Bay 59-3074 |
رقم الكتالوجGC19060 |
Bay 59-3074 عبارة عن ناهض جزئي لمستقبلات القنب CB1 / CB2 الانتقائية مع قيم Ki من 48.3 و 45.5 نانومتر عند مستقبلات CB1 و CB2 البشرية ، على التوالييحتوي Bay 59-3074 على خصائص مسكنة
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Cas No.: 406205-74-1
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Bay 59-3074 is a novel, selective CB1/CB2 receptor partial agonist with Ki values of 48.3 and 45.5 nM at human CB1 and CB2 receptors respectively . Orally active CB1 agonist in vivo. target: CB1/CB2 receptor partial agonist.Ki: 48.3 and 45.5 nM (CB1 and CB2 receptors)In vitro: analgesic, antihyperalgesic, and antiallodynic properties in rat models of acute and chronic pain. The reference concentration is 10 uM. [1]In vivo: administration of BAY 59-3074 (ED50 value: 0.41 mg/kg).Orally active CB1 agonist in vivo. [2] BAY 59-3074 (0.3-3 mg/kg, p.o.) induce antihyperalgesic and antiallodynic effects against thermal or mechanical stimuli in rat models of chronic neuropathic. Antiallodynic efficacy of BAY 59-3074 (1 mg/kg, p.o.) in the spared nerve injury model was maintained after 2 weeks of daily administration. However, tolerance developed rapidly (within 5 days) for cannabinoid-related side effect. [1] BAY 59-3074 have analgesic, antihyperalgesic, and antiallodynic properties in rat models of acute and chronic pain.[1]
References:
[1]. De Vry J et al. 3-[2-cyano-3-(trifluoromethyl)phenoxy]phenyl-4,4,4-trifluoro-1-butanesulfonate (BAY 59-3074): a novelcannabinoid Cb1/Cb2 receptor partial agonist with antihyperalgesic and antiallodynic effects. J Pharmacol Exp Ther. 2004 Aug;310(2):620-32
[2]. De Vry J et al. Discriminative stimulus effects of the structurally novel cannabinoid CB1/CB2 receptor partial agonist BAY 59-3074 in the rat. Eur J Pharmacol. 2004 Nov 28;505(1-3):127-33.
Cas No. | 406205-74-1 | SDF | |
Canonical SMILES | O=S(CCCC(F)(F)F)(OC1=CC=CC(OC2=CC=CC(C(F)(F)F)=C2C#N)=C1)=O | ||
Formula | C18H13F6NO4S | M.Wt | 453.36 |
الذوبان | DMSO : ≥ 34 mg/mL (75.00 mM) | 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. |
||
Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.2058 mL | 11.0288 mL | 22.0575 mL |
5 mM | 0.4412 mL | 2.2058 mL | 4.4115 mL |
10 mM | 0.2206 mL | 1.1029 mL | 2.2058 mL |
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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 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.
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Average Rating: 5
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