AM630 (Synonyms: 6-Iodopravodoline) |
| カタログ番号GC10147 |
CB2の逆作用薬であり、CB1受容体の部分作動薬です。
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 selective and competitive antagonist of cannabinoid receptors with Ki values of 5 μM and 31.2 nM for CB1 receptor and CB2 receptor, respectively [1].
In CB1-transfected CHO cells, AM630 significantly inhibited the production of cAMP stumilated by forskolin. In CB2-transfected cells, AM630 promoted forskolin to stimulate cyclic AMP production with EC50 value of 230.4 nM. AM630 also exerted to have inhibitory effect on the binding of GTPγS to membranes from CB2-transfected cells. Besides that, AM630 was found to activate the TRPA1 channels and subsequently desensitizing TRPA1 and TRPV1 channels in TG sensory neurons. Moreover, AM630 significantly weakened the thermal hyperalgesia induced by CAP (capsaicin) in WT mice [1, 2].
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. British journal of pharmacology, 1999, 126(3): 665-672.
2. Patil M, Patwardhan A, Salas M M, et al. Cannabinoid receptor antagonists AM251 and AM630 activate TRPA1 in sensory neurons. Neuropharmacology, 2011, 61(4): 778-788.
| Cas No. | 164178-33-0 | SDF | |
| 同義語 | 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 |
| 溶解度 | 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 | 0.3965 mL | 1.9827 mL | 3.9654 mL |
| 10 mM | 0.1983 mL | 0.9914 mL | 1.9827 mL |
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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 ddH2O, 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%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 2 reference(s) in Google Scholar.)
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