Cannabinoides

Carboxylic acid with phenol function

Tedalinab is an effective and selective cannabinoid receptor 2 agonist.

Applications Acetaminophen-d3 is deuterium labeled Acetaminophen (A161220), an analgesic and antipyretic agent used as a pain reliever to treat headache, muscle aches, and arthritis (1,2,3). References (1) McGill, M. R. and Jaeschke, H. Pharm Res. 30, 2174 (2013)(2) Fairbrother, J.E., et al.: Anal. Profiles Drug Subs., 3, 1 (1974) (3) Hinson, J.A., et al.: Rev. Biochem. Toxicol., 2, 103 (1980)

JTE-907 是一种具有高度选择性和口服活性的 CB2 受体反向激动剂。JTE-907在体内展现出抗炎活性。

Applications (5Z,8Z,11Z,14Z)-2-[[Tris(1-methylethyl)silyl]oxy]-5,8,11,14-eicosatetraenoic Acid 1-[[[Tris(1-methylethyl)silyl]oxy]methyl]ethyl Ester is an intermediate in the synthesis of 2-Arachidonoylglycerol (A765050), an major endocannabinoid, which can inhibit synaptic transmission by presynaptic cannabinoid CB1 receptors. References Baur, R., et al.: J. Neurochem., 126, 29 (2013); Fanelli, F., et al.: J. Lipid. Res., 53, 481 (2012);

Rimonabant (SR141716) is an inverse agonist for the cannabinoid receptor CB1.

Rimonabant hydrochloride (SR 141716A) 是中心大麻素受体 1 的高效选择性反向激动剂, Ki 值为1.8 nM。它也能够抑制分枝杆菌膜蛋白3。

TM38837 is an antagonist of cannabinoid receptor type 1 (CB1), with potential for the treatment of obesity and type 2 diabetes.

Stability Light Sensitive Applications A cannabinoid anticancer quinone, HU-331, is more potent and less cardiotoxic than Doxorubicin and thus it has a high potential for development as a new anticancer drug. References Dana, B., et al.: J. Clin. Oncol., 11, 644 (1993), Feleszko, W., et al.: Clin. Cancer Res., 6, 2044 (2000), Kogan, N., et al.: J. Med. Chem., 47, 3800 (2004),

Applications 2-(5-methyl-2-furyl)ethanamine (cas# 30796-85-1) is a useful research chemical.

ML-193: GPR55 antagonist, IC50 221nM, 27x selective over GPR35/CB1/CB2, may aid Parkinson's symptoms.

Applications Labelled JWH 018 (P283650). It is the 18th compound synthesized in a series of more than 470 analogs and metabolites of ∆9-Tetrahydro- cannabinol (THC) (T293200), the active component of marijuana. JWH 018 acts as cannabinoid receptor. References Matsuda, L., et al.: Nature, 346, 561 (1990), Gerard, C., et al.: Biochem. J., 279, 129 (1991), Parkkari, T., et al.: Bioorg. Med. Chem., 14, 5252 (2006), Salo, O., et al.: J. Med. Chem., 49, 554 (2006),

OMDM-5 is a potent vanilloid receptor type 1 (TRPV1, EC50 = 75 nM) agonist, showing weak ligand activity at cannabinoid type 1 receptor (CB1, Ki=4.9 μM).

A-836339: Potent cannabinoid, CB2-focused (Ki=0.64nM), lesser CB1 affinity (Ki=270nM); analgesic, anti-inflammatory in mice.

Applications (-)-Isoperitenone, is a derivative of (-)-Cannabidiol (C175300), a major, non psychotropic constituent of cannabis. References Hanus, L. et al.: Organic & Biomolecular Chemistry, Vol.3, Issue 6 (2005);

Applications Acetaminophen Mercapurate Disodium Salt is a metabolite of Acetaminophen (A161220), an analgesic and antipyretic agent used as a pain reliever to treat headache, muscle aches, and arthritis (1,2). References (1) McGill, M. R. and Jaeschke, H. Pharm Res. 30, 2174 (2013)(2) Potter, D.W. et al.: Mol. Pharmacol., 29, 155 (1986)

Applications (4R,7S)Tedalinab is a stereoisomer of Tedalinab(T013730) is a cannabinoid receptor modulator that is useful for treating non-immediate type allergic diseases. References Muthuppalaniappan, M., et al.: PCT Int. Appl. WO 2006129178 A1 20061207. Dec 7, 2006; Narayanan, S., et al.: U.S. Pat. Appl. Publ. US 20090312385 A1 20091217. Dec 17, 2009

Applications Falcarinol is a covalent cannabinoid CB1 receptor antagonist and induces pro-allergic effects in skin. A natural pesticide produced by carrots and red ginseng, protecting hosts roots from various fungal diseases. It has been shown to have nutritional benefits, reducing the risk of developing specific forms of cancer. References Czepa, A., et al.: J. Agric. Food Chem., 52, 4508 (2004), Radulovic, N., et al.: Chem. Nat. Compds., 44, 390 (2008),

