WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H121095
CAS#: 1978336-95-6
Description: Selvigaltin, also known as GB0139, is a galectin-3 inhibitor. GB0139 protects against acute lung injury by inhibiting neutrophil recruitment and activation. B0139 decreased inflammation severity via a reduction in neutrophil and macrophage recruitment and neutrophil activation. GB0139 reduced LPS-mediated increases in interleukin (IL)-6, tumor necrosis factor alpha (TNFα) and macrophage inflammatory protein-1-alpha. In vitro, GB0139 inhibited Gal-3-induced neutrophil activation, monocyte IL-8 secretion, T cell apoptosis and the upregulation of pro-inflammatory genes encoding for IL-8, TNFα, IL-6 in alveolar epithelial cells in response to mechanical stretch.
Hodoodo Cat#: H121095
Name: Selvigaltin
CAS#: 1978336-95-6
Chemical Formula: C19H16BrF3N4O4S
Exact Mass: 532.00
Molecular Weight: 533.320
Elemental Analysis: C, 42.79; H, 3.02; Br, 14.98; F, 10.69; N, 10.51; O, 12.00; S, 6.01
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Synonym: Selvigaltin; GB0139; GB-0139; GB 0139
IUPAC/Chemical Name: 5-bromopyridin-3-yl 3-deoxy-1-thio-3-[4-(3,4,5- trifluorophenyl)-1H-1,2,3-triazol-1-yl]-α-Dgalactopyranoside
InChi Key: FNCLKJPMEFPXOR-QFACEVIFSA-N
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
SMILES Code: BrC1=CN=CC(S[C@H]2O[C@H](CO)[C@H](O)[C@H](N3C=C(C4=CC(F)=C(F)C(F)=C4)N=N3)[C@H]2O)=C1
Appearance: To be determined
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 533.32 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Zetterberg FR, MacKinnon A, Brimert T, Gravelle L, Johnsson RE, Kahl-Knutson B, Leffler H, Nilsson UJ, Pedersen A, Peterson K, Roper JA, Schambye H, Slack RJ, Tantawi S. Discovery and Optimization of the First Highly Effective and Orally Available Galectin-3 Inhibitors for Treatment of Fibrotic Disease. J Med Chem. 2022 Oct 13;65(19):12626-12638. doi: 10.1021/acs.jmedchem.2c00660. Epub 2022 Sep 26. PMID: 36154172; PMCID: PMC9574852.
2: Tabel M, Wolf A, Szczepan M, Xu H, Jägle H, Moehle C, Chen M, Langmann T. Genetic targeting or pharmacological inhibition of galectin-3 dampens microglia reactivity and delays retinal degeneration. J Neuroinflammation. 2022 Sep 17;19(1):229. doi: 10.1186/s12974-022-02589-6. PMID: 36115971; PMCID: PMC9482176.
3: Humphries DC, Mills R, Boz C, McHugh BJ, Hirani N, Rossi AG, Pedersen A, Schambye HT, Slack RJ, Leffler H, Nilsson UJ, Wang W, Sethi T, Mackinnon AC. Galectin-3 inhibitor GB0139 protects against acute lung injury by inhibiting neutrophil recruitment and activation. Front Pharmacol. 2022 Aug 8;13:949264. doi: 10.3389/fphar.2022.949264. PMID: 36003515; PMCID: PMC9393216.
4: Gaughan EE, Quinn TM, Mills A, Bruce AM, Antonelli J, MacKinnon AC, Aslanis V, Li F, O'Connor R, Boz C, Mills R, Emanuel P, Burgess M, Rinaldi G, Valanciute A, Mills B, Scholefield E, Hardisty G, Findlay EG, Parker RA, Norrie J, Dear JW, Akram AR, Koch O, Templeton K, Dockrell DH, Walsh TS, Partridge S, Humphries D, Wang-Jairaj J, Slack RJ, Schambye H, Phung D, Gravelle L, Lindmark B, Shankar- Hari M, Hirani N, Sethi T, Dhaliwal K. An Inhaled Galectin-3 Inhibitor in COVID-19 Pneumonitis: A Phase Ib/IIa Randomized Controlled Clinical Trial (DEFINE). Am J Respir Crit Care Med. 2023 Jan 15;207(2):138-149. doi: 10.1164/rccm.202203-0477OC. PMID: 35972987; PMCID: PMC9893334.
5: Humphries DC, Mills R, Dobie R, Henderson NC, Sethi T, Mackinnon AC. Selective Myeloid Depletion of Galectin-3 Offers Protection Against Acute and Chronic Lung Injury. Front Pharmacol. 2021 Aug 30;12:715986. doi: 10.3389/fphar.2021.715986. PMID: 34526900; PMCID: PMC8435800.
6: Kumar A, Paul M, Panda M, Jayaram S, Kalidindi N, Sale H, Vetrichelvan M, Gupta A, Mathur A, Beno B, Regueiro-Ren A, Cheng D, Ramarao M, Ghosh K. Molecular mechanism of interspecies differences in the binding affinity of TD139 to Galectin-3. Glycobiology. 2021 Nov 18;31(10):1390-1400. doi: 10.1093/glycob/cwab072. PMID: 34228782.
7: St-Gelais J, Denavit V, Giguère D. Efficient synthesis of a galectin inhibitor clinical candidate (TD139) using a Payne rearrangement/azidation reaction cascade. Org Biomol Chem. 2020 May 27;18(20):3903-3907. doi: 10.1039/d0ob00910e. PMID: 32400847.
