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Larixyl acetate

MCE China：Larixyl acetate

Brand：MedChemExpress (MCE)

Cat. No.HY-101795

CAS：4608-49-5

Purity：99.46%

Storage：Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Larixyl acetate is a potent and selective TRPC6 inhibitor with IC50 values of 0.58 μM and 6.83 μM against hTRPC6-YFP and hTRPC3-YFP, respectively. Larixyl acetate prevents HPV and is effective in protecting against traumatic brain injury-induced systemic endothelial dysfunction.

In Vitro：Larixyl acetate (1-10 μM, 3 minutes) exerts its anti-inflammatory activity by inhibiting the phosphorylation of ERK1/2, AKT, and Src, suppressing fMLP-induced neutrophil migration, and inhibiting the interaction between βγ subunits and Src or PLCβ[2]. Larixyl acetate (5 μM, 1 hour) effectively improves TBI-induced aortic endothelial dysfunction by inhibiting TRPC6 activity[3]. Larixyl acetate (5 μM, 72 hours) significantly reduces the expression of ER stress genes and improves cell function in a cardiac hypertrophy cell model (H9c2 rat cardiomyocytes induced by Ang II)[5].

In Vivo：Larixyl acetate (5 mg/kg, i.p., once dailly for 7 days) significantly improves aortic endothelial dysfunction in TBI mice by inhibiting TRPC6 activity, particularly enhancing acetylcholine-induced dilation[3]. Larixyl acetate (5 mg/kg, i.p., once daily for 4 weeks) improves cardiac function in pressure overload-induced heart failure model by inhibiting TRPC6, reducing cardiac hypertrophy, fibrosis, and apoptosis[4].

IC50 & Target：hTRPC6 0.58 μM (IC50) hTRPC3 6.83 μM (IC50)

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References：

[1]. Urban N, et al. Identification and Validation of Larixyl Acetate as a Potent TRPC6 Inhibitor. Mol Pharmacol. 2016 Jan;89(1):197-213.  [Content Brief]

[2]. Liao HR, et al. Larixol inhibits fMLP-induced superoxide anion production and chemotaxis by targeting the βγ subunit of Gi-protein of fMLP receptor in human neutrophils. Biochem Pharmacol. 2022 Jul;201:115091.  [Content Brief]

[3]. Chen X, et al. The TRPC6 inhibitor, larixyl acetate, is effective in protecting against traumatic brain injury-induced systemic endothelial dysfunction. J Neuroinflammation. 2019 Jan 31;16(1):21.  [Content Brief]

[4]. Wang J, et al. The analgesic action of larixyl acetate, a potent TRPC6 inhibitor, in rat neuropathic pain model induced by spared nerve injury. J Neuroinflammation. 2020 Apr 16;17(1):118.  [Content Brief]

[5]. Jia M, et al. Larixyl acetate, a TRPC6 inhibitor, attenuates pressure overload‑induced heart failure in mice. Mol Med Rep. 2024 Mar;29(3):49.  [Content Brief]