CapsaicinCapsaicin
MedChemExpress (MCE)
HY-10448
404-86-4
(E)-Capsaicin
99.79%
4°C, protect from light *In solvent : -80°C, 1 year
-20°C, 6 months (protect from light)
Room temperature in continental US
may vary elsewhere.
Capsaicin ((E)-Capsaicin), an active component of chili peppers, is a TRPV1 agonist. Capsaicin has pain-relieving, antioxidant, anti-inflammatory, anti-cancer and certain neurotoxic effects.
Capsaicin (50-300 μM
24-72 hours) shows an augmented decrease in cell growth in a dose- and time-dependent manner. The observed IC50 value is around 150 μM[2]. Capsaicin (50-300 μM
24-72 hours) shows increase in cytosolic cytochrome c, activation of caspase 3 and PARP (p85) levels, and decreases anti-apoptotic Bcl-2 protein and increases pro-apoptotic Bad/Bax expression[2]. Capsaicin increases the nuclear condensation, nuclear DNA fragmentation and sub-G1 DNA content[2]. Capsaicin suppresses the cell cycle progression at the G1/S phase in FaDu cells by decreasing the expression of the regulators of cyclin B1 and D1, as well as cyclin-dependent protein kinases cdk-1, cdk-2 and cdk-4[2].
Capsaicin suppresses the development of lung carcinoma by amending the protein expressions of apoptotic regulators p53, Bcl-2, Bax and caspase-3[2]. Capsaicin (2 μg in 40 μL per mice, injected into the plantar surface of the left hind paw) induces pain-related behaviour in mice[4]. Capsaicin (3-30 μg in 10 μL per rat, plantar injection) induces secondary mechanical hypersensitivity (SMH) (used clinically as a model to potentially predict neuropathic pain) in rats[5]. Capsaicin (0-500 μg in 25 μL per rat, injected subcutaneously into the center of the right vibrissae pad) induces pain in the orofacial region or rats[6]. In high dose, Capsaicin may should be adminstered under anesthesia condition[7][8]. Capsaicin is more pungent than Dihydrocapsaicin (HY-N0361) [9]. Note: The spicy taste is choking, please take precautions. Capsaicin ((E)-Capsaicin) LD50 under different circumstances: Animal Backgroud Route LD50 References Rat adult ip 10 mg/kg [10] female
51-54 g ip 10.40-13.20 mg/kg [11] female
141 g ip 9.50 mg/kg [11] male po 161.2 mg/kg [12] female po 148.1 mg/kg [12] Mice male
25-35 g iv 0.56 mg/kg [11] male po 118.8 mg/kg [12] male ip 7.56 mg/kg [10] female po 97.4 mg/kg [12] female
30 g ip 6.50 mg/kg [11] ip 7.65 mg/kg [11] im 7.80 mg/kg [11] sc 9.00 mg/kg [11] po 60-75 mg/kg [11] po 190 mg/kg [11] pr >218 mg/kg [11] dermal >512 mg/kg [11] intratracheal 1.60 mg/kg [11] Hamster male
65 g ip >120 mg/kg [11] Guinea Pig male
405 g ip >1.10 mg/kg [11] Rabbit adult
503 g ip >50 mg/kg [11]
EC50: 290 nM (hTRPV1, in HEK293 cell)[1] Cellular Effect Cell Line Type Value Description References
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[1]. McNamara FN, et al. Effects of piperine, the pungent component of black pepper, at the human vanilloid receptor (TRPV1). Br J Pharmacol. 2005 Mar
144(6):781-90. [Content Brief]
[2]. Shin YH, et al. The Effect of Capsaicin on Salivary Gland Dysfunction. Molecules. 2016 Jun 25
21(7). [Content Brief]
[3]. Anandakumar P, et al. Capsaicin provokes apoptosis and restricts benzo(a)pyrene induced lung tumorigenesis in Swiss albino mice. Int Immunopharmacol. 2013 Jun 6
17(2):254-259. [Content Brief]
[4]. Nah JJ, et al. Effect of ginsenosides, active components of ginseng, on capsaicin-induced pain-related behavior. Neuropharmacology. 2000 Aug 23
39(11):2180-4. [Content Brief]
[5]. Joshi SK, et al Comparison of antinociceptive actions of standard analgesics in attenuating capsaicin and nerve-injury-induced mechanical hypersensitivity. Neuroscience. 2006 Dec 1
143(2):587-96. [Content Brief]
[6]. Pelissier T, et al. The orofacial capsaicin test in rats: effects of different capsaicin concentrations and morphine. Pain. 2002 Mar
96(1-2):81-7. [Content Brief]
[7]. Matsuda H, et al. Roles of capsaicin-sensitive sensory nerves, endogenous nitric oxide, sulfhydryls, and prostaglandins in gastroprotection by momordin Ic, an oleanolic acid oligoglycoside, on ethanol-induced gastric mucosal lesions in rats. Life Sci. 1999
65(2):PL27-32. [Content Brief]
[8]. Demirbilek S, et al. Small-dose capsaicin reduces systemic inflammatory responses in septic rats. Anesth Analg. 2004 Nov
99(5):1501-1507. [Content Brief]
[9]. Friedman JR, et al. Anticancer Activity of Natural and Synthetic Capsaicin Analogs. J Pharmacol Exp Ther. 2018 Mar
364(3):462-473. [Content Brief]
[10]. Glinsukon T, et al. Acute toxicity of capsaicin in several animal species[J]. Toxicon, 1980, 18(2): 215-220.
[11]. Kawada T, Iwai K. In vivo and in vitro metabolism of dihydrocapsaicin, a pungent principle of hot pepper [Capsicum annuum], in rats[J]. Agricultural and Biological Chemistry (Japan), 1985, 49(2).
[12]. Saito A, Yamamoto M. Acute oral toxicity of capsaicin in mice and rats[J]. The Journal of toxicological sciences, 1996, 21(3): 195-200.