Stability Hygroscopic Applications A labelled cannabinoid receptor ligand. References Huffman, J., et al.: Bioorg Med. Chem., 9, 2863 (2001), Govaerts, S., et al.: Eur. J. Pharm. Sci., 23, 233 (2004), Bosier, B., et al.: J. Neurochem., 102, 1996 (2007),

Polyphenol

Applications An analgesic compound which acts as a partial agonist at both the CB1 and CB2 cannabinoid receptors. Synthetic Cannabinoids References Compton, D., et al.: J. Pharmacol. Exper. Ther., 263, 1118 (1992), Tetko, I., et al.: J. Med. Chem., 44, 2411 (2001), Huffman, J., et al.: Bioorg. Med. Chem., 11, 539 (2003),

BML-190 (Indomethacin morpholinylamide) 是一种 CB2 受体的配体,其对 CB2 受体 (Ki:435 nM) 和 CB1受体 (Ki> 2 μM)。

CB1 antagonist 2 (AM4113) is caimabinoid 1 (CB1) antagonist which inhibits CB1 in vivo with an IC50 of 25.5 nM.

Δ8-THC-C8 is a semi-synthetic cannabinoid. It acts as an agonist for the cannabinoid receptor 1 (CB1) with an EC50 value of 13.8 nM.

Applications It is a drug which acts as a potent but unselective agonist for the cannabinoid receptor CB1 or CB2.Synthetic Cannabinoids Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package References Yamada., et al.: J. Med. Chem., 39, 1967 (1996),

WIN 55,212-2 Mesylate ((R)-(+)-WIN 55212) is a potent aminoalkylindole cannabinoid (CB) receptor agonist with Kis of 62.3 and 3.3 nM for human recombinant CB1 and CB2 receptors, respectively. Cannabinoid analogue WIN 55,212-2 Mesylate exhibited a novel anticancer effect against human tumors.

RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB1) receptor with a pIC50 of 7.54 in Ca2+ mobilization assay.

Bay 59-3074 is a CB1/CB2 receptor partial agonist (Ki: 48.3/45.5 nM).

CB2R PAM, an oral drug, boosts CB2 receptor response to specific agonists, showing potential in neuropathic pain relief.

Applications 1-(5-Fluoropentyl)-N-tricyclo[3.3.1.13,7]dec-1-yl-1H-indazole-3-carboxamide is a derivative made in the synthesis of fluorescent heterocyclic aminoadamantanes as multifunctional neuroprotective agents. Synthetic cannabinoids References Jacques, J., et al.: Bioorg. Med. Chem., 19, 3935 (2011);

Applications AB-CHMINACA Metabolite M4 is a synthetic cannabinoid. AB-CHMINACA Metabolite M4 is structurally related to AB-FUBINACA, a high affinity ligand of the central CB1 receptor.Synthetic Cannabinoids References Banister, Samuel D., et al.: ACS Chem. Neurosci., 7, 1241 (2016),

Cannabichromevarin is a phytocannabinoid naturally found in very low levels compared to other cannabinoids from which it differs in having a propyl chain in place of a pentyl chain1. Based on its structure, it is believed to act as a potent anandamine inhibitor similarly to cannabichromene, however, the majority of its pharmacological and toxicological properties are currently unknown. In vitro assays have shown cannabichromevarin protect against oxidative stress in vitro in macrophages2. It was recently shown to be effective for treatment-resistant epilepsy in a patented combination with cannabidiol in a recent open-ended clinical trial3.

Applications The 3-methylbutyl homolog of JWH 073 (B693550). An analgesic compound which acts as a partial agonist at both the CB1 and CB2 cannabinoid receptors.

Olivetol, found in lichens, is an organic antioxidant and THC synthesis precursor.

A cannabinoid receptor agonist, which binds more selectively to CB2 than CB1 receptors (1000-fold). GW833972A inhibits vagus nerve depolarization induced by tussive agents, such as hypertonic saline (EC50 = 6.5 μM), capsaicin (EC50 = 33.9 μM) or PGE2 (EC50 = 15.9 μM).

CB2R/FAAH modulator-1: agonizes CB2R, inhibits FAAH (IC50=4 μM), alters cytokine production; used in inflammation research. Ki: CB2R=14.8 nM, CB1R=241.3 nM.

CB2 modulator 1 is a potent CB2 modulator. It can be used for the research for immune disorders, osteoporosis, inflammation, renal ischemia.

Stability Light Sensitive Applications Cannabigerorcinic Acid is a compound that takes part in the biosynthesis of daurichromenic acid synthase which is active in anti-HIV biosynthesis. References Iijima, M. et al.: Plant Phys., 174, 2213 (2017);

Applications 2Z)-1-Chloro-2-decene is an intermediate in the synthesis of Falcarinol which is a covalent cannabinoid CB1 receptor antagonist and induces pro-allergic effects in skin. A natural pesticide produced by carrots and red ginseng, protecting hosts roots from various fungal diseases. It has been shown to have nutritional benefits, reducing the risk of developing specific forms of cancer. References Czepa, A., et al.: J. Agric. Food Chem., 52, 4508 (2004), Radulovic, N., et al.: Chem. Nat. Compds., 44, 390 (2008),

ML-184 (CID2440433) is a potent synthetic agonist of GPR55 with EC50 of 0.26 μM.