Benzenamine; Jenloga; Catapres; Clonidine monohydrochloride; Duraclon; Catapres-TTS; Kapvay
| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| 2g |
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Purity: ≥98%
Clonidine HCl (Catapres, Duraclon, Jenloga, Catapres-TTS, and Kapvay), the hydrochloride salt of clonidine, is a direct-acting α2 adrenergic agonist with antihypertensive effects. It activates α2 adrenergic with an ED50 of 0.02±0.01 mg/kg. Clonidine is a sympathomimetic medication that has been used to treat a variety of pain conditions, migraines, menopausal flushing, diarrhea, high blood pressure, attention deficit hyperactivity disorder (ADHD), anxiety disorders, and withdrawal from alcohol, opioids, or smoking. By activating brain α2-receptors, clonidine lowers blood pressure by reducing peripheral vascular resistance. This is how it treats high blood pressure.
| Targets |
α2-adrenergic receptor
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| ln Vitro |
Clonidine (0.01, 0.1 or 1 μM) significantly and dose-dependently increases the expression of CGRP (α and β) mRNA in endothelial cells. Endothelial cells treated with 1 μM clonidine for 24 hours exhibit a significant increase in NO production. Clonidine-induced CGRP production is modulated by the NO pathway[2].
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| ln Vivo |
Clonidine (50 μg/kg, i.p.) causes a three-hour period of significant rat body temperature reduction, peaking one hour after administration. Rats treated intracerebroventricularly with neutral doses of phentolamine 15 minutes prior to clonidine significantly counteract the hypothermia caused by clonidine[1]. PCP-induced dopamine efflux in the prefrontal cortex is potently suppressed by clonidine (0.003-0.05 mg/kg, i.p.). Clonidine cannot suppress PCP-induced dopamine overflow in the prefrontal cortex when the alpha-2A receptor antagonist BRL-44408 is administered beforehand[3]. Clonidine (0.6 μg i.c.) has no effect on blood pressure in SO rats that have been pretreated with DMSO. On the other hand, clonidine significantly (P < 0.05, one-way ANOVA) lowers blood pressure in SO rats following central adenosine A1R blockade (DPCPX). Contrarily, clonidine (0.6 μg i.c.) significantly lowers blood pressure in ABD rats that have received DMSO pretreatment; crucially, central A1R blockade (DPCPX pretreatment) has no effect on the clonidine-evoked drop in blood pressure in ABD rats (P > 0.05, one-way ANOVA). In SO rats pretreated with DPCPX, clonidine significantly (P < 0.05) raises the RVLM pERK1/2 level in comparison to either basal or clonidine treatment in SO rats pretreated with DMSO. This increase coincides with the onset of the hypotensive response. Clonidine significantly (P < 0.05) increases RVLM pERK1/2 in ABD rats pretreated with vehicle (DMSO), and this response is unaffected by DPCPX pretreatment[4].
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| Animal Protocol |
On the day of the experiment, two hours before the baseline sample collection starts, the flow rate is increased to 2 μL/min. Following the collection of four baseline samples, animals are pretreated with an intraperitoneal (i.p.) injection of either 0.9% saline (the vehicle), clonidine (0.0033, 0.01, or 0.05 mg/kg), or guanfacine (0.05 or 0.5 mg/kg). Twenty minutes later, the animals receive an injection of PCP (2.5 mg/kg, i.p.). Dialysates are collected every twenty minutes. BRL (1.0 mg/kg) is given 20 minutes before clonidine in a different study. Furthermore, in certain control studies, the animals are given a single injection of saline, clonidine (0.01 or 0.05 mg/kg), guanfacine (0.5 mg/kg), or BRL (1.0 mg/kg).
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| References |
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| Molecular Formula |
C9H10CL3N3
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| Molecular Weight |
266.5
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| Exact Mass |
264.99
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| Elemental Analysis |
C, 40.55; H, 3.78; Cl, 39.90; N, 15.76
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| CAS # |
4205-91-8
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| Related CAS # |
Clonidine; 4205-90-7
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| Appearance |
Solid powder
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| SMILES |
C1CN=C(N1)NC2=C(C=CC=C2Cl)Cl.Cl
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| InChi Key |
ZNIFSRGNXRYGHF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H9Cl2N3.ClH/c10-6-2-1-3-7(11)8(6)14-9-12-4-5-13-9;/h1-3H,4-5H2,(H2,12,13,14);1H
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| Chemical Name |
N-(2,6-dichlorophenyl)-4,5-dihydro-1H-imidazol-2-amine;hydrochloride
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (375.16 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7523 mL | 18.7617 mL | 37.5235 mL | |
| 5 mM | 0.7505 mL | 3.7523 mL | 7.5047 mL | |
| 10 mM | 0.3752 mL | 1.8762 mL | 3.7523 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03121261 | Active Recruiting |
Drug: levobupivacaine Drug: clonidine |
Inguinal Hernia Spinal Anesthesia |
University Hospital Dubrava | May 1, 2017 | Phase 4 |
| NCT01530373 | Active Recruiting |
Drug: solifenacin Drug: clonidine |
Hot Flashes Breast Cancer |
University of Arkansas | February 2012 | Phase 2 |
| NCT03653832 | Active Recruiting |
Drug: Dexmedetomidine Drug: Clonidine Drug: Propofol |
Critical Illness | University of Edinburgh | December 10, 2018 | Phase 3 |
| NCT04603911 | Active Recruiting |
Drug: Liposomal bupivacaine Drug: Bupivacaine, epinephrine, dexamethasone, and clonidine |
Breast Cancer | Tufts Medical Center | December 4, 2020 | Phase 2 |
| NCT03396588 | Active Recruiting |
Drug: Clonidine Drug: Morphine |
Neonatal Abstinence Syndrome | Henrietta Bada | December 7, 2017 | Phase 3 |
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