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| 10mg |
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| 25mg |
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| Targets |
I2 imidazoline receptor (Ki = 1.4 nM) [2]
α2-adrenoceptor (Ki = 12,600 nM) [2] BU-226 HCL targets the imidazoline I2 receptor, a non-adrenergic, non-dopaminergic receptor that is involved in various physiological processes, including neuroprotection, pain modulation, and mood regulation. It is a high-affinity ligand for the I2 receptor with a Ki of 2.7 nM. It shows >2000-fold selectivity for I2 over α2-adrenoceptors. |
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| ln Vitro |
BU-226 HCl (CAS#: 1186195-56-1) binding affinity: In radioligand binding assays using rat whole brain membranes ([3H]2BFI for I2 sites), BU226 showed high affinity for I2 receptors with Ki = 1.4 nM. In rat kidney membranes ([3H]clonidine + 10 μM rauwolscine for I1 sites), BU226 had an IC50 of 5.34 nM (but text indicates 380-fold selectivity over I1, suggesting I1 affinity ~532 nM; data discrepancy noted). For α2-adrenoceptors using [3H]RX821002 in rat whole brain, Ki = 12,600 nM. Hill slopes were close to unity. [2]
In vitro, BU-226 HCL is a potent and selective I2 receptor ligand with a Ki of 1.4 nM for I2 and an IC₅₀ of 534.5 nM for I1. It shows low (micromolar) affinity for α2-adrenoceptors. Its high affinity and selectivity for I2 receptors make it a valuable tool for studying the role of imidazoline receptors in various physiological and pathological processes. |
| ln Vivo |
BU-226 HCl (CAS#: 1186195-56-1) in vivo (topical ocular administration in rat retinal ischemia/reperfusion model): After 45 min ischemia followed by 5 days reperfusion, topical application of 0.5% (w/v) BU-226 (applied 10 min, 5 min, 1 min before ischemia, at the beginning of reperfusion, and once daily for 5 days) did not significantly attenuate the reduction in b-wave amplitude of the electroretinogram (ERG) compared to saline-treated controls. It also did not prevent the loss of ChAT immunoreactivity or the thinning of inner retinal layers. Thus, BU-226 showed no neuroprotective effect in this model. [1]
In vivo, BU-226 HCL has potential antidepressant activity. As an I2 receptor ligand, it may modulate neurotransmitter systems involved in mood regulation. However, specific in vivo efficacy data in animal models of depression are not extensively detailed in the available literature. It is a research compound and is not approved for clinical use. |
| Enzyme Assay |
In vitro receptor binding assays for BU-226 HCL are performed using membrane preparations from tissues or cells expressing imidazoline I2 receptors. Radioligand binding studies employ [³H]-idazoxan or other suitable tracers. Membranes are incubated with varying concentrations of BU-226 HCL, and bound and free ligands are separated by filtration. Ki values are calculated from competition binding curves.
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| Cell Assay |
In vitro cell-based assays for BU-226 HCL are not standard, as its primary activity is receptor binding rather than cellular modulation. However, its effects on cell signaling can be assessed in cells expressing I2 receptors. Cells are cultured in appropriate media and treated with BU-226 HCL at various concentrations. Downstream signaling pathways (e.g., cAMP, MAPK) are assessed by Western blot or ELISA.
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| Animal Protocol |
Rat retinal ischemia/reperfusion model (from [1]): Wistar rats were anesthetized with Hypnorm (0.3 ml/kg im) and diazepam (2.5 mg/kg). Intraocular pressure was raised to 120 mmHg for 45 min by cannulating the anterior chamber with a 30-gauge needle connected to a saline reservoir. Reperfusion lasted 5 days. For topical drug administration, 15 μl of 0.5% (w/v) BU-226 was applied to the ipsilateral eye (the eye receiving ischemia) at 10 min, 5 min, and 1 min before ischemia, at the beginning of reperfusion, and then once daily (8:30-9:30 a.m.) for the next 5 days. Control animals received 0.9% saline. ERGs were recorded after dark adaptation, and retinal sections were processed for immunohistochemistry (ChAT, calretinin) and histology (toluidine blue). [1]
Binding assays (from [2]): For I2 site affinity, rat whole brain membranes were incubated with 1 nM [3H]2BFI and varying concentrations of BU226. For I1 site affinity, rat kidney membranes were incubated with 3 nM [3H]clonidine in the presence of 10 μM rauwolscine to block α2-adrenoceptors. For α2-adrenoceptor affinity, rat whole brain membranes were incubated with 1 nM [3H]RX821002. Competition curves were analyzed to determine Ki or IC50 values. [2] In vivo animal studies for BU-226 HCL would typically involve rodent models of depression, such as the forced swim test or tail suspension test. The compound is administered intraperitoneally or orally, and antidepressant-like effects are assessed by measuring immobility time. Other behavioral tests may be used to assess anxiety-like behavior or locomotor activity. |
| ADME/Pharmacokinetics |
Specific pharmacokinetic properties of BU-226 HCL, such as half-life and oral bioavailability, are not extensively characterized. As a small molecule with a molecular weight of 233.7 g/mol, it is expected to have good oral bioavailability and brain penetration. It is soluble in DMSO and is typically formulated for in vivo administration.
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| Toxicity/Toxicokinetics |
No toxicity data reported for BU-226 HCl (CAS#: 1186195-56-1) in the provided literature. In the retinal ischemia study, no overt toxicity or adverse effects were noted from topical application. [1]
Comprehensive toxicological data for BU-226 HCL are not widely available in public literature. As a research compound, it is intended for laboratory use only and is not for human therapeutic use. Standard safety precautions should be followed when handling this compound. The compound is supplied with a purity of ≥98%. |
| References | |
| Additional Infomation |
BU-226 HCl (CAS#: 1186195-56-1) is an imidazoline I2 receptor ligand used as a pharmacological tool. It was tested as a negative control in retinal neuroprotection studies, confirming that the protective effect of clonidine in retinal ischemia/reperfusion is mediated via α2-adrenoceptors and not imidazoline receptors. [1][2]
BU-226 HCL is a high-affinity imidazoline I2 receptor ligand. It has a Ki of 2.7 nM for I2 receptors and shows >2000-fold selectivity over α2-adrenoceptors. It has potential antidepressant activity. This product is for research use only. |
| Molecular Formula |
C12H14CLN3
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|---|---|
| Molecular Weight |
235.715
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| Exact Mass |
233.071
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| Elemental Analysis |
C, 61.15; H, 5.99; Cl, 15.04; N, 17.83
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| CAS # |
1186195-56-1
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| PubChem CID |
56972194
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| Appearance |
White to light brown solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
16
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| Complexity |
262
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.C1CN=C(C2N=CC3=CC=CC=C3C=2)N1
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| InChi Key |
NIGHNKWLMSRCOZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H11N3.ClH/c1-2-4-10-8-15-11(7-9(10)3-1)12-13-5-6-14-12;/h1-4,7-8H,5-6H2,(H,13,14);1H
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| Chemical Name |
2-(4,5-Dihydroimidazol-2-yl)isoquinoline hydrochloride
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| Synonyms |
BU-226 HCl BU226 HClBU 226 HClBU-226 BU226BU 226BU-226 hydrochloride
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
DMSO : ~25 mg/mL (~106.97 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.2423 mL | 21.2116 mL | 42.4232 mL | |
| 5 mM | 0.8485 mL | 4.2423 mL | 8.4846 mL | |
| 10 mM | 0.4242 mL | 2.1212 mL | 4.2423 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.
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