| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
Galectin-3 (Gal-3). Selvigaltin is an orally bioavailable and selective small-molecule inhibitor of galectin-3, a beta-galactoside-binding lectin involved in inflammation, fibrosis, and tumor progression. Selvigaltin displays >100-fold selectivity over galectin-1 and low CYP P450 inhibition. It inhibits galectin-3 expression in human monocyte THP1 cells (IC50=220.3 nM) and reduces TGFbeta-stimulated pro-fibrotic gene expression in human liver stellate cells (LX2).
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| ln Vitro |
Selvigaltin inhibits galectin-3 expression in human monocyte THP1 cells with an IC50 of 220.3 nM and reduces TGFbeta-stimulated pro-fibrotic gene expression in human liver stellate cell line LX2 in vitro. It has a binding Kd of 25 nM in fluorescence polarization assays and displays >100-fold selectivity over galectin-1.
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| ln Vivo |
Selvigaltin (30 mg/kg, p.o., daily for 5 days) reduces the high fat diet (HFD)-induced increase in plasma cholesterol, ALT plasma levels, collagen deposition, fibrosis and normalizes plasma triglycerides levels in HFD rabbits. At 0.3, 1.0, and 5.0 mg/kg p.o. daily for 4 weeks, it reduces AST, ALT, bilirubin levels and HFD-induced increase of inflammation markers, particularly IL6 mRNA. In a mouse CCl4-induced liver fibrosis model, GB1211 (2 or 10 mg/kg twice daily, oral) reduces fibrosis.
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| Enzyme Assay |
Galectin-3 binding is measured using fluorescence polarization (FP) assays. Selvigaltin is incubated with recombinant galectin-3 and a fluorescently labeled lactose probe. The displacement of the probe by the inhibitor reduces polarization, and the Kd (25 nM) is calculated. For enzyme selectivity, Selvigaltin is screened against a panel of 87 targets (enzymes, receptors, ion channels) to confirm no off-target affinity.
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| Cell Assay |
THP1 cells are treated with Selvigaltin at various concentrations, and galectin-3 expression is measured by Western blot or ELISA to determine the IC50 (220.3 nM). LX2 human hepatic stellate cells are stimulated with TGFbeta with or without Selvigaltin, and pro-fibrotic gene expression (e.g., collagen, IL6, TGFbeta3) is measured by qPCR.
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| Animal Protocol |
In the HFD rabbit model of metabolic-associated steatohepatitis, rabbits are fed a high fat diet, then treated orally with Selvigaltin (30 mg/kg, daily for 5 days) to assess acute effects on liver function biomarkers. In the CCl4-induced mouse liver fibrosis model, Selvigaltin (2 mg/kg or 10 mg/kg, twice daily, oral) is administered, and liver fibrosis is assessed by histological staining and biomarker analysis.
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| ADME/Pharmacokinetics |
Selvigaltin (GB1211) is orally bioavailable with a molecular weight of 533.32 and formula C19H16BrF3N4O4S. In DMSO, solubility is 12.5 mg/mL (23.44 mM) with ultrasonic warming to 60degC. In clinical pharmacokinetic studies, the tablet formulation displayed higher bioavailability than the capsule, with minimal food effect. Storage should be at -20degC protected from light.
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| Toxicity/Toxicokinetics |
Selvigaltin is generally well tolerated in clinical and preclinical studies. In healthy participants, the tablet formulation was well tolerated during all treatments. In participants with hepatic impairment, single-dose PK and safety studies have been conducted. However, comprehensive toxicology data are not provided in the reference sources.
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| References | |
| Additional Infomation |
GB1211 is an orally effective galactoglucan-3 (Gal-3) inhibitor.
Selvigaltin (GB1211) is in clinical development as an oral therapy for liver fibrosis and cirrhosis. It is not yet approved by any regulatory agency. The tablet formulation has shown favorable pharmacokinetics and tolerability in clinical trials. The compound also shows anti-tumor activity by restoring T-cell activity and reducing tumor growth and metastasis. It decreases galectin-3 levels in the liver and reduces biomarkers of liver function, inflammation, and fibrosis. |
| Molecular Formula |
C19H16BRF3N4O4S
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|---|---|
| Molecular Weight |
533.32
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| Exact Mass |
532.002
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| CAS # |
1978336-95-6
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| PubChem CID |
122443488
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| Appearance |
White to off-white solid powder
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| LogP |
1.9
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
32
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| Complexity |
625
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| Defined Atom Stereocenter Count |
5
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| SMILES |
C1(F)C(F)=CC(=CC=1F)C1=CN(N=N1)[C@@H]1[C@H]([C@@H](SC2=CN=CC(Br)=C2)O[C@@H]([C@@H]1O)CO)O
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| InChi Key |
FNCLKJPMEFPXOR-QFACEVIFSA-N
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| InChi Code |
InChI=1S/C19H16BrF3N4O4S/c20-9-3-10(5-24-4-9)32-19-18(30)16(17(29)14(7-28)31-19)27-6-13(25-26-27)8-1-11(21)15(23)12(22)2-8/h1-6,14,16-19,28-30H,7H2/t14-,16+,17+,18-,19-/m1/s1
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| Chemical Name |
(2R,3R,4S,5R,6R)-2-(5-bromopyridin-3-yl)sulfanyl-6-(hydroxymethyl)-4-[4-(3,4,5-trifluorophenyl)triazol-1-yl]oxane-3,5-diol
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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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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 : ~12.5 mg/mL (~23.44 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 | 1.8750 mL | 9.3752 mL | 18.7505 mL | |
| 5 mM | 0.3750 mL | 1.8750 mL | 3.7501 mL | |
| 10 mM | 0.1875 mL | 0.9375 mL | 1.8750 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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