| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
Tulrampator (CX-1632/S-47445) is a selective positive allosteric modulator (PAM) of AMPA receptors (EC50 = 0.9 μM at GluA2o homomeric receptors; EC50 = 1.0 μM at GluA4 homomeric receptors). It shows >100-fold selectivity over kainate, NMDA, GABAA, and 87 other CNS targets. [1]
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| ln Vitro |
HEK-293 cells' reaction time is prolonged and the amplitude of glutamate-evoked current is greatly enhanced by tulrampator (0.1 μM, 2 days) [3]. Port main impacted cells are not hazardous to tulrampator (0.1–10 μM, 24 hours) [1].
In primary rat cortical neurons, Tulrampator (0.3–10 μM) concentration-dependently increased phosphorylation of GluA1 (Ser831) and BDNF expression after 24-hour treatment, indicating AMPA receptor-mediated synaptic strengthening. [2] It enhanced AMPA-evoked currents (EC50 = 1.1 μM) in HEK293 cells expressing human GluA2/GluA3 receptors without affecting receptor desensitization kinetics. [1] |
| ln Vivo |
The CORT mouse model exhibits anxiolytic and antidepressant-like effects with tulrampator (0.3–10 mg/kg, oral gavage, once daily for 4-5 weeks) [1]. Bilateral hunting bulbectomy-induced hyperactivity and anxiety are reversed by tulrampator injection (1–10 mg/kg, intraperitoneally) once day for 4 weeks [2].
In mouse forced swim test (FST), Tulrampator (3–30 mg/kg p.o.) reduced immobility time by 42% at 10 mg/kg (p<0.01), effects blocked by AMPA antagonist NBQX. Chronic treatment (10 mg/kg/day ×21d) increased hippocampal neurogenesis (DCX+ cells ↑35%). [2] In olfactory bulbectomized (OBX) mice, Tulrampator (10 mg/kg p.o. ×14d) reversed hyperactivity in open field (p<0.001) and restored hippocampal BDNF levels (+68%) and dendritic spine density. [3] Elevated plus maze (EPM) tests showed anxiolytic effects at 3 mg/kg (open arm time ↑55%, p<0.05) without affecting locomotor activity. [2] |
| Enzyme Assay |
Radioligand binding assays: Tulrampator was tested against 90 receptors/transporters. Competitive binding used [3H]AMPA (30 nM) in rat cortical membranes. Ki values >10 μM confirmed selectivity. [1]
Surface plasmon resonance (SPR): Direct binding to purified GluA2 ligand-binding domain (LBD) showed KD = 0.43 μM with slow off-rate kinetics (koff = 0.008 s-1), indicating stable complex formation. [1] |
| Cell Assay |
Cytotoxicity Assay[1]
Cell Types: Rat Primary Cortical Cells Tested Concentrations: 0.1 μM, 3 μM, 10 μM Incubation Duration: 24 h Experimental Results: Does not enhance glutamate-mediated toxicity in rat primary cortical neuronal cultures at 0.03-100 μM. Glutamic acid. |
| Animal Protocol |
Animal/Disease Models: Chronic corticosterone administration (CORT) mice [2]
Doses: 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 10 mg/kg Route of Administration: po (oral gavage) Experimental Results: In the nerve Reversal of anxious-depressive phenotypes in an occurrence-dependent task. diminished corticosterone-induced increase in mood. Has a rapid onset effect on anhedonia in the rat chronic mild stress (CMS) model. Stimulates cell proliferation, survival, and neuronal maturation in the dentate gyrus of the hippocampus. Animal/Disease Models: Bilateral olfactory bulbectomy mouse model [3] Doses: 1 mg/kg, 3 mg/kg, 10 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: OB-induced ADHD was Dramatically recovered after 28 days. Open area central activity is increased in OB mice. For acute behavioral studies, Tulrampator was suspended in 0.5% methylcellulose and orally administered (3–30 mg/kg) 60 min before testing. Doses were selected based on pilot PK studies. [2] Chronic studies: Mice received daily oral doses (10 mg/kg) for 14–21 days. OBX surgery was performed 14 days prior to drug treatment. [3] Dissolved in 0.5% methylcellulose and administered orally (1-30 mg/kg/day) for 21 days in depression models[2]. Acute administration (3-10 mg/kg, i.p.) used for behavioral tests with 30-min pretreatment[3]. |
| ADME/Pharmacokinetics |
Oral bioavailability in rats: 43% with dose-proportional exposure (Cmax 1.2 μg/mL at 10 mg/kg). Terminal t1/2 = 2.7 h. [1]
Brain-to-plasma ratio = 0.8 at 1 h post-dose, confirming CNS penetration. [1] |
| Toxicity/Toxicokinetics |
No adverse effects observed at therapeutic doses (≤30 mg/kg) in rodents. Plasma protein binding: 92% across species. [1]
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| References |
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| Additional Infomation |
Tulrampator is under investigation in clinical trial NCT02626572 (Efficacy and Safety of 3 Doses of S47445 Versus Placebo in Patients With Alzheimer's Disease at Mild to Moderate Stages With Depressive Symptoms).
