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imidazoline I2 receptors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Imidazoline Receptor (11) 5-HT Receptor (1) Adrenergic Receptor (3) Apoptosis (2) Histamine Receptor (1) Reference Standards (2) TNF Receptor (2)
By Research Areas:	Inflammation/Immunology (7) Neurological Disease (11)

Targets Recommended: Imidazoline Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-100904

RX 801077 hydrochloride 1 Publications Verification 2 BFI	Imidazoline Receptor	Neurological Disease Inflammation/Immunology
RX 801077 hydrochloride (2 BFI) is a selective **imidazoline I2 receptor (I2R) agonist with a K_i** value of 70.1 nM. RX 801077 hydrochlorideshows anti-inflammation and neuroprotection. RX 801077 hydrochloride has the potential for the research of traumatic brain injury (TBI) .

HY-101170

BU224 hydrochloride	Imidazoline Receptor Apoptosis TNF Receptor	Neurological Disease Inflammation/Immunology
BU224 hydrochloride is a selective and high affinity **imidazoline I₂ receptor ligand, with a K_i** of 2.1 nM. BU224 hydrochloride is sometimes used as an I₂ receptor antagonist. BU224 hydrochloride exerts neuroprotective effects, with anti-inflammatory and anti-apoptotic properties. BU224 hydrochloride improves memory in 5XFAD mice, enlarging dendritic spines and reducing Aβ-induced changes in NMDARs. BU224 hydrochloride can be used for Alzheimer's disease research .

HY-14561

Idazoxan RX 781094	Adrenergic Receptor Imidazoline Receptor	Neurological Disease
Idazoxan (RX 781094) is a potent antagonist of *α2 adrenergic receptor* (α2AR) and potential I2 imidazoline receptor** agonist. Idazoxan can be used in the research of antidepression and schizophrenia. Idazoxan has oral bioactivity .

HY-101380A

BU226 hydrochloride	Imidazoline Receptor	Neurological Disease
BU226 hydrochloride is a selective **imidazoline 2 (I₂) receptors ligand with an K_i of 1.4 nM for I₂ and an IC₅₀** of 534.5 nM for I₁. BU226 hydrochloride can be used for researching antidepressant .

HY-W714108

Metrazoline o-Methyl-tracizoline	Imidazoline Receptor Adrenergic Receptor	Neurological Disease
Metrazoline (o-Methyl-tracizoline) is the ligand for adrenergic receptor (low affinity) and **imidazoline I2 receptor** .

HY-170994

I2-IRs ligand-1	Imidazoline Receptor	Neurological Disease Inflammation/Immunology
I2-IRs ligand-1 (Compound 12d) is an orally active and BBB-penetrable compound. I2-IRs ligand-1 has a high affinity for imidazoline I₂ receptors (I₂-IRs) (pK_i: 9.98). I2-IRs ligand-1 can improve cognitive impairment in senescent mice and exhibits analgesic, anti-inflammatory, and neuroprotective activities. I2-IRs ligand-1 can be used for the research of Alzheimer's disease and related pain disorders .

HY-100904A

RX 801077 2 BFI free base	Imidazoline Receptor	Neurological Disease Inflammation/Immunology
RX 801077 (2 BFI free base) is a selective **imidazoline I2 receptor (I2R) agonist with a K_i** value of 70.1 nM. RX 801077 shows anti-inflammation and neuroprotection. RX 801077 has the potential for the research of traumatic brain injury (TBI) .

HY-101170R

BU224 hydrochloride (Standard)	Reference Standards Imidazoline Receptor Apoptosis TNF Receptor	Neurological Disease Inflammation/Immunology
BU224 (hydrochloride) (Standard) is the analytical standard of BU224 (hydrochloride). This product is intended for research and analytical applications. BU224 hydrochloride is a selective and high affinity imidazoline I2 receptor ligand, with a Ki of 2.1 nM. BU224 hydrochloride is sometimes used as an I2 receptor antagonist. BU224 hydrochloride exerts neuroprotective effects, with anti-inflammatory and anti-apoptotic properties. BU224 hydrochloride improves memory in 5XFAD mice, enlarging dendritic spines and reducing Aβ-induced changes in NMDARs. BU224 hydrochloride can be used for Alzheimer's disease research .

HY-W182790

Garsevil LSL 60101
Garsevil (LSL 60101) is a biphasic, selective imidazoline I₂ receptor (I₂-IR) ligand, with a pK_i of 9.03 and a K_i of 0.9 nM at the high-affinity site, and a pK_i of 5.25 and a K_i of 5.6 nM at the low-affinity site. Garsevil is applicable to research related to Alzheimer's disease .

HY-101301A

RS 45041-190 hydrochloride	Imidazoline Receptor	Neurological Disease
RS 45041-190 hydrochloride is a high-affinity ligand for I2 imidazoline receptors, with the pK_is of 8.66, 9.37, 9.32, and 8.85 in rat, rabbit, dog and baboon kidney, respectively. RS 45041-190 hydrochloride shows moderate potency for the inhibition of monoamine oxidase A in vitro (pIC₅₀= 6.12), but had much lower potency for monoamine oxidase B (pIC₅₀ = 4.47) .

HY-182597

Tracizoline	Imidazoline Receptor 5-HT Receptor Adrenergic Receptor	Neurological Disease
Tracizoline is an orally active **I2-imidazoline receptor** agonist. Tracizoline functionally modulates I2-imidazoline receptors, regulates hippocampal FADD cell fate adaptor, attenuates mechanical and thermal hyperalgesia, activates α₂A-adrenergic receptors with very weak partial agonism, and induces antidepressant-like activity via 5-HT₁A receptor activation. Tracizoline can be used for the research of inflammatory pain, neuropathic pain, and depression .

HY-100904R

RX 801077 hydrochloride (Standard) 2 BFI (Standard)	Imidazoline Receptor Reference Standards	Neurological Disease Inflammation/Immunology
RX 801077 (hydrochloride) (Standard) is the analytical standard of RX 801077 (hydrochloride) (HY-100904). This product is intended for research and analytical applications. RX 801077 hydrochloride (2 BFI) is a selective imidazoline I2 receptor (I2R) agonist with a Ki value of 70.1 nM. RX 801077 hydrochlorideshows anti-inflammation and neuroprotection. RX 801077 hydrochloride has the potential for the research of traumatic brain injury (TBI) .

HY-182296

SCH 79687	Histamine Receptor	Inflammation/Immunology
SCH 79687 is an orally active histamine H3 receptor antagonist, with a K_i of 1.9 nM in rats and 13 nM in guinea pigs. SCH 79687 acts as a competitive antagonist against (R)-α-methylhistamine. SCH 79687 attenuates the inhibitory effect of (R)-α-methylhistamine-induced sympathetic hypertensive responses in guinea pigs. When used in combination with H1 antagonists, SCH 79687 inhibits Compound 48/80 (HY-115768)-induced nasal congestion in cats. SCH 79687 can be used for the research of allergic rhinitis .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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imidazoline I2 receptors

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