Clobenpropit dihydrobromide (Synonyms: VUF 9153) |
Catalog No.GC10490
One-Click Copy Product Info
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El dihidrobromuro de clobenpropit es un potente antagonista/agonista inverso de la histamina H3R con un pEC50 de 8,07 para la histamina H3LR.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 145231-35-2
Sample solution is provided at 25 µL, 10mM.
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Clobenpropit is a selective histamine H3 receptor antagonist (Ki = 0.17 nM in rat cortical membranes).[1] Clobenpropit (0.3, 0.1, and 3 nM) reduces inhibition of electrically induced contractions in isolated guinea pig ileum longitudinal muscle by the H3 receptor agonist (R)-α-methylhistamine. It does not inhibit histamine-induced contractions in isolated guinea pig ileum or tachycardia in isolated right atria at concentrations up to 1 μM, indicating a lack of functional antagonist activity at H1 and H2 receptors, respectively. Clobenpropit (1 and 3 mg/kg) decreases the duration of the tonic, clonic, and convulsive coma phases of electrically induced convulsions in mice, an effect that can be blocked by (R)-α-methylhistamine or imetit.[2] Clobenpropit (0.1 μM) also increases GABA release and inhibits NMDA-induced neurotoxicity in primary rat cortical neurons.[3]
Reference:
[1]. Solt, L.A., Kumar, N., Nuhant, P., et al. Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand. Nature 472(7344), 491-494 (2011).
[2]. Yokoyama, H., Onodera, K., Maeyama, K., et al. Clobenpropit (VUF-9153), a new histamine H3 receptor antagonist, inhibits electrically induced convulsions in mice. Eur. J. Pharmacol. 260(1), 23-28 (1994).
[3]. Dai, H., Fu, Q., Shen, Y., et al. The histamine H3 receptor antagonist clobenpropit enhances GABA release to protect against NMDA-induced excitotoxicity through the cAMP/protein kinase A pathway in cultured cortical neurons. Eur. J. PHarmacol. 563(1-3), 117-123 (2007).
| Cas No. | 145231-35-2 | SDF | |
| Sinónimos | VUF 9153 | ||
| Chemical Name | (Z)-3-(1H-imidazol-5-yl)propyl N'-4-chlorobenzylcarbamimidothioate dihydrobromide | ||
| Canonical SMILES | ClC1=CC=C(C=C1)C/N=C(N)\SCCCC2=CN=CN2.Br.Br | ||
| Formula | C14H17ClN4S.2HBr | M.Wt | 470.65 |
| Solubility | 30 mg/ml in DMSO, 2.5 mg/ml in Ethanol, 20 mg/ml in water | 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 | 2.1247 mL | 10.6236 mL | 21.2472 mL |
| 5 mM | 424.9 μL | 2.1247 mL | 4.2494 mL |
| 10 mM | 212.5 μL | 1.0624 mL | 2.1247 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 29 reference(s) in Google Scholar.)