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CB-1-IN-1

" in TargetMol Product Catalog
  • Inhibitors & Agonists
    15
    TargetMol | Inhibitors_Agonists
  • Natural Products
    1
    TargetMol | Natural_Products
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    TargetMol | Inhibitors_Agonists
CB1-IN-1
DBPR211
T59961429239-98-4
CB1-IN-1 (DBPR211) is a peripherally restricted CB1R antagonist, for CB1R and CB2R with Ki of 0.3 nM and 21 nM,respectively.
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CB-6644
T106932316817-88-4In house
CB-6644 is a small molecule inhibitor of the ATPase activity of the RUVBL1 2 complex. It specifically interacts with RUVBL1 2 in cancer cells and blocks the ATPase activity of RUVBL1 2 with a half-maximal inhibitory concentration (IC50) of 15 nM[1].
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COR659
T36520544450-68-2
COR659 is a GABAB positive allosteric modulator (PAM) . COR659 suppresses alcohol and chocolate self-administration in rats[1]. COR659 apparently exerts its effects via a composite mechanism, including positive allosteric modulation of the GABAB receptor and an action at the cannabinoid CB1 receptor[3]. COR659 (0, 2.5, 5 and 10 mg kg) treatment is completely ineffective on lever-responding (FR10) for regular food pellets in food-deprived Wistar rats[1].COR659 is able to suppress lever-responding for a sucrose solution in sP rats and a chocolate solution in Wistar rats[2]. Animal Model: Male sP and Wistar rats[1]. [1]. Paola Maccioni, et al. Suppressing effect of COR659 on alcohol, sucrose, and chocolate self-administration in rats: involvement of the GABA B and cannabinoid CB 1 receptors. Psychopharmacology (Berl). 2017 Sep;234(17):2525-2543. [2]. Francesca Ferlenghi, et al. The GABA B receptor positive allosteric modulator COR659: In vitro metabolism, in vivo pharmacokinetics in rats, synthesis and pharmacological characterization of metabolically protected derivatives. Eur J Pharm Sci. 2020 Dec 1;155:105544. [3]. Paola Maccioni, et al. Anti-addictive properties of COR659 - Additional pharmacological evidence and comparison with a series of novel analogues. Alcohol. 2019 Mar;75:55-66.
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6-8 weeks
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CB2R-IN-1
T106971257555-79-5
CB2R-IN-1 is a potent inverse agonist of the cannabinoid CB2 receptor (Ki: 0.9 nM).
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8-10 weeks
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o-2050
T230991883545-42-3
O-2050 is a high-affinity cannabinoid CB1 receptor antagonist with a Ki of 2.5 nM and inhibits the cannabinoid CB2 receptor with a Ki of 0.2 nM. O-2050 decreased food intake and stimulated locomotion in mice [1].
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8-10 weeks
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OMDM169
OMDM 169,OMDM-169
T28235130193-44-1
OMDM169 is a potent and selective MAGL inhibitor. OMDM169 could enhances 2-AG levels and of exerts analgesic activity via indirect activation of cannabinoid receptors. OMDM169 exhibited 0.13 microMing activities in
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10-14 weeks
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azd1940
UNII-0J0035E9FT, AZD-1940, AZD 1940
T30252881413-29-2
AZD1940 (UNII-0J0035E9FT) is a high affinity CB(1) CB(2) receptor agonist of the cannabinoid with oral activity. Application in the study of orofacial pain.
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6-8 weeks
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(R)-(+)-Docosahexaenyl-1'-Hydroxy-2'-Propylamide
T380281282618-08-9
N-Acyl ethanolamines (NAEs) have diverse biological actions that are strongly affected by the associated acyl group. Docosahexaenoyl ethanolamide (DHEA) has potential signaling roles in cancer, inflammation, and neurological development and functioning. At least some of DHEA's effects are mediated through cannabinoid (CB) receptors, while some NAEs also act as vanilloid receptor agonists and voltage-gated K+ channel blockers. (R)-(+)-Docosahexaenyl-1'-hydroxy-2'-propylamide is a homolog of DHEA, characterized by the addition of an (R)-α-methyl group at the methylene carbon adjacent to the amide nitrogen. A similar modification of arachidonoyl ethanolamide to produce R-1 methanandamide imparts higher affinity for the CB receptor as well as improved metabolic stability. The physiological actions of this compound have not been evaluated.
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ACEA
Arachidonoyl 2'-Chloroethylamide, 2'-chloro-AEA
T38138220556-69-4
Arachidonoyl 2-chloroethylamide (ACEA) is a potent and selective cannabinoid (CB) receptor 1 agonist with Ki values of 1.4 and >2,000 nM for CB1 and CB2 receptors, respectively. In whole animal experiments, ACEA induces hypothermia in mice with the same efficacy as arachidonoyl ethanolamide , in spite of its higher affinity for the CB1 receptor. These data have been interpreted to indicate that ACEA may be a substrate for fatty acid amide hydrolase (FAAH), and thus only transiently available in whole animal experiments.
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6-8 weeks
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GAT229
T38204889860-85-9
GAT229 is a positive allosteric modulator of cannabinoid receptor 1 (CB1) and the S-(-) enantiomer of the CB1 modulator GAT211. It does not activate the receptor on its own but enhances the binding and activity of CB agonists. GAT229 (1 μM) enhances the binding of the CB1 full agonist CP 55,940 to CHO cells expressing human recombinant CB1 (hCB1), as well as the activity of 2-arachidonoyl glycerol , arachidonoyl ethanolamide , and CP 55,940 in arrestin2 recruitment assays and increases ERK1/2 and PLCβ3 phosphorylation in HEK293 cells expressing hCB1. GAT229 (1 μM) enhances depolarization-induced suppression of excitation but does not inhibit excitatory postsynaptic currents (EPSCs) in murine autaptic hippocampal neurons. GAT229 (0.2%, topical) reduces intraocular pressure by 5.8 and 7.7 mm Hg after 6 and 12 hours, respectively, in a transgenic mouse model of ocular hypertension using nose, ear, eye mutation (nee) mice.
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6-8 weeks
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Telaglenastat hydrochloride
CB-839 hydrochloride
T393091874231-60-3
Telaglenastat (CB-839) hydrochloride is a first-in-class, reversible, and orally active inhibitor of glutaminase 1 (GLS1), selectively inhibiting the splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C), as opposed to GLS2. Telaglenastat hydrochloride has an IC50 of 23 nM for endogenous glutaminase in mouse kidney and 28 nM in the brain, inducing autophagy and exhibiting antitumor activity.
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1-2 weeks
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(±)-Ibipinabant
(±)-BMS6462, SLV319, (±)-SLV319
T4654362519-49-1
(±)-Ibipinabant ((±)-SLV319) has been utilized in clinical trials for the treatment of obesity and type 2 diabetes.
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Linderalactone
T5S1897728-61-0
1. Linderalactone showed significant inhibitory effects on superoxide anion generation by human neutrophils in response to fMLP CB, values of IC5 is 8.48 μg mL.
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CB-25
T78083869376-63-6
CB-25 is a partial agonist ligand of CB1 cannabinoid receptors, augmenting Forskolin-induced cAMP formation in cancer cells, though not affecting hCB1-CHO cells [1].
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8-10 weeks
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Linoleoyl Ethanolamide
T842568171-52-8
Linoleoyl Ethanolamide is an endocannabinoid agent. It acts by binding to TRPV1 increasing ERK phosphorylation and AP-1 dependent transcription in CB-receptor in an independent manner.
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