AM630 (Synonyms: 6-Iodopravodoline) |
Catalog No.GC10147
One-Click Copy Product Info
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AM630 es un potente y selectivo agonista inverso del receptor CB2
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 es un potente y selectivo agonista inverso del receptor CB2 [1]. AM630 mejora los niveles de cAMP estimulados por forskolin, inhibe la unión [14S]-GTPγS y antagoniza los efectos inhibidores del agonista CB₂ CP55940 en el cAMP [2-3]. AM630 se usa comúnmente en la ansiedad y la investigación neuroconductual [4].
En las células de macrófagos de ratón RAW264.7, AM630 (200nM; 5d) inhibe la diferenciación de osteoclastos[5]. En las células hCB2 CHO, AM630 (10μM; 24h) aumenta la producción de cAMP estimulada por forskolin [6]. En los mioblastos C2C12, el pretratamiento con AM630 (5μM; 2h) combinado con anandamida aumentó significativamente la actividad de la COX y la expresión de la proteína COX-1[7].
En ratones CD-1, AM630 (0.3mg/kg, 1mg/kg, 10mg/kg; ip; 1.5h) aumentó la escisión cortical de FADD, Bax, cytochrome c y PARP [8]. El tratamiento AM630 (1 mg/kg; ip; inyección única) reduce la relación LC3-II/LC3-I y aumenta la expresión de SQSTM1/p62 en las vajigas de ratones con cistitis inducida por cyclophosphamide (CYP)[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.
| Experimentos celulares [1]: | |
Líneas celulares | Células de macrófagos de ratón RAW264.7 |
Método de preparación | Las células de macrófagos de ratón RAW264.7 fueron cultivadas en DMEM, que contenía FBS inactivado por calor del 10%, 100U/mL de penicilina, 100U/mL de estreptomicina y 2mM de l-glutamina por debajo de 37℃ en una incubadora de CO2 al 5%. Células RAW264.7 tratadas por RANKL de 100ng/mL sin o con 200nM AM630 durante 5 días. |
Condiciones de reacción | 200nM; 5d |
Áreas de aplicación | AM630 inhibe la diferenciación de los osteoclastos. |
| Experimentos con animales [2]: | |
Modelos animales | Ratones CD-1 |
Método de preparación | Los grupos de ratones CD-1 asignados aleatoriamente fueron tratados de forma aguda (i.p.) con el agonista completo del receptor CB2 selectivo JWH 133 (1 y 3 mg/kg, 1h, n =6) y los agonistas inversos del receptor CB2 AM630 (0,3, 1 y 10 mg/kg, 1,5 h, n = 5), JTE 907 (3 y 10 mg/kg, 1,5h, n = 4) y raloxifeno (2 mg/kg, 1,5h, n =5). |
Forma de dosificación | 0,3 mg/kg, 1 mg/kg, 10 mg/kg; ip; 1,5h |
Áreas de aplicación | AM630 aumentó la escisión cortical de FADD, Bax, citocromo c y PARP. |
References: | |
| Cas No. | 164178-33-0 | SDF | |
| Sinónimos | 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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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
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- 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.)