| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
GlyT1 Inhibitor 1 targets GlyT1, a sodium- and chloride-dependent glycine transporter responsible for the reuptake of glycine from the synaptic cleft. Inhibition of GlyT1 increases synaptic glycine levels, which enhances NMDA receptor function and has potential antipsychotic and neurological applications.
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| ln Vitro |
In vitro, GlyT1 Inhibitor 1 potently inhibits rGlyT1 with an IC₅0 of 38 nM. The compound belongs to a novel pyrrolo[3,4-c]pyrazole amide chemotype and has demonstrated antipsychotic activity in preclinical models.
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| ln Vivo |
Following oral dosing at 0.1, 1, and 3 mg/kg, compound 46, also known as GlyT1 inhibitor 1, demonstrated in vivo efficacy in the rat new object recognition (NOR) assay [1].
In vivo, GlyT1 Inhibitor 1 (10 mg/kg, oral administration) elevates glycine levels in rat cerebrospinal fluid (CSF). This pharmacodynamic effect confirms target engagement and supports the compound's potential for treating neurological disorders associated with NMDA receptor hypofunction, such as schizophrenia. |
| Enzyme Assay |
For in vitro enzyme/receptor binding assays, GlyT1 Inhibitor 1 is evaluated using radioligand binding or functional uptake assays with recombinant rat GlyT1 expressed in appropriate cell lines. The compound is incubated with the transporter and a labeled substrate (e.g., [3H]-glycine), and the inhibition of glycine uptake is measured to determine IC₅0 values.
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| Cell Assay |
For in vitro cellular assays, GlyT1 Inhibitor 1 is dissolved in DMSO and applied to cells expressing recombinant GlyT1. Glycine uptake is measured using radiolabeled glycine or fluorescent glycine analogs. The compound's potency is determined by measuring the concentration-dependent inhibition of glycine transport.
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| Animal Protocol |
In vivo animal studies with GlyT1 Inhibitor 1 typically involve oral administration in rats. A common protocol includes dosing at 10 mg/kg, followed by collection of cerebrospinal fluid at various time points to measure glycine elevation as a pharmacodynamic marker of GlyT1 inhibition.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for GlyT1 Inhibitor 1 are limited. The compound has a molecular weight of 387.43 and is soluble in DMSO at 20 mg/mL. It should be stored as a powder at -20degC for up to 3 years or in solvent at -80degC for 1 year.
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| Toxicity/Toxicokinetics |
Toxicology data for GlyT1 Inhibitor 1 are not extensively reported. As a research compound targeting neurotransmitter transporters, it is intended for laboratory use only and should be handled with appropriate safety precautions. No clinical toxicity data are available.
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| References | |
| Additional Infomation |
GlyT1 Inhibitor 1 (CAS#: 1820934-93-7) has the molecular formula C22H21N₅O2 and molecular weight 387.43. The compound is a selective and potent GlyT1 inhibitor with reported antipsychotic activity. It is supplied as a research reagent and is not approved for human therapeutic use.
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| Molecular Formula |
C22H21N5O2
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|---|---|
| Molecular Weight |
387.434444189072
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| Exact Mass |
387.169
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| CAS # |
1820934-93-7
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| PubChem CID |
118479295
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| Appearance |
White to off-white solid powder
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| LogP |
2.3
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
29
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| Complexity |
646
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1C=C(C#N)C=CC=1OC(C)C)N1CC2C(=CN(C3C=CN=C(C)C=3)N=2)C1
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| InChi Key |
CIEHAYBWEMOJMN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H21N5O2/c1-14(2)29-21-5-4-16(10-23)9-19(21)22(28)26-11-17-12-27(25-20(17)13-26)18-6-7-24-15(3)8-18/h4-9,12,14H,11,13H2,1-3H3
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| Chemical Name |
3-[2-(2-methylpyridin-4-yl)-4,6-dihydropyrrolo[3,4-c]pyrazole-5-carbonyl]-4-propan-2-yloxybenzonitrile
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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 : ~25 mg/mL (~64.53 mM)
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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 | 2.5811 mL | 12.9056 mL | 25.8111 mL | |
| 5 mM | 0.5162 mL | 2.5811 mL | 5.1622 mL | |
| 10 mM | 0.2581 mL | 1.2906 mL | 2.5811 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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