LH 21 |
Catalog No.GC12538
One-Click Copy Product Info
|
silent CB1 antagonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 611207-11-5
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
IC50: 631 ±98 and 690 ± 41 nM for human and rat CB1 receptors, respectively
LH 21 is a CB1 antagonist.
The endogenous cannabinoid system plays a critical modulatory role in feeding behavior and metabolism, acting at both peripheral and central levels. Recently studies suggest that the chronic administration of cannabinoid CB1 receptor antagonists is effective in experimental obesity.
In vitro: Previous study showed that LH-21 was able to inhibit the binding of [3H]CP55940 to cloned human and rat CB1 receptors with IC50 values of 631 ±98 nM, and 690 ± 41 nM, respectively. LH-21 acted as an inverse agonist in a cAMP functional assay using cultured cells expressing human, rat or mouse CB1 receptor. In addition, in CHO cells overexpressing CB1, LH-21 was able to elevate cAMP, further confirming that LH-21 acted as an inverse agonist of CB1 in this model [1].
In vivo: Animal study showed that when given acutely LH-21 could decrease food intake and enhance the anorectic actions of oleoylethanolamide, a feeding suppressant lipid acting on peripheral sensory terminals in a similar way as rimonabant. However, unlike rimonabant, chronic administration of LH-21 at 3 mg/kg was able to reduce feeding but did not improve hypercholesterolaemia or hypertriglyceridaemia; nor did it reduce liver fat deposits in Zucker rats [2].
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Chen, R. Z.,Frassetto, A.,Lao, J.Z., et al. Pharmacological evaluation of LH-12, a newly discovered molecule that binds to cannabinoid CB1 receptor. European Journal of Pharmacology 584, 338-342 (2008).
[2] Pavón, F. J.,Serrano, A.,Pérez-Valero, V., et al. Central versus peripheral antagonism of cannabinoid CB1 receptor in obesity: Effects of LH-21, a peripherally acting neutral cannabinoid receptor antagonist, in Zucker rats. Journal of Neuroendocrinology 20, 116-123 (2008).
| Cas No. | 611207-11-5 | SDF | |
| Chemical Name | 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-3-hexyl-1H-1,2,4-triazole | ||
| Canonical SMILES | CCCCCCC1=NN(C2=CC=C(Cl)C=C2Cl)C(C3=CC=C(Cl)C=C3)=N1 | ||
| Formula | C20H20Cl3N3 | M.Wt | 407.1 |
| Solubility | ≤10mg/ml in ethanol;10mg/ml in DMSO;10mg/ml in dimethyl formamide | 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 | 2.4564 mL | 12.282 mL | 24.564 mL |
| 5 mM | 491.3 μL | 2.4564 mL | 4.9128 mL |
| 10 mM | 245.6 μL | 1.2282 mL | 2.4564 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: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 13 reference(s) in Google Scholar.)