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H3R antagonist 8
Catalog No. T213009 Copy Product Info
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H3R antagonist 8 is a selective non-imidazole histamine H3 receptor antagonist (IC50= 0.35 μM) that also exhibits hERG channel blocking activity (IC50= 0.67 μM). It suppresses seizures by antagonizing the H3 receptor and reduces tonic hindlimb extension (THLE) in mice in the maximal electroshock seizure (MES) model (ED50= 20.21 mg/kg). Additionally, it shortens the total movement distance induced by pentylenetetrazol (PTZ) in AB strain zebrafish larvae. H3R antagonist 8 is applicable in epilepsy research.
H3R antagonist 8
Copy Product Info🥰Excellent
Catalog No. T213009
H3R antagonist 8 is a selective non-imidazole histamine H3 receptor antagonist (IC50= 0.35 μM) that also exhibits hERG channel blocking activity (IC50= 0.67 μM). It suppresses seizures by antagonizing the H3 receptor and reduces tonic hindlimb extension (THLE) in mice in the maximal electroshock seizure (MES) model (ED50= 20.21 mg/kg). Additionally, it shortens the total movement distance induced by pentylenetetrazol (PTZ) in AB strain zebrafish larvae. H3R antagonist 8 is applicable in epilepsy research.
H3R antagonist 8
Cas No. 3097193-89-7
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.
For research use only—not for human use. No sales to individuals. Use as intended only.
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Chemical Properties
Storage & Solubility Information
| Description | H3R antagonist 8 is a selective non-imidazole histamine H3 receptor antagonist (IC50= 0.35 μM) that also exhibits hERG channel blocking activity (IC50= 0.67 μM). It suppresses seizures by antagonizing the H3 receptor and reduces tonic hindlimb extension (THLE) in mice in the maximal electroshock seizure (MES) model (ED50= 20.21 mg/kg). Additionally, it shortens the total movement distance induced by pentylenetetrazol (PTZ) in AB strain zebrafish larvae. H3R antagonist 8 is applicable in epilepsy research. |
| Targets&IC50 | H3 receptor:0.35 μM |
| In vitro | H3R antagonist 8 (Compound 6n) exhibits potent H3 receptor antagonistic activity in HEK-293 cells expressing human H3R, as demonstrated by a CRE-driven luciferase assay, with an IC50 value of 0.35 μM. Additionally, H3R antagonist 8 (0.1-100 μM) shows hERG channel blocking activity in HEK-293 cells stably expressing hERG potassium channels, using the patch-clamp technique, with an IC50 value of 0.67 μM. |
| In vivo | H3R antagonist 8 (Compound 6n) administered at 30 mg/kg via intraperitoneal injection in a single dose effectively eliminated tonic hind limb extension (THLE) in male Kunming mice within the maximal electroshock (MES) induced seizure model. Additionally, H3R antagonist 8 (Compound 6n) at 1 μM, with a pretreatment duration of 3 hours, significantly reduced the total movement distance in AB strain zebrafish larvae induced by pentylenetetrazol (PTZ). |
| Molecular Weight | 398.93 |
| Formula | C23H27ClN2O2 |
| Cas No. | 3097193-89-7 |
| Smiles | ClC=1C=CC=CC1C=2OC(=NC2C3=CC=C(OCCCN(CC)CC)C=C3)C |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
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