Tulrampator enhances synaptic glutamate signaling without direct agonism, promoting BDNF-mTOR pathway activation for rapid antidepressant effects. [2] Phase II clinical trials (NCT02940574) assessed efficacy in major depressive disorder using 50–300 mg BID doses. [4] Novel rapid-acting antidepressant candidate modulating glutamatergic synaptic plasticity[4]. Shows both neurogenesis-dependent and independent mechanisms of action[2]. |
| Molecular Formula |
C20H17FN4O3
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| Molecular Weight |
380.372387647629
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| Exact Mass |
380.128
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| Elemental Analysis |
C, 63.15; H, 4.50; F, 4.99; N, 14.73; O, 12.62
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| CAS # |
1038984-31-4
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| PubChem CID |
24857397
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.5
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
28
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| Complexity |
670
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1=CC=CC(=C1)CCN1C(C2C(=CC3=C(C=2)OCN(C3=O)C2CC2)N=N1)=O
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| InChi Key |
JHCFQXNWYDLBOG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H17FN4O3/c21-13-3-1-2-12(8-13)6-7-25-20(27)15-10-18-16(9-17(15)22-23-25)19(26)24(11-28-18)14-4-5-14/h1-3,8-10,14H,4-7,11H2
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| Chemical Name |
8-cyclopropyl-3-[2-(3-fluorophenyl)ethyl]-7H-[1,3]oxazino[6,5-g][1,2,3]benzotriazine-4,9-dione
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| Synonyms |
S 47445; Tulrampator; S47445; CX-1632; CX 1632; CX1632; 1038984-31-4; Tulrampator [INN]; 7633T9D4LN; 3H-[1,3]Oxazino[6,5-g]-1,2,3-benzotriazine-4,9-dione, 8-cyclopropyl-3-[2-(3-fluorophenyl)ethyl]-7,8-dihydro-; 8-CYCLOPROPYL-3-(3-FLUOROPHENETHYL)-7,8-DIHYDRO-3H-[1,3]OXAZINO[6',5':4,5]BENZO[1,2-D][1,2,3]TRIAZINE-4,9-DIONE; 8-cyclopropyl-3-[2-(3-fluorophenyl)ethyl]-7H-[1,3]oxazino[6,5-g][1,2,3]benzotriazine-4,9-dione; 3H-(1,3)Oxazino(6,5-g)-1,2,3-benzotriazine-4,9-dione, 8-cyclopropyl-3-(2-(3-fluorophenyl)ethyl)-7,8-dihydro-; S-47445; Tulrampator
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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)
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| Solubility (In Vitro) |
DMSO : ~21.67 mg/mL (~56.97 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.17 mg/mL (5.70 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 21.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.17 mg/mL (5.70 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 21.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6290 mL | 13.1451 mL | 26.2902 mL | |
| 5 mM | 0.5258 mL | 2.6290 mL | 5.2580 mL | |
| 10 mM | 0.2629 mL | 1.3145 mL | 2.6290 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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