological Activity: Libvatrep (SAF312) is a non-competitive TRPV1 antagonist with an IC50 of 0.35-0.69 µM in HEK293T cells. It binds to the vanilloid pocket and an allosteric site, preventing S4/S5 conformational changes and channel opening. Libvatrep can be used for research on ocular surface pain and eye pain after photorefractive keratectomy[1][2][3][4].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Libvatrep | 99.54% | Libvatrep (SAF312) is a non-competitive TRPV1 antagonist with an IC50 of 0.35-0.69 µM in HEK293T cells. It binds to the vanilloid pocket and an allosteric site, preventing S4/S5 conformational changes and channel opening. Libvatrep can be used for research on ocular surface pain and eye pain after photorefractive keratectomy. | ||||||||||||||||||||
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References
- [1]. Fan J, et al. Structural basis of TRPV1 inhibition by SAF312 and cholesterol. Nature communications. 2024 Aug 06;15(1):6689. [Content Brief]
- [2]. Thompson V, et al. Topical ocular TRPV1 antagonist SAF312 (Libvatrep) for postoperative pain after photorefractive keratectomy. Translational Vision Science & Technology. 2023 Mar 1;12(3):7-.
- [3]. Mogi M, et al. Ocular Pharmacology and Toxicology of TRPV1 Antagonist SAF312 (Libvatrep). Translational vision science & technology. 2023 Sep 01;12(9):5.
- [4]. CHEN W, et al. Quinazolinone derivatives useful as vanilloid antagonists: US8349852B2. 2013‑01‑08.