| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
Glycine Transporter 2 (GlyT2) [1][2]
|
|---|---|
| ln Vivo |
Intrathecal administration of ALX1393 (10–30 nmol) in rats significantly increased paw withdrawal thresholds to mechanical stimuli (von Frey test) and reduced formalin-induced Phase 2 flinching behavior, indicating potent antinociception in acute pain models. This effect was blocked by the glycine receptor antagonist strychnine. [1]
Intracerebroventricular (i.c.v.) injection of ALX1393 (0.1–10 μg) in rats attenuated thermal hyperalgesia in the Complete Freund's Adjuvant (CFA)-induced inflammatory pain model and mechanical allodynia in the sciatic nerve ligation-induced neuropathic pain model. Efficacy was stronger in inflammatory pain than neuropathic pain. [2] ALX1393 (icv; 25, 50, and 100 μg) in normal rats suppresses late-phase responses in the formalin test but does not impact locomotor performance. ALX1393 reduces mechanical hyperalgesia and cold hyperalgesia in a dose-dependent manner [2]. |
| Animal Protocol |
Acute pain (Formalin test): Rats received intrathecal (i.t.) injections of ALX1393 (3–30 nmol) dissolved in saline via lumbar puncture (L5–L6). Nociceptive behaviors (flinching/lifting) were quantified 0–60 min post-formalin injection. [1]
Inflammatory/Neuropathic pain: Rats underwent i.c.v. cannulation. ALX1393 (0.1–10 μg in saline) was administered 14 days post-CFA injection (inflammatory) or 7 days post-nerve ligation (neuropathic). Pain thresholds were assessed via plantar test (thermal) and von Frey filaments (mechanical). [2] |
| References |
|
| Additional Infomation |
ALX1393 exerts antinociception by inhibiting GlyT2 in the spinal cord, thereby increasing synaptic glycine levels and enhancing glycinergic inhibitory neurotransmission. This mechanism is validated by strychnine reversibility. [1]
The differential efficacy of i.c.v.-administered ALX1393 in inflammatory vs. neuropathic pain suggests region-specific GlyT2 modulation in supraspinal pain pathways. Notably, it did not impair motor function (rotarod test). [2] CNS-penetrant GlyT2 inhibitor showing superior efficacy in neuropathic vs inflammatory pain models [2]. |
| Molecular Formula |
C23H22FNO4
|
|---|---|
| Molecular Weight |
395.423490047455
|
| Exact Mass |
395.153
|
| Elemental Analysis |
C, 69.86; H, 5.61; F, 4.80; N, 3.54; O, 16.18
|
| CAS # |
949164-09-4
|
| Related CAS # |
ALX-1393 TFA
|
| PubChem CID |
16078939
|
| Appearance |
White to off-white solid powder
|
| LogP |
4.622
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
29
|
| Complexity |
499
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
C1=CC=C(C=C1)COC2=CC=CC=C2C(C3=CC(=CC=C3)F)OC[C@@H](C(=O)O)N
|
| InChi Key |
ADUSZEGHFWRTQS-AIBWNMTMSA-N
|
| InChi Code |
InChI=1S/C23H22FNO4/c24-18-10-6-9-17(13-18)22(29-15-20(25)23(26)27)19-11-4-5-12-21(19)28-14-16-7-2-1-3-8-16/h1-13,20,22H,14-15,25H2,(H,26,27)/t20-,22?/m0/s1
|
| Chemical Name |
(2S)-2-amino-3-[(3-fluorophenyl)-(2-phenylmethoxyphenyl)methoxy]propanoic acid
|
| Synonyms |
ALX-1393; ALX 1393; ALX1393; O-[2-benzyloxyphenyl-3-flurophenyl]methyl-L-serine; O-(2-benzyloxyphenyl-3-flurophenyl)methyl-L-serine; 949164-09-4; (2S)-2-amino-3-{[2-(benzyloxy)phenyl](3-fluorophenyl)methoxy}propanoic acid; CHEMBL475562;
|
| 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 |
| 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
|
|---|---|
| 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 | 2.5290 mL | 12.6448 mL | 25.2896 mL | |
| 5 mM | 0.5058 mL | 2.5290 mL | 5.0579 mL | |
| 10 mM | 0.2529 mL | 1.2645 mL | 2.5290 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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