| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| Other Sizes |
| Targets |
HexylHIBO targets the group I metabotropic glutamate receptors, mGlu1a and mGlu5a. These are G protein-coupled receptors that play important roles in synaptic plasticity, learning, and memory. It acts as an antagonist, blocking the activation of these receptors by glutamate. It shows weak or no activity at other mGluR subtypes, including group II (mGluR2) and group III (mGluR4a) receptors.
|
|---|---|
| ln Vitro |
As a result, ambient glutamate levels influence cortical excitability by potently activating mGluRs [1].
In vitro, HexylHIBO is a group I mGluR antagonist with Kb values of 140 µM at mGlu1a and 110 µM at mGlu5a receptors. It is selective for group I mGluRs over group II and III receptors. It shows no significant binding affinity for AMPA, NMDA, and kainate receptors. This selectivity profile makes it a useful tool for studying group I mGluR function. |
| ln Vivo |
In vivo, HexylHIBO has been shown to inhibit NMDA-induced seizures in mice when administered via intracerebroventricular (i.c.v.) injection at doses of 6.3 and 12.5 mg/kg. This suggests that group I mGluR antagonism can modulate glutamatergic transmission and seizure activity. Its effects in other in vivo models would be detailed in the primary literature.
|
| Enzyme Assay |
The binding affinity and functional activity of HexylHIBO are assessed using in vitro receptor binding and functional assays. Its affinity for mGlu1a and mGlu5a receptors is measured in radioligand binding assays, where its Kb (inhibition constant) values are determined. Its selectivity is confirmed by testing it against other mGluR subtypes and ionotropic glutamate receptors.
|
| Cell Assay |
The cellular activity of HexylHIBO is evaluated in cells expressing group I mGluRs. Its ability to antagonize receptor activation is assessed by measuring downstream signaling events, such as intracellular calcium mobilization or phosphoinositide hydrolysis. By blocking the receptor, it prevents glutamate-induced signaling, and its potency as an antagonist is determined.
|
| Animal Protocol |
In animal studies, HexylHIBO is typically administered via intracerebroventricular (i.c.v.) injection to directly target the central nervous system. In models of seizures, it is given prior to the seizure-inducing agent (e.g., NMDA), and its ability to inhibit seizure activity is assessed. The compound's effects on behavior and neurological function can be evaluated.
|
| ADME/Pharmacokinetics |
HexylHIBO has a molecular weight of 256.3 and a formula of C12H20N2O4. It is soluble in DMSO (100 mg/mL) and in 1M NaOH. It is recommended to be stored in a dark place at 2-8°C. Detailed pharmacokinetic parameters, such as half-life and bioavailability, are not extensively documented.
|
| Toxicity/Toxicokinetics |
Toxicology data for HexylHIBO is limited, as it is a research compound not intended for human use. Its safety profile has not been established in formal toxicology studies. Standard laboratory safety precautions should be followed when handling this compound.
|
| References |
|
| Additional Infomation |
HexylHIBO (CAS: 334887-43-3) is a valuable research tool for studying the role of group I metabotropic glutamate receptors. Its selectivity for mGlu1a and mGlu5a over other glutamate receptors makes it a useful compound for dissecting the specific functions of these receptors in the brain. It is used in neuroscience research to investigate synaptic plasticity, learning, memory, and neurological disorders.
|
| Molecular Formula |
C12H20N2O4
|
|---|---|
| Exact Mass |
256.142
|
| CAS # |
334887-43-3
|
| PubChem CID |
3984764
|
| Appearance |
Off-white to light yellow solid powder
|
| Density |
1.176 g/cm3
|
| LogP |
1.745
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
18
|
| Complexity |
352
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CCCCCCC1C(=O)NOC=1CC(C(=O)O)N
|
| InChi Key |
OKJBLHIYOWSQDJ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C12H20N2O4/c1-2-3-4-5-6-8-10(18-14-11(8)15)7-9(13)12(16)17/h9H,2-7,13H2,1H3,(H,14,15)(H,16,17)
|
| Chemical Name |
2-amino-3-(4-hexyl-3-oxo-1,2-oxazol-5-yl)propanoic acid
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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.) |
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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
