BTS 72664 (350 μM) weakly binds to voltage-gated sodium ion channels on the synaptosome membrane of rat brain, with a Ki value of 350 μM[1]. BTS 72664 (300 μM; 0–6 sec) significantly reduced the outflow of 86Rb+ from depolarized, calcium-exposed rat synaptosomes by up to 50%[1]. BTS 72664 inhibited veratrine-induced glutamate outflow from rat synaptosomes but did not affect basal outflow[1]. BTS 72664 (3–100 μM) reduced NMDA-induced depolarization in the wedge-shaped tissue of rat cerebral cortex by about 20% and had no significant activity against non-NMDA glutamate receptors[1]. BTS 72664 (0.3-300 μM) can reduce spontaneous epileptiform discharges in the wedge-shaped tissue of the rat cerebral cortex. Its inhibitory efficacy against coulin-induced spontaneous epileptiform discharges (SED) (frequency IC50 of 94 μM) is stronger than that against magnesium ion removal-induced SED (frequency IC50 of 189 μM) [1]. BTS 72664 (100 μM; 20-45 min) can cause a mean hyperpolarization of the resting membrane potential of CA1 pyramidal neurons in rat hippocampal slices by 9.5 mV [1]. BTS 72664 (10-100 μM) can reduce NMDA-induced currents in cultured Swiss mouse cortical neurons with an IC50 of 43 μM [1]. BTS 72664 (10-100 μM) enhances GABA-induced currents in cultured Swiss mouse cortical neurons via a benzodiazepine-independent, cucurbitacin-sensitive GABAA channel mechanism, producing a 511% enhancement at 100 μM [1].

BTS 72664 (1.9-9.4 mg/kg; orally; single dose; once daily; for 5 consecutive days) effectively protected mice from biscoline-induced seizures, with a peak ED50 of 1.9 mg/kg (orally), and no rapid tolerance was observed after 5 days of daily administration [1]. BTS 72664 (47.5-77.2 mg/kg; orally; single dose) protected mice from seizures induced by maximal dose electroshock, with a peak ED50 of 47.5 mg/kg (orally), and a duration of action of 4-6 hours, and its effect of raising the seizure threshold was stronger than its effect of inhibiting the generalization of seizures [1]. BTS 72664 (14 mg/kg; orally; single dose) protected mice from pentylenetetrazole-induced seizures, with an ED50 of 14 mg/kg (orally), and significantly raised the seizure threshold [1]. BTS 72664 (60 mg/kg; orally; single dose) protected mice from cucurbitacin-induced seizures with an ED50 of 60 mg/kg (orally) [1]. BTS 72664 (25 mg/kg; orally; single dose) protected mice from 4-aminopyridine-induced seizures with an ED50 of 25 mg/kg (orally) [1]. BTS 72664 (18 mg/kg; orally; single dose) protected mice from NMDA-induced seizures with an ED50 of 18 mg/kg (orally) [1]. BTS 72664 (9 mg/kg; orally; single dose) protected DBA/2 mice from auditory-induced seizures with an ED50 of 9 mg/kg (orally) [1]. BTS 72664 (29 mg/kg; orally; single dose) protected GEPR-9 rats from seizures with an ED50 of 29 mg/kg (orally) [1]. BTS 72664 (4.6 mg/kg; orally; single dose) protected rats from biscourin-induced seizures with an ED50 of 4.6 mg/kg (orally), with minimal interspecies efficacy compared to mice [1]. BTS 72664 (90 mg/kg; orally; single dose) protected rats from maximally induced seizures by electroconvulsive therapy with an ED50 of 90 mg/kg (orally), with minimal interspecies efficacy compared to mice [1]. BTS 72664 (100-150 mg/kg; orally; single dose) dose-dependently improved seizure parameters in amygdala-ignited rats, with an oral dose of 150 mg/kg increasing the seizure threshold by 177% and reducing seizure duration by 65% [1]. BTS 72664 (50 mg/kg; orally; every 12 hours; for a total of 4 doses), administered 15 minutes after vascular occlusion, reduced the volume of ischemic lesions in rats with permanent middle cerebral artery occlusion by 31% and accelerated their functional recovery [1]. In a rat model of permanent middle cerebral artery occlusion, BTS 72664 (20-35 mg/kg; intraperitoneally; single initial dose; every 12 hours; followed by 3 doses) administered 60 minutes after occlusion reduced the volume of ischemic lesions by 40%, and hypothermia did not contribute to neuroprotection [1]. Administration of BTS 72664 (50 mg/kg; orally; single dose) 15 minutes after cortical injury rapidly and persistently eliminated elevated levels of extracellular glutamate, glycine, and serine associated with cortical diffusion inhibition in rats [1].

Animal/Disease Models:Swiss CD1 Mice [1]
Doses: 1.9 mg/kg (30 minutes after administration); 9.4 mg/kg (60 minutes after administration); 2.8 mg/kg (long-term administration)
Route of Administration:Oral; Single dose; Oral; Once daily; For 5 consecutive days
Experimental Results:Oral administration of 1.9 mg/kg prevented biscourin-induced seizures, with an ED50 of 1.9 mg/kg 30 minutes after administration. Oral administration of 9.4 mg/kg prevented biscourin-induced seizures, with an ED50 of 9.4 mg/kg 60 minutes after administration. Compared with a single dose, continuous oral administration of 2.8 mg/kg for 5 days did not significantly reduce the anticonvulsant efficacy.

