BW 373U86 (Synonyms: SNC86) |
Catalog No.GC16521
One-Click Copy Product Info
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BW 373U86(SNC86)은 1.49nM의 IC50을 갖는 δ-오피오이드 수용체 작용제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 155836-50-3
Sample solution is provided at 25 µL, 10mM.
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Ki: 1.8, 15, 85 and 34 nM for delta, mu, epsilon and kappa receptor
Opioid receptors are heterogeneous and at least four types, mu,.delta, kappa and epsilon, are known to exist. Currently, all clinically used opiates act through the mu receptor to induce analgesia; however, they also induce unwanted side effects such as respiratory depression, dependence, constipation and muscle rigidity.BW 373U86 is a novel, potent and selective nonpeptidic delta opioid receptor agonist.
In vitro: BW 373U86 was a potent delta receptor-selective ligand in receptor binding assays. The Ki values were 1 .8 ± 0.4, 15 ± 3, 85 ± 4 and 34 ± 3 nM for delta, mu, epsilon and kappa receptor binding sites, respectively. BW 373U86 inhibited electncally evoked muscle contraction of mouse vas deferens with an ED50 value of 0.2 ± 0.06 nM [1].
In vivo: BW 373U86 inhibited the acoustic startle reflex after subcutaneous administration from 0.2- to 2-mg/kg doses in rats, and this inhibition was blocked by naltnndole. BW 373U86 also induced a dose-dependent increase of locomotor activity in rats at similar doses. This effect was inhibited by naltnndole [3].
Clinical trial: Up to now, BW 373U86 is still in the preclinical development stage.
Reference:
[1] Chang KJ, Rigdon GC, Howard JL, McNutt RW. A novel, potent and selective nonpeptidic delta opioid receptor agonist BW 373U86. J Pharmacol Exp Ther. 1993 Nov;267(2):852-7.
| Cas No. | 155836-50-3 | SDF | |
| Synonyms | SNC86 | ||
| Chemical Name | 4-((R)-((2S,5R)-4-allyl-2,5-dimethylpiperazin-1-yl)(3-hydroxyphenyl)methyl)-N,N-diethylbenzamide | ||
| Canonical SMILES | OC1=CC([C@@H](C2=CC=C(C(N(CC)CC)=O)C=C2)N3[C@@H](C)CN(CC=C)[C@H](C)C3)=CC=C1 | ||
| Formula | C27H37N3O2 | M.Wt | 435.61 |
| Solubility | <43.56mg/ml in 1eq. HCl | Storage | Store at 4°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 | 2.2956 mL | 11.4782 mL | 22.9563 mL |
| 5 mM | 459.1 μL | 2.2956 mL | 4.5913 mL |
| 10 mM | 229.6 μL | 1.1478 mL | 2.2956 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
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: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)