| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Org 24461 (40 min) effectively inhibited glycine uptake in CHO cells stably expressing hGlyT-1b, with an IC50 value of 100 nM [1][2]. Org 24461 (0.1–30 μM; 20 min) reversed the prolongation of NMDA-mediated diffusion inhibition latency in isolated chicken retinas induced by 7-chlorokynuric acid (1), with an IC50 value of 0.36 μM, and in the absence of 7-chlorokynuric acid, Org 24461 (10–30 μM) shortened the NMDA-induced diffusion inhibition latency [1]. Org 24461 (0.3 mM; 90 min) effectively inhibited the release of [3H]glycine in isolated chicken retinas induced by oxygen-glucose deprivation, without affecting glycine efflux under basal normoxic conditions [2]. Org 24461 (pre-incubated for 5 minutes; incubated at 37°C for 10 minutes) effectively inhibited the uptake of high-affinity [3H]glycine by rat cortical synaptosomes (IC50 = 1.3 μM) and striatal synaptosomes (IC50 = 1.8 μM). Org 24461 inhibited the uptake of [3H]glycine in rat hippocampal P2 synaptosomes by an IC50 of 2.5 μM at low [3H]glycine concentrations and by an IC50 of 28 μM at high [3H]glycine concentrations [4]. Org 24461 did not affect the spontaneous efflux of [3H]glycine in perfused rat hippocampal slices, but inhibited the efflux of [3H]glycine stimulated by glycine in the same preparation [4].
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|---|---|
| ln Vivo |
Org 24461 (10 mg/kg; intraperitoneal injection; single dose) significantly reduced extracellular dopamine concentration in striatal cells of conscious rats, but had no effect on glutamate or serine levels [3]. Org 24461 (10 mg/kg; intraperitoneal injection; single dose; combined with risperidone 1 mg/kg intraperitoneal injection) restored extracellular dopamine concentration in striatal cells of conscious rats to normal, maintained high extracellular glycine concentration, and significantly increased extracellular glutamate concentration [3]. Org 24461 (2-8 mg/kg; intraperitoneal injection; single dose) inhibited PCP-induced kinesthesia in male NMRI mice, with an ID50 of 3.8 mg/kg intraperitoneal injection [4]. Org 24461 (3-30 mg/kg; intraperitoneal injection; single dose) inhibited D-amphetamine-induced kinesthesia in male NMRI mice, with an ID50 of 13.5 mg/kg (intraperitoneal injection) [4]. Org 24461 (1–10 mg/kg; intraperitoneal injection; single dose) dose-dependently reversed PCP-induced changes in electroencephalographic power spectrum in awake male Wistar rats [4]. Org 24461 (10 mg/kg; intravenous injection; single dose) significantly reversed L-701324-induced decrease in the firing rate of single neurons in the dorsal raphe nucleus of rats [5].
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| Animal Protocol |
Animal/Disease Models:NMRI (male, 25-33 g, phencyclidine/PCP-induced hyperperistalsis model) [4]
Doses: 2 mg/kg; 4 mg/kg; 8 mg/kg Route of Administration: Intraperitoneal injection; single dose Experimental Results: Dose-dependent inhibition of PCP-induced hyperperistalsis, ID50 value of 3.8 mg/kg (intraperitoneal injection) Animal/Disease Models:NMRI (male, 25-33 g, D-amphetamine-induced hyperperistalsis model) [4] Doses: 3 mg/kg; 10 mg/kg; 30 mg/kg Route of Administration: Intraperitoneal injection; Single dose Experimental Results: Dose-dependent inhibition of D-amphetamine-induced hyperperistalsis, ID50 value of 13.5 mg/kg (intraperitoneal injection) Animal/Disease Models:Wistar mice (male, 500 g, PCP-induced EEG power spectrum change model) [4] Doses: 1 mg/kg; 3 mg/kg; 10 mg/kg Route of Administration: Intraperitoneal injection; single dose Experimental Results: In the prefrontal cortex and sensorimotor cortex, the dose-dependent reduction in high-frequency (5-30 Hz) power induced by PCP was attenuated. In the prefrontal cortex, a 10 mg/kg intraperitoneal dose induced synchronous peaks in the 3-5 Hz and 8-20 Hz frequency bands. Animal/Disease Models:Wistar mice (male, 250-300 g, neuronal function decline induced by NMDA receptor glycine B site blockade) [5] Doses: 10 mg/kg Route of Administration: Intravenous injection; single dose Experimental Results: Reversed L-701324-induced inhibition of dorsal raphe nucleus neuronal firing, restoring the firing frequency from 3.64 Hz to near control levels (7.64 Hz vs. 7.92 Hz), which was statistically significant. The firing frequency increased within 1 minute after injection, peaked at 4-5 minutes, and then gradually decreased. When administered alone, there was a tendency to increase the firing frequency of dorsal raphe nucleus neurons, but this effect was not significant. |
| References |
|
| Molecular Formula |
C19H20F3NO3
|
|---|---|
| Molecular Weight |
367.36
|
| CAS # |
372198-80-6
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=C(CN(CCC(C1=CC=CC=C1)OC2=CC=C(C(F)(F)F)C=C2)C)O
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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 |
| 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
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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 | 2.7221 mL | 13.6106 mL | 27.2213 mL | |
| 5 mM | 0.5444 mL | 2.7221 mL | 5.4443 mL | |
| 10 mM | 0.2722 mL | 1.3611 mL | 2.7221 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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