| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
NMDA receptor NR1A/2B subunit (GluN2B-containing NMDA receptors). BZAD01 is a selective NMDA NR2B inhibitor (antagonist) with a Ki of 72 nM. It is a GluN2B subtype-selective NMDA antagonist. BZAD01 is orally bioactive, making it suitable for in vivo studies.
|
|---|---|
| ln Vitro |
BZAD01 selectively inhibits NMDA receptors containing the NR2B subunit with a Ki of 72 nM. The compound's selectivity for NR2B-containing NMDA receptors over other NMDA receptor subtypes makes it a valuable tool for studying the role of NR2B in neurological function and disease. BZAD01 improves postural asymmetry and apomorphine-induced rotation in animal models of Parkinson's disease.
|
| ln Vivo |
In vivo, BZAD01 has been evaluated in the unilateral 6-hydroxydopamine (6-OHDA) lesion rat model of Parkinson's disease. BZAD01 co-administration prevented chronic levodopa-induced potentiation of apomorphine rotation. However, levodopa-treated rats were slower than either controls or BZAD01-treated rats in the locomotor test. BZAD01 has also shown neuroprotective effects in the 6-OHDA rat model.
|
| Enzyme Assay |
In vitro receptor binding assays for BZAD01 involve measuring its affinity for NMDA NR2B-containing receptors using radioligand binding techniques. Membranes from cells or tissues expressing GluN2B-containing NMDA receptors are incubated with a radiolabeled NMDA ligand and increasing concentrations of BZAD01. Bound and free ligand are separated by filtration, and radioactivity is measured. Ki values (72 nM) are determined from competition binding curves.
|
| Cell Assay |
In vitro cellular assays for BZAD01 involve treating neuronal cells expressing NMDA receptors with the compound and measuring NMDA receptor-mediated calcium influx or electrophysiological responses. Cells are loaded with calcium-sensitive fluorescent dyes and treated with NMDA in the presence or absence of BZAD01. The compound's ability to inhibit NMDA-induced calcium influx is measured. These assays confirm the functional antagonism of BZAD01 at NR2B-containing NMDA receptors.
|
| Animal Protocol |
In vivo animal studies for BZAD01 typically involve administration to rodent models of Parkinson's disease. Parkinsonism is induced by microinjection of 6-hydroxydopamine (6-OHDA) into the medial forebrain bundle of Sprague-Dawley rats. Efficacy is assessed using a battery of behavioral tests including balance beam, apomorphine-induced rotation, body axis bias, head position bias, and disengage sensorimotor latency test. BZAD01 prevents chronic levodopa-induced potentiation of apomorphine rotation.
|
| ADME/Pharmacokinetics |
Pharmacokinetic studies of BZAD01 show that the compound is orally bioactive. BZAD01 has a LogP of 4.6 and is soluble in DMSO at 100 mg/mL (276.04 mM) and in methanol at 250 mg/mL (690.09 mM). The compound should be protected from light during transportation and storage. Powder is stable at -20°C for 3 years and at 4°C for 2 years.
|
| Toxicity/Toxicokinetics |
Preclinical toxicity studies of BZAD01 are limited. The compound has been evaluated in rat models of Parkinson's disease at doses that produce behavioral effects without overt toxicity. BZAD01 has shown neuroprotective effects in the 6-OHDA rat model. Comprehensive toxicological evaluation is needed to support clinical development. The compound's selectivity for NR2B-containing NMDA receptors may contribute to a more favorable side effect profile compared to non-selective NMDA antagonists.
|
| References | |
| Additional Infomation |
BZAD01 is a potent, selective, and orally bioactive NMDA NR2B inhibitor (antagonist) with a Ki of 72 nM. It is a GluN2B subtype-selective NMDA antagonist. BZAD01 improves postural asymmetry and apomorphine-induced rotation in animal models of Parkinson's disease. The compound has been studied for its potential in treating Parkinson's disease and other neurological conditions and has shown neuroprotective effects in the 6-OHDA rat model.
|
| Molecular Formula |
C16H12N2OF6
|
|---|---|
| Molecular Weight |
362.26968
|
| Exact Mass |
362.085
|
| CAS # |
305339-41-7
|
| PubChem CID |
9863769
|
| Appearance |
White to off-white solid powder
|
| LogP |
4.6
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
25
|
| Complexity |
455
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
N=C(C1=CC=C(OC(F)(F)F)C=C1)NCC2=CC=CC=C2C(F)(F)F
|
| InChi Key |
YGOCAMFQDLFNQK-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C16H12F6N2O/c17-15(18,19)13-4-2-1-3-11(13)9-24-14(23)10-5-7-12(8-6-10)25-16(20,21)22/h1-8H,9H2,(H2,23,24)
|
| Chemical Name |
4-(trifluoromethoxy)-N'-[[2-(trifluoromethyl)phenyl]methyl]benzenecarboximidamide
|
| Synonyms |
BZAD 01; BZAD-01; BZAD01
|
| 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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
MEthanol : ~250 mg/mL (~690.09 mM)
DMSO : ~100 mg/mL (~276.04 mM) |
|---|---|
| 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 | 2.7604 mL | 13.8019 mL | 27.6037 mL | |
| 5 mM | 0.5521 mL | 2.7604 mL | 5.5207 mL | |
| 10 mM | 0.2760 mL | 1.3802 mL | 2.7604 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
