AM630 (Synonyms: 6-Iodopravodoline) |
Catalog No.GC10147
One-Click Copy Product Info
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AM630 is a potent and selective CB2 receptor inverse agonist.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 164178-33-0
Sample solution is provided at 25 µL, 10mM.
AM630 is a potent and selective CB2 receptor inverse agonist [1]. AM630 enhances forskolin-stimulated cAMP levels, inhibits [14S]-GTPγS binding, and antagonizes the inhibitory effects of the CB₂ agonist CP55940 on cAMP [2-3]. AM630 is commonly used in anxiety and neurobehavioral research [4].
In RAW264.7 mouse macrophage cells, AM630 (200nM; 5d) inhibits osteoclast differentiation [5]. In hCB2 CHO cells, AM630 (10μM; 24h) enhances forskolin-stimulated cAMP production [6]. In C2C12 myoblasts, pretreatment with AM630 (5μM; 2h) combined with anandamide significantly increased COX activity and COX-1 protein expression [7].
In CD-1 mice, AM630 (0.3mg/kg, 1mg/kg, 10mg/kg; ip; 1.5h) increased cortical FADD, Bax, cytochrome c, and PARP cleavage [8]. AM630 (1 mg/kg; ip; single injection) treatment reduces the LC3-II/LC3-I ratio and increases SQSTM1/p62 expression in the bladders of mice with cyclophosphamide (CYP)-induced cystitis [9].
References:
[1]. Ross R A, Brockie H C, Stevenson L A, et al. Agonist-inverse agonist characterization at CB1 and CB2 cannabinoid receptors of L759633, L759656 and AM630[J]. British journal of pharmacology, 1999, 126(3): 665.
[2]. Murataeva N, Mackie K, Straiker A. The CB2-preferring agonist JWH015 also potently and efficaciously activates CB1 in autaptic hippocampal neurons[J]. Pharmacological research, 2012, 66(5): 437-442.
[3]. Morgan N H, Stanford I M, Woodhall G L. Functional CB2 type cannabinoid receptors at CNS synapses[J]. Neuropharmacology, 2009, 57(4): 356-368.
[4]. Crowe M S, Nass S R, Gabella K M, et al. The endocannabinoid system modulates stress, emotionality, and inflammation[J]. Brain, behavior, and immunity, 2014, 42: 1-5.
[5]. Li W, Sun Y. Nrf2 is required for suppressing osteoclast RANKL-induced differentiation in RAW 264.7 cells via inactivating cannabinoid receptor type 2 with AM630[J]. Regenerative Therapy, 2020, 14: 191-195.
[6]. Bolognini D, Cascio M G, Parolaro D, et al. AM630 behaves as a protean ligand at the human cannabinoid CB2 receptor[J]. British journal of pharmacology, 2012, 165(8): 2561-2574.
[7]. Kim J, Watkins B A. Cannabinoid receptor antagonists and fatty acids alter endocannabinoid system gene expression and COX activity[J]. The Journal of Nutritional Biochemistry, 2014, 25(8): 815-823.
[8]. Salort G, Alvaro-Bartolome M, Garcia-Sevilla J A. Regulation of cannabinoid CB2 receptor constitutive activity in vivo: repeated treatments with inverse agonists reverse the acute activation of JNK and associated apoptotic signaling in mouse brain[J]. Psychopharmacology, 2017, 234(6): 925-941.
[9]. Liu Q, Wu Z, Liu Y, et al. Cannabinoid receptor 2 activation decreases severity of cyclophosphamide‐induced cystitis via regulating autophagy[J]. Neurourology and Urodynamics, 2020, 39(1): 158-169.
| Cell experiment [1]: | |
Cell lines | RAW264.7 mouse macrophage cells |
Preparation Method | The RAW264.7 mouse macrophage cells were culture in DMEM, which contained heat-inactivated FBS of 10%, 100U/mL penicillin, 100U/mL streptomycin and 2mM l-glutamine under 37℃ in a 5% CO2 incubator. Treated RAW264.7 cells by RANKL of 100ng/mL without or with 200nM AM630 for 5 days. |
Reaction Conditions | 200nM; 5d |
Applications | AM630 inhibits osteoclast differentiation. |
| Animal experiment [2]: | |
Animal models | CD-1 mice |
Preparation Method | Groups of randomly allocated CD-1 mice were acutely treated (i.p.) with the selective CB2 receptor full agonist JWH 133 (1 and 3mg/kg, 1h, n =6) and the CB2 receptor inverse agonists AM630 (0.3, 1, and 10mg/kg, 1.5 h, n = 5), JTE 907 (3 and 10mg/kg, 1.5h, n = 4) and raloxifene (2mg/kg, 1.5h, n =5). |
Dosage form | 0.3mg/kg, 1mg/kg, 10mg/kg; ip; 1.5h |
Applications | AM630 increased cortical FADD, Bax, cytochrome c, and PARP cleavage. |
References: | |
| Cas No. | 164178-33-0 | SDF | |
| Synonyms | 6-Iodopravodoline | ||
| Chemical Name | [6-iodo-2-methyl-1-(2-morpholin-4-ylethyl)indol-3-yl]-(4-methoxyphenyl)methanone | ||
| Canonical SMILES | CC1=C(C2=C(N1CCN3CCOCC3)C=C(C=C2)I)C(=O)C4=CC=C(C=C4)OC | ||
| Formula | C23H25IN2O3 | M.Wt | 504.36 |
| Solubility | 45mg/mL in DMSO; 10mg/mL in DMF; Sparingly soluble in aqueous buffers | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9827 mL | 9.9136 mL | 19.8271 mL |
| 5 mM | 396.5 μL | 1.9827 mL | 3.9654 mL |
| 10 mM | 198.3 μL | 991.4 μL | 1.9827 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 2 reference(s) in Google Scholar.)