| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Ki: 70.1 nM (imidazoline I2 receptor)[1]
Imidazoline I2 receptor (I2R). RX 801077 hydrochloride is a selective agonist at this receptor. |
|---|---|
| ln Vitro |
RX 801077 hydrochloride (2 BFI) is a selective imidazoline I2 receptor agonist with a Ki of 70.1 nM (or 9.8 nM in some reports). It has been shown to possess anti-inflammatory and neuroprotective effects. The compound enhances supraspinal morphine analgesia in mice.
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| ln Vivo |
In a rat model of traumatic brain injury, RX 801077 hydrochloride (5, 10, 20 mg/kg; intraperitoneal injection; twice daily for 3 days) suppresses the NLRP3 inflammasome-induced inflammation and necroptosis[2].
In vivo, RX 801077 hydrochloride has been studied for its potential therapeutic applications in traumatic brain injury (TBI). Its anti-inflammatory and neuroprotective effects suggest that it may be beneficial in conditions characterized by neuroinflammation and neuronal injury. The compound has also been shown to enhance supraspinal morphine analgesia in mice. |
| Enzyme Assay |
In vitro receptor binding assays for RX 801077 hydrochloride are performed to evaluate its affinity for the imidazoline I2 receptor. Radioligand binding studies using membrane preparations from cells or tissues expressing the I2 receptor are conducted. The compound's ability to displace a specific radiolabeled I2 receptor ligand is measured to calculate its Ki value.
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| Cell Assay |
In vitro cell-based assays are conducted using cells expressing the imidazoline I2 receptor. The cells are treated with RX 801077 hydrochloride, and receptor activation is measured by assessing downstream signaling events. The compound's anti-inflammatory and neuroprotective effects can be evaluated in cell culture models of inflammation and oxidative stress.
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| Animal Protocol |
Animal/Disease Models: 280-300 g, Male adult SD (Sprague-Dawley) rats (TBI model)[2]
Doses: 5, 10, 20 mg/kg Route of Administration: Ip; twice (two times) daily for 3 days Experimental Results: Attenuated neurological deficits, brain edema, BBB permeability and cortical tissue loss in a rat model of TBI, decreased microglial activation, neutrophil infiltration, and proinflammatory cytokine IL-1β secretion, decreased the expression of RIP1 and RIP3 in neurons in the pericontusional cortex. In vivo studies are conducted in animal models to evaluate the effects of RX 801077 hydrochloride on neuroprotection, inflammation, and pain. The compound is administered via various routes, and its effects on neurological outcomes, inflammatory markers, and pain responses are assessed. In traumatic brain injury models, the compound's neuroprotective effects are evaluated. |
| ADME/Pharmacokinetics |
No detailed pharmacokinetic data are publicly available for RX 801077 hydrochloride. As a research compound, its ADME properties would be characterized in standard preclinical studies to guide in vivo experiments. The compound has a LogP of 1.547, indicating moderate lipophilicity.
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| Toxicity/Toxicokinetics |
No specific toxicity data are publicly available for RX 801077 hydrochloride. As a selective imidazoline I2 receptor agonist, its toxicity profile would be expected to be related to its mechanism of action. Standard safety assessments would be required for any therapeutic development.
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| References | |
| Additional Infomation |
RX 801077 hydrochloride (2 BFI) is a selective imidazoline I2 receptor agonist with anti-inflammatory and neuroprotective effects. It has been studied for potential therapeutic applications in traumatic brain injury and pain modulation. The compound is not approved for human therapeutic use and is strictly for research purposes. It has the CAS number 89196-95-2.
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| Molecular Formula |
C11H11CLN2O
|
|---|---|
| Molecular Weight |
222.67
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| Exact Mass |
222.056
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| CAS # |
89196-95-2
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| Related CAS # |
RX 801077;72583-92-7
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| PubChem CID |
45073465
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| Appearance |
White to off-white solid powder
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| Boiling Point |
348.1ºC at 760 mmHg
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| Flash Point |
164.4ºC
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| LogP |
2.349
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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 |
15
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| Complexity |
252
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CN=C(N1)C2=CC3=CC=CC=C3O2.Cl
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| InChi Key |
RFNFFVDVGWOSNZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H10N2O.ClH/c1-2-4-9-8(3-1)7-10(14-9)11-12-5-6-13-11;/h1-4,7H,5-6H2,(H,12,13);1H
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| Chemical Name |
2-(1-benzofuran-2-yl)-4,5-dihydro-1H-imidazole;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, avoid exposure to moisture. |
| 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: 20.83 mg/mL (93.55 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 | 4.4910 mL | 22.4548 mL | 44.9095 mL | |
| 5 mM | 0.8982 mL | 4.4910 mL | 8.9819 mL | |
| 10 mM | 0.4491 mL | 2.2455 mL | 4.4910 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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