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Animal/Disease Models:Swiss CD1 Mice [1]
Doses: 47.5 mg/kg (30 minutes after administration); 77 mg/kg (60 minutes after administration); 77.2 mg/kg (peak protection)
Route of Administration: Oral; Single Dosage
Experimental Results: 30 minutes after administration, oral administration of 47.5 mg/kg effectively protected mice from seizures induced by maximal electroshock. 60 minutes after administration, oral administration of 77 mg/kg effectively protected mice from seizures induced by maximal electroshock. Peak protection against seizures induced by maximal electroshock was provided 30 minutes after administration, with a duration of action of 4-6 hours, at a dose of 77.2 mg/kg orally. TID20 at 5.7 mg/kg orally increased the epileptic current threshold by 20%.

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Animal/Disease Models:Swiss CD1 mice [1]
Doses: 14 mg/kg
Route of Administration: Oral; Single dose
Experimental Results: Oral administration of 14 mg/kg prevented subcutaneous pentylenetetrazol-induced seizures. Oral administration of 5.6 mg/kg increased the initial myoclonic threshold of pentylenetetrazol-induced seizures by 20% (TID20). Oral administration of 1.1 mg/kg increased the threshold of generalized tonic-clonic seizures induced by pentylenetetrazol by 20%.

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Animal/Disease Models:Swiss CD1 mouse [1]
Doses: 60 mg/kg
Route of Administration: Oral; single dose
Experimental Results: Oral ED50 of 60 mg/kg can prevent epileptic seizures caused by subcutaneous injection of bitter substances.

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Animal/Disease Models:Swiss CD1 mouse [1]
Doses: 25 mg/kg
Route of Administration: Oral; single dose
Experimental Results: Oral administration of 25 mg/kg of ED50 prevented intraventricular injection of 4-aminopyridine-induced seizures.

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Animal/Disease Models:Swiss CD1 mouse [1]
Doses: 18 mg/kg
Route of Administration: Oral; single dose
Experimental Results: Oral ED50 of 18 mg/kg can prevent intraventricular NMDA-induced seizures.

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Animal/Disease Models:DBA/2 Mice [1]
Doses: 9 mg/kg
Route of Administration: Oral; Single Dosage
Experimental Results: Oral administration of 9 mg/kg had a protective effect against auditory epilepsy in DBA/2 mice, with an ED50 of 9 mg/kg.

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Animal/Disease Models:GEPR-9 rats [1]
Doses: 29 mg/kg
Route of Administration: Oral; Single dose
Experimental Results: The ED50 of the oral dose was 29 mg/kg, which had a protective effect against epilepsy in GEPR-9 rats.

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Animal/Disease Models:Rats [1]
Doses: 4.6 mg/kg
Route of Administration: Oral; Single dose
Experimental Results: Oral ED50 of 4.6 mg/kg protected rats from bispus-induced seizures.

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Animal/Disease Models:Rat [1]
Doses: 90 mg/kg
Route of Administration: Oral; Single dose
Experimental Results: Oral ED50 of 90 mg/kg protected rats from seizures induced by maximal electroshock.

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Animal/Disease Models:Rats [1]
Doses: 100 mg/kg; 150 mg/kg
Route of Administration: Oral; Single Dosage
Experimental Results: 100 mg/kg oral dose increased the mean ignition threshold by 68% 150 mg/kg oral dose increased the mean ignition threshold by 177% 150 mg/kg oral dose reduced the mean seizure severity by 59% 150 mg/kg oral dose reduced the mean seizure duration by 65% (from 69 seconds to 24 seconds) 150 mg/kg oral dose reduced the mean post-discharge duration by 68% (from 105 seconds to 34 seconds) 150 mg/kg oral dose caused mild ataxia, but no significant motor impairment was observed in the rotarod test.

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Animal/Disease Models:Rats [1]
Doses: 50 mg/kg
Route of Administration: Oral; every 12 hours; 4 times in total
Experimental Results: Two days after injury, brain volume was reduced by 31% (treatment group: 56.9 mm3; control group: 82.6 mm3). On day 8 after injury, and when data from days 3, 6 and 8 were combined, the treatment group showed a significant reduction in contralateral forelimb dysfunction compared to the control group.

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Animal/Disease Models:Rats [1]
Doses: 20 mg/kg (subsequent doses); 35 mg/kg (initial dose)
Route of Administration: Intraperitoneal injection; single initial dose; intraperitoneal injection; every 12 hours; 3 subsequent doses
Experimental Results: Six days after injury, brain lesion volume decreased by 40% (treatment group: 43.6 mm3; control group: 72.0 mm3). No decrease in core body temperature was observed 18 hours after the first intraperitoneal injection of 35 mg/kg.

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Animal/Disease Models:Rats [1]
Doses: 50 mg/kg
Route of Administration: Oral; single dose
Experimental Results: Eliminated transient increases in extracellular glutamate, glycine, and serine levels in the parietal cortex caused by injury. Did not alter extracellular GABA levels, but reduced extracellular glutamate levels compared to the control group treated with anesthetic alone. Rapid onset of action (30 minutes after administration) and lasted at least 2.25 hours from peak levels in the brain.

[1]. BTS 72664-- a novel CNS drug with potential anticonvulsant, neuroprotective, and antimigraine properties. CNS Drug Rev. 2001;7(2):146-171.

C13H11CLN4O

274.71

165383-52-8

Typically exists as solids at room temperature

ClC(C=C1)=CC=C1O[C@@H](C2=CC=NC3=NC=NN23)C

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

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

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.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*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).

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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)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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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).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)