| Description | Capsiate is an orally active TRPV1 agonist, a non-irritating capsaicin analog that acts as an antiallergic agent with anti-inflammatory, antioxidant, hypoglycemic, and inhibitory angiogenic activity. |
| In vitro | Capsiate在表达TRPV1[3]的HEK293细胞中引发电流响应。Capsiate (5至25 µM) 抑制了Src以及人脐静脉内皮细胞(HUVECs)中VEGF诱导的增殖和管形成。[1] |
| In vivo | Capsiate（0.03~0.54 mM; s.c.）在小鼠中引发痛觉反应。[3] Capsiate局部应用可减少被动皮肤过敏反应小鼠模型中的抗原诱导的耳部厚度增加，并在异位性皮炎小鼠模型中减少表皮厚度以及嗜酸性粒细胞和肥大细胞的浸润。[3] Capsiate（10 mg/kg）降低自由进食引起的体重增加的小鼠模型中的体重增长和腹围脂肪重量，同时增加氧消耗、脂肪氧化和碳水化合物氧化。[4] |
| Target activity | TRPV1:290 nM(EC50) |
| molecular weight | 306.4 |
| Molecular formula | C18H26O4 |
| CAS | 205687-01-0 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 90.0 mg/mL (293.7 mM), Sonication is recommended. |
| References | 1. Pyun BJ, et al. Capsiate, a nonpungent capsaicin-like compound, inhibits angiogenesis and vascular permeability via a direct inhibition of Src kinase activity. Cancer Res. 2008;68(1):227-235. 2. Iida T, et al. TRPV1 activation and induction of nociceptive response by a non-pungent capsaicin-like compound, capsiate. Neuropharmacology. 2003;44(7):958-967. 3. Lee, et al. Capsiate Inhibits DNFB-Induced Atopic Dermatitis in NC/Nga Mice through Mast Cell and CD4+ T-Cell Inactivation. J Invest Dermatol. 2015;135(8):1977-1985. 4. Haramizu S, et al. Capsiate, a non-pungent capsaicin analog, reduces body fat without weight rebound like swimming exercise in mice. Biomed Res. 2011;32(4):279-28 |