Synonym
SPL-334; SPL334; SPL 334
IUPAC/Chemical Name
4-[[2-[(2-Cyanophenyl)methylsulfanyl]-4-oxothieno[3,2-d]pyrimidin-3-yl]methyl]benzoic acid
InChi Key
UWWSCLNCHCROLL-UHFFFAOYSA-N
InChi Code
InChI=1S/C22H15N3O3S2/c23-11-16-3-1-2-4-17(16)13-30-22-24-18-9-10-29-19(18)20(26)25(22)12-14-5-7-15(8-6-14)21(27)28/h1-10H,12-13H2,(H,27,28)
SMILES Code
O=C(O)C1=CC=C(CN(C(SCC2=CC=CC=C2C#N)=NC3=C4SC=C3)C4=O)C=C1
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
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
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
Biological target:
SPL-334 causes a significant reduction in the production of Th2 cytokines IL-5 and IL-13 and the levels of the chemokine CCL11 (eotaxin-1) in the airways.
In vivo activity:
SPL-334 shows promise as a potential therapeutic agent for interstitial lung disease (ILD). In a mouse model of ILD induced by bleomycin, daily administration of SPL-334 showed no toxicity and prevented weight loss and cellular changes induced by bleomycin. When administered therapeutically, SPL-334 reduced weight loss, cellular changes, and collagen accumulation in the lungs, accompanied by decreased levels of profibrotic cytokines.
Reference: J Pharmacol Exp Ther. 2015 Oct;355(1):13-22. https://pubmed.ncbi.nlm.nih.gov/26209236/
|
Solvent |
mg/mL |
mM |
comments |
Solubility |
DMSO |
20.0 |
46.14 |
|
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
433.50
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:
1. Luzina IG, Lockatell V, Todd NW, Kopach P, Pentikis HS, Atamas SP. Pharmacological In Vivo Inhibition of S-Nitrosoglutathione Reductase Attenuates Bleomycin-Induced Inflammation and Fibrosis. J Pharmacol Exp Ther. 2015 Oct;355(1):13-22. doi: 10.1124/jpet.115.224675. Epub 2015 Jul 24. PMID: 26209236.
2. Ferrini ME, Simons BJ, Bassett DJ, Bradley MO, Roberts K, Jaffar Z. S-nitrosoglutathione reductase inhibition regulates allergen-induced lung inflammation and airway hyperreactivity. PLoS One. 2013 Jul 25;8(7):e70351. doi: 10.1371/journal.pone.0070351. PMID: 23936192; PMCID: PMC3723687.
In vivo protocol:
1. Luzina IG, Lockatell V, Todd NW, Kopach P, Pentikis HS, Atamas SP. Pharmacological In Vivo Inhibition of S-Nitrosoglutathione Reductase Attenuates Bleomycin-Induced Inflammation and Fibrosis. J Pharmacol Exp Ther. 2015 Oct;355(1):13-22. doi: 10.1124/jpet.115.224675. Epub 2015 Jul 24. PMID: 26209236.
2. Ferrini ME, Simons BJ, Bassett DJ, Bradley MO, Roberts K, Jaffar Z. S-nitrosoglutathione reductase inhibition regulates allergen-induced lung inflammation and airway hyperreactivity. PLoS One. 2013 Jul 25;8(7):e70351. doi: 10.1371/journal.pone.0070351. PMID: 23936192; PMCID: PMC3723687.
1: Luzina IG, Lockatell V, Todd NW, Kopach P, Pentikis HS, Atamas SP. Pharmacological In Vivo Inhibition of S-Nitrosoglutathione Reductase Attenuates Bleomycin-Induced Inflammation and Fibrosis. J Pharmacol Exp Ther. 2015 Oct;355(1):13-22. doi: 10.1124/jpet.115.224675. Epub 2015 Jul 24. PubMed PMID: 26209236.
2: Ferrini ME, Simons BJ, Bassett DJ, Bradley MO, Roberts K, Jaffar Z. S-nitrosoglutathione reductase inhibition regulates allergen-induced lung inflammation and airway hyperreactivity. PLoS One. 2013 Jul 25;8(7):e70351. doi: 10.1371/journal.pone.0070351. PMID: 23936192; PMCID: PMC3723687.
3: Hayashida K, Bagchi A, Miyazaki Y, Hirai S, Seth D, Silverman MG, Rezoagli E, Marutani E, Mori N, Magliocca A, Liu X, Berra L, Hindle AG, Donnino MW, Malhotra R, Bradley MO, Stamler JS, Ichinose F. Improvement in Outcomes After Cardiac Arrest and Resuscitation by Inhibition of S-Nitrosoglutathione Reductase. Circulation. 2019 Feb 5;139(6):815-827. doi: 10.1161/CIRCULATIONAHA.117.032488. PMID: 30586713; PMCID: PMC6361